U.S. patent application number 13/736358 was filed with the patent office on 2013-05-30 for compositions and methods for promoting weight loss and increasing energy.
This patent application is currently assigned to NORTHERN INNOVATIONS AND FORMULATIONS CORP.. The applicant listed for this patent is Northern Innovations and Formulations Corp.. Invention is credited to James Akrong, Phil Apong, John Doherty.
Application Number | 20130136810 13/736358 |
Document ID | / |
Family ID | 45556338 |
Filed Date | 2013-05-30 |
United States Patent
Application |
20130136810 |
Kind Code |
A1 |
Doherty; John ; et
al. |
May 30, 2013 |
COMPOSITIONS AND METHODS FOR PROMOTING WEIGHT LOSS AND INCREASING
ENERGY
Abstract
The present invention relates to compositions comprising plants
and extracts of plants with chlorogenic acids and antioxidants
and/or caffeine; methods for preparing the same; and methods to
promote weight loss through the administration of compositions
containing these plants and plant extracts in specific
proportions.
Inventors: |
Doherty; John; (Oakville,
CA) ; Apong; Phil; (Oakville, CA) ; Akrong;
James; (Oakville, CA) |
|
Applicant: |
Name |
City |
State |
Country |
Type |
Northern Innovations and Formulations Corp.; |
Oakville |
|
CA |
|
|
Assignee: |
NORTHERN INNOVATIONS AND
FORMULATIONS CORP.
Oakville
CA
|
Family ID: |
45556338 |
Appl. No.: |
13/736358 |
Filed: |
January 8, 2013 |
Related U.S. Patent Documents
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Application
Number |
Filing Date |
Patent Number |
|
|
12849076 |
Aug 3, 2010 |
8372447 |
|
|
13736358 |
|
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Current U.S.
Class: |
424/738 ;
424/725 |
Current CPC
Class: |
A61K 36/534 20130101;
A61K 36/534 20130101; A61K 36/9066 20130101; A61K 36/48 20130101;
A61K 36/889 20130101; A61K 36/899 20130101; A61K 36/28 20130101;
A61K 36/258 20130101; A61K 36/889 20130101; A61K 36/45 20130101;
A61K 36/899 20130101; A61P 3/04 20180101; A61K 2300/00 20130101;
A61K 2300/00 20130101; A61K 2300/00 20130101; A61K 2300/00
20130101; A61K 2300/00 20130101; A61K 2300/00 20130101; A61K
2300/00 20130101; A61K 36/258 20130101; A61K 2300/00 20130101; A61K
36/9066 20130101; A61K 36/28 20130101; A61K 36/48 20130101; A61K
36/45 20130101 |
Class at
Publication: |
424/738 ;
424/725 |
International
Class: |
A61K 36/28 20060101
A61K036/28 |
Claims
1-23. (canceled)
24. A comestible composition, comprising an extract of Smallanthus
sonchifolius, at least one substance for increasing energy and at
least one fibre.
25. The composition of claim 24, wherein the fibre is
water-soluble.
26. The composition of claim 25, wherein the water-soluble fibre is
selected from the group consisting of Plantago ovata, Avena sativa,
Cichorium intybus and mixture thereof.
27. The composition of claim 26, wherein the at least one substance
for increasing energy is Lepidium meyenii, Pytchopetalum olacides
or a mixture thereof.
28. The composition of claim 24, further comprising Gentiana lutea
or an extract thereof.
29. The composition of claim 25, further comprising Gentiana lutea
or an extract thereof.
30. The composition of claim 26, further comprising Gentiana lutea
or an extract thereof.
31. The composition of claim 27, further comprising Gentiana lutea
or an extract thereof.
Description
FIELD OF THE INVENTION
[0001] The present invention relates to novel methods and
compositions comprising chlorogenic acids for promoting weight
loss, for the treatment of obesity, managing weight gain, or
maintenance of normal body weight and for increasing energy of an
individual participating in a weight loss regimen.
BACKGROUND OF THE INVENTION
[0002] Obesity is one of the most common medical disorders and
affects about 30-40% of the population of the United States, 10% of
which may be severe and morbid. Complications of obesity include
insulin resistance, diabetes mellitus (and its complications,
including oxidative stress), hypertension, cardiovascular disease,
hyperlipidemia, sleep apnea, cancer, pulmonary hypertension,
cholecystitis, and osteoarthritis are major reasons for medical
intervention. The mortality from obesity is estimated at 300,000 to
400,000 per annum in the United States. The exact etiology of
obesity is unknown but occurs when energy intake exceeds energy
expenditure.
[0003] One main contributing factor in obesity is overeating, which
results in an excess of energy being consumed in relation to the
amount of energy expended by an individual. The excess energy is
then stored largely as fat. An individual's body weight is
essentially governed by the net effect of energy consumed versus
energy expended. Daily energy expenditure consists of three
components: basal metabolic rate, adaptive thermogenesis and
physical activity. All of the aforementioned components must be in
a balance of energy expenditure in an individual with energy or
food intake so that an individual does not gain nor lose body
weight. Therefore, for that person to lose body weight from a
reduction in adipose tissue, more energy must be expended by the
individual than taken into the body.
[0004] Losing weight and keeping it off is very difficult for most
individuals. Weight gain results when an individual's caloric
intake exceeds the number of calories expended as energy. In
attempting to lose weight, an individual may utilize a regimen of
caloric deficit (i.e. decreasing caloric intake so that calories
expended as energy exceed caloric intake). Generally, the result is
an adaptive response of a lowered basal (resting) metabolic rate.
Caloric deficit can also cause a loss of skeletal muscle. Thus,
weight loss or reducing caloric intake results in a lowering of
resting energy expenditure and loss of lean body mass. This makes
it harder to keep the weight off once the individual has attained
his desired weight goal.
[0005] When the body encounters an energy deficit in the course of
weight-reducing diets, it tends to save energy by reducing
thermogenesis. This factor contributes to a failure in sustaining
body weight after body weight loss. These circumstances require
continually stimulated thermogenesis. After losing weight for a
short duration, an individual's weight stabilizes. In order to
maintain body weight there is a need to control food intake,
stimulate thermogenesis and increase energy levels on an ongoing
basis.
[0006] Some undesired effects encountered by individuals desiring
to loss weight include fatigue, low energy, and a lack of
motivation and/or depression.
[0007] Another undesired effect of increased accumulation of body
fat is an increased oxidative stress through the generation of
reactive oxygen species and the downregulation of antioxidative
enzymes. This downregulation of antioxidative enzymes can
contribute to the pathogenesis of diabetes, hypertension and
atherosclerosis. Thus it is desirable to provide an individual
means to reduce stored body fat and simultaneously offer protection
from reactive oxygen species.
[0008] Increased oxidative stress due to increased body fat is
thought to be an early contributor to hypertension, coronary heart
disease, type 2 diabetes mellitus, stroke and even some forms of
cancer and is therefore an attractive target strategy for combating
the negative effects of excessive body fat while aiming to reduce
the volume of stored body fat in an individual.
[0009] With the unprecedented rise in obesity throughout the world,
there exists both a need and want from individuals for improved
aids, methods and interventions directed to reducing body fat and
maintaining lowered levels of body fat, while also supplying
beneficial antioxidant activity.
[0010] While not necessarily obese, many individuals who are
overweight can also suffer from many similar conditions known to be
associated with obesity including, among others, poor self-esteem
and low self-confidence, poor dietary and exercise habits, lack of
energy and anxiety. Many of these individuals would benefit from
the prevention or correction some of these conditions if they were
able to prevent weight gain and/or maintain a normal body
weight.
[0011] Therefore, there is a need to provide individuals
compositions useful for increasing energy and promoting weight
loss, for the treatment of obesity, prevention of weight gain or
maintenance of normal body weight and increasing energy.
SUMMARY OF THE INVENTION
[0012] The present invention provides for a dietary supplement that
provides any one or more of the following benefits: help reduce and
control appetite; help control food cravings; help reduce hunger
cravings; help induce feeling of fullness (satiety); promote and
support weight loss; help reduce body mass index (BMI); help reduce
waist and thigh measurements; increase metabolism; increase
thermogenesis; and increase energy.
[0013] In aspects, the present invention relates to methods and
compositions that utilize plants and/or portions thereof containing
chlorogenic acids.
[0014] According to another aspect of the invention, the dietary
supplement further comprises at least one substance for increasing
energy.
[0015] According to another aspect of the invention, the dietary
supplement further comprises at least one thermogenic
substance.
[0016] According to another aspect of the invention, the dietary
supplement further comprises at least one satiety-promoting
ingredient.
[0017] According to another aspect of the invention, the dietary
supplement further comprises at least one antioxidant.
[0018] According to another aspect of the invention, the dietary
supplement further comprises at least one prebiotic.
[0019] According to another aspect of the invention, the dietary
supplement further comprises at least one probiotic.
[0020] According to another aspect of the invention, the dietary
supplement further comprises at least one substance that decreases
harmful cholesterol.
[0021] According to an aspect of the invention, there is provided a
dietary supplement comprising Smallanthus sonchifolius and/or
Phyllostachys edulis.
[0022] In aspects of the invention, extracts are obtained from the
Smallanthus sonchifolius and/or Phyllostachys edulis.
[0023] The compositions of the invention may further comprise
various Smallanthus sonchifolius and/or Phyllostachys edulis and
extracts thereof, Smallanthus sonchifolius and/or Phyllostachys
edulis combined with different amounts of biologically active small
molecules or other therapeutic agents. The compositions of the
present invention are particularly useful for promoting weight loss
and/or the treatment of obesity.
[0024] The present invention is further directed to a weight loss
composition useful for treatment of obesity, comprising as an
active component an effective amount of at least one specific
chlorogenic acid extracted from Smallanthus sonchifolius and/or
Phyllostachys edulis and at least one substance for increasing
energy.
[0025] The present invention is further directed to a weight loss
composition useful for treatment of obesity, comprising as an
active component an effective amount of at least one specific
chlorogenic acid extracted from Smallanthus sonchifolius and/or
Phyllostachys edulis, at least one substance for increasing energy
and at least one antioxidant and/or at least one thermogenic
substance and methods of using same.
[0026] The present invention is further directed to a weight loss
composition useful for treatment of obesity, comprising as an
active component an effective amount of at least one specific
chlorogenic acid extracted from Smallanthus sonchifolius and/or
Phyllostachys edulis, at least one substance for increasing energy,
at least one antioxidant, at least one thermogenic substance and at
least one prebiotic and/or probiotic and methods of using same.
[0027] The present invention is further directed to the weight loss
composition for promoting weight loss in an individual in need
thereof.
[0028] The present invention is further directed to methods for
promoting weight loss by administering the weight loss composition
to an individual in need thereof.
[0029] The present invention is further directed to the use of the
weight loss composition in the preparation of a medicament for
promoting weight loss in an individual in need thereof.
[0030] The present invention is further directed to methods for
promoting weight loss by administering the combination of raw
plants and standardized plant extracts in specific proportions.
[0031] Specific embodiments of the present invention are understood
to comprise tubers and/or leaves of Smallanthus sonchifolius and/or
Phyllostachys edulis; methods for preparing the same; and methods
of preparing a dietary supplement to aid in body fat loss, promote
lipolysis while affording protection against reactive oxygen
species resulting from the .beta.-oxidation of fats.
[0032] In another particular aspect of the present invention, there
is provided a weight loss composition useful for treatment of
obesity, comprising as an active component an effective amount of
at least one specific chlorogenic acid extracted from Smallanthus
sonchifolius and/or Phyllostachys edulis, and a physiologically
acceptable carrier, at least one substance for increasing energy
and/or at least one antioxidant and methods of using same.
[0033] In another embodiment of the present invention using
Smallanthus sonchifolius and/or Phyllostachys edulis extracts,
Smallanthus sonchifolius and/or Phyllostachys edulis extracts
comprise about 1% to about 99% by weight of the composition. In a
preferred embodiment, Smallanthus sonchifolius and/or Phyllostachys
edulis extracts comprise about 10% to about 60% by weight of the
composition. In a more preferred embodiment, Smallanthus
sonchifolius and/or Phyllostachys edulis extracts comprise about
20% to about 50% by weight of the composition.
[0034] In an embodiment, the composition of the invention comprises
Smallanthus sonchifolius and/or Phyllostachys edulis extract
present in an amount of about 35% to about 40% by weight at least
one substance for increasing energy and/or a thermogenic substance.
Alternatively, the compositions of the invention can be
administered sequentially or simultaneously in combination with at
least one substance for increasing energy and/or a thermogenic
substance.
[0035] In an embodiment, the composition of the invention comprises
Smallanthus sonchifolius and/or Phyllostachys edulis extract having
at least 1% chlorogenic acids by weight.
[0036] In an embodiment, the composition of the invention comprises
Smallanthus sonchifolius and/or Phyllostachys edulis extract
comprises about 20 to 90% chlorogenic acids by weight and about 5
to 40% 5-caffeoylquinic acid by weight.
[0037] In an embodiment, the composition of the invention comprises
Smallanthus sonchifolius and/or Phyllostachys edulis extract
comprises about 45% chlorogenic acids by weight and about 10%
5-caffeoylquinic acid by weight.
[0038] According to in an embodiment of the invention is a
comestible composition comprising an extract of Smallanthus
sonchifolius and/or Phyllostachys edulis and at least one substance
for increasing energy wherein the extract of Smallanthus
sonchifolius and/or Phyllostachys edulis comprises at least one
specific chlorogenic acid, in an amount of at least 5% by weight.
And according to in an embodiment of the invention the at least one
specific chlorogenic acid is 5-caffeoylquinic acid.
[0039] In another aspect, the dietary supplement comprises phenolic
acids selected from the group consisting of caffeic, chlorogenic,
rosamarinic and ferrulic. More preferably, the compositions include
at least 5% chlorogenic acids by weight of the composition;
preferably including at least 10% chlorogenic acids by weight of
the composition. Most preferably, the compositions are obtained
from the extraction of Smallanthus sonchifolius and/or
Phyllostachys edulis parts with an aqueous organic solution
mixture, in particular a water and ethanol solution mixture,
comprising small molecule compounds.
[0040] In another aspect, the dietary supplement comprises phenolic
acids selected from the group consisting of caffeic, chlorogenic,
rosamarinic and ferrulic. More preferably, the compositions include
at least 5% chlorogenic acids by weight of the composition;
preferably including at least 10% chlorogenic acids by weight of
the composition. Most preferably, the compositions are obtained
from the extraction of Smallanthus sonchifolius and/or
Phyllostachys edulis plant parts with an aqueous organic solution
mixture, in particular a water and ethanol solution mixture,
comprising small molecule compounds.
[0041] In another aspect, the dietary supplement comprises about
100 to 700 mg Smallanthus sonchifolius and/or Phyllostachys edulis
extract and about 100 to 700 mg caffeine.
[0042] In another aspect, the dietary supplement comprises about
150 to 400 mg Smallanthus sonchifolius and/or Phyllostachys edulis
extract.
[0043] In another aspect, the dietary supplement comprises about
200 to 400 mg Smallanthus sonchifolius and/or Phyllostachys edulis
extract and about 100 to 700 mg caffeine.
[0044] In another aspect, the dietary supplement comprises about
200 mg Smallanthus sonchifolius and/or Phyllostachys edulis extract
and 200 mg caffeine.
[0045] In another aspect, the dietary supplement comprises about
200 mg Smallanthus sonchifolius extract and/or Phyllostachys edulis
extract (containing about 45% by weight chlorogenic acids and about
5% by weight 5-caffeoylquinnic acid), about 200 mg of a substance
for increasing energy in a capsule or tablet.
[0046] The Smallanthus sonchifolius or Phyllostachys edulis
extracts obtained according to an aspect of the present invention
have at least 1% by weight total phenolics, preferably at least 20%
by weight total phenolics, and most preferably at least 40% by
weight total phenolics.
[0047] One aspect of the invention comprises a composition
containing about 100 to 700 mg Smallanthus sonchifolius or
Phyllostachys edulis with 1-90% by weight chlorogenic acids.
[0048] One aspect of the invention comprises a composition
comprising about 150 to 400 mg Smallanthus sonchifolius or
Phyllostachys edulis extract containing about 5% to 70% by weight
chlorogenic acids and about 100 to 700 mg caffeine.
[0049] In another aspect, the dietary supplement comprises about
200 mg Smallanthus sonchifolius or Phyllostachys edulis extract and
about 100 to 700 mg caffeine.
[0050] In another aspect, the dietary supplement comprises about
200 mg Smallanthus sonchifolius or Phyllostachys edulis extract and
200 mg caffeine.
[0051] In another aspect, the extract of Smallanthus sonchifolius
or Phyllostachys edulis comprises about 45 to 50% chlorogenic acids
by weight and about 5 to 15% 5-caffeoylquinic acid by weight and
the caffeine contains about 10% to 100% by weight
1,3,7-trimethylxanthine.
[0052] In another aspect, the Smallanthus sonchifolius or
Phyllostachys edulis extract contains about 45% by weight
chlorogenic acids and about 5% by weight 5-caffeoylquinnic
acid.
[0053] Specific embodiments of the present invention are understood
to function in the capacity of a dietary supplement to aid in body
fat loss, lipolysis while affording protection against reactive
oxygen species resulting from the .beta.-oxidation of fats.
DETAILED DESCRIPTION OF THE EMBODIMENTS
[0054] As used herein, unless otherwise specified, the term "manage
weight gain" includes, but is not limited to, treating, preventing
or reducing weight gain, suppressing appetite.
[0055] As used herein, unless otherwise specified, the term
"preventing," includes, but is not limited to, inhibition or the
averting of symptoms associated with a particular disease or
disorder.
[0056] As used herein, unless otherwise specified, the term
"treating" refers to the administration of the composition after
the onset of symptoms of the disease or disorder whereas
"preventing" refers to the administration prior to the onset of the
symptoms, particularly to patients at risk of the disease or
disorder.
[0057] As used herein, unless otherwise specified, the term "obese"
includes, but is not limited to, a person having a Body Mass Index
(BMI) of greater than or equal to about 26.
[0058] As used herein, unless otherwise specified, the term
"average weight" or "of average weight" includes, but is not
limited to, a person having a Body Mass Index (BMI) of less than
about 26.
[0059] As used herein, the term "thermogenic" refers to an
ingredient, which increases energy expenditure, also known as
metabolic rate. It is the process of burning stored body fat. The
certain thermogenic ingredient may also have a property of inducing
satiety.
[0060] The term "standardized" as used in the field of naturally
derived nutritional products refers to the process for delivering a
product with a specific minimum level of one or more plant
constituents. Standardization represents the level of concentration
of particularly desired elements from a plant source. Methods for
standardizing plant substances are well known in the art.
Furthermore, the measurement of particular plant constituents on
which standardization is based is also well known in the art.
[0061] The term "about" when used as a modifier of a numerical
range or amount designates an approximation of the range or the
amount whereby minor deviations from the range or amount are within
the scope of the invention. Such deviations are known in the art of
manufacturing formulations having a number of different ingredients
of varying weight and consistency.
[0062] The term "effective amount" shall be understood to mean an
amount or quantity of the composition that is required to cause the
metabolic effects described herein. This amount is readily
determined by observation both before and after administration of
the compositions described herein.
[0063] Unless specified otherwise, the term "% by weight" as used
herein with reference to the standardized extract denotes the
percent of the total weight of the extract contributed by the
active component. This theoretical value can differ from the
experimental value, because in practice, the extract typically may
retain some of the water and/or other substances such as alcohols
(e.g., ethanol) that may be used in preparing the final product. In
addition, the chemical composition of the plant material from a
particular plant may vary with, for example, the conditions under
which the plant is grown (e.g., soil or climate).
[0064] The term "% by weight of the composition" as used herein
shall be understood to denote the percentage of the dietary
ingredients in the composition useful for supplementing the diet of
an individual.
[0065] A particular compound or mixture of compounds can exhibit
pharmacological activity over a readily ascertainable range of
compositions and dosages. Therefore it will be understood that the
percentages by weight recited throughout are meant to include such
variations outside the stated percentages or percentage ranges as
would be expected by one skilled in the art.
[0066] As used herein, unless otherwise specified, the term
"physiologically acceptable carrier," includes, but is not limited
to, a carrier medium that does not interfere with the effectiveness
of the biological activity of any active ingredients, is chemically
inert, and is not toxic to the consumer or patient to whom it is
administered.
[0067] As used herein, unless otherwise specified, the term
"pharmaceutically acceptable salts" refers to salts prepared from
pharmaceutically acceptable non-toxic acids and bases, including
inorganic and organic acids and bases.
[0068] It has now been shown that various raw botanicals and
various extracts of raw botanical materials in the specific
proportions reduce and control appetite; help induce feeling of
satiety; promote and support weight loss; help reduce body mass
index (BMI); help reduce waist and thigh measurements; increase
metabolism; increase thermogenesis; and increase energy.
[0069] Phenolic compounds, widely distributed in food plants, act
as primary antioxidants and thus may be beneficial for improving
and/or preventing a number of chronic diseases. Phenolic compounds
occur in nature as mixtures of esters, ethers, or free acids.
[0070] A major class of phenolic compounds are the hydroxycinnamic
acids, which are found in almost every existing plant. Caffeic,
ferulic and p-coumaric acids are trans-cinnamic acids that occur
naturally in their free forms or as a family of mono or diesters
with (-)-quinic acid, collectively known as chlorogenic acids.
Chlorogenic acids are antioxidant components produced by plants in
response to environmental stress conditions such as infections by
microbial pathogens, mechanical wounding, and excessive UV or
visible light levels. The main classes of chlorogenic acids found
in nature are the caffeoylquinic acids, dicaffeoylquinic acids,
and, less commonly, feruloylquinic acids, each group with at least
three isomers. The term "chlorogenic acid" comprises
3-caffeoylquinic acid, 4-caffeoylquinic acid, 5-caffeoylquinic
acid, 3,4-dicaffeoylquinic acid, 3,5-dicaffeoylquinic acid,
4,5-dicaffeoylquinic acid, 3-feruloylquinic acid, 4-feruloylquinic
acid, 5-feruloylquinic acid, 3-feruloyl-4-caffeoylquinic acid and
other structural isomeric chlorogenic acids such as
3-O-(3'-methylcaffeoyl)quinic acid, 5-O-caffeoyl-4-methylquinic
acid and 3-O-caffeoyl-1-methylquinic acid or mixtures thereof.
[0071] Phenolic compounds are known to be anti-tumor agents.
Chlorogenic acid has been shown to exert cancer preventive
activities in animal models. Chlorogenic acid, an ester of caffeic
acid and quinic acid, is an antioxidant in vitro and is suspected
to be beneficial in preventing cardiovascular disease. Also,
chlorogenic acid has shown to have a chemopreventative effect on
rat stomach cancer, and to inhibit methylazoxymethanol induced
large intestinal tumors in hamsters. Other beneficial properties
such as hypoglycaemic, antiviral and hepatoprotective activities
have been also attributed to chlorogenic acids in in vitro and in
vivo and epidemiological studies.
[0072] Chlorogenic acid, the main phenolic acid in coffee, is able
to protect the gastric mucosa against irritations, and, therefore,
improves the digestibility of foods, beverages and medicaments. The
improved digestibility is expressed through a much reduced systemic
acid secretion (such as causes heartburn, etc.) which has been
found to be directly dependent on an increased level of chlorogenic
acid content in roasted coffee.
[0073] The chlorogenic acids of the present invention are not
particularly limited, and, for instance, those commercially
available, or those prepared from various plants in accordance with
known methods can be used. Organically synthesized chlorogenic acid
can be used in addition to or in place of the botanical
extract.
[0074] It is now believed that certain dietary polyphenolic
compounds, in addition to their antioxidant activities, may alter
glucose metabolism. For instance, recent studies have linked heavy
regular use of coffee to decreased risk for type 2 diabetes. The
actions of caffeine seem unlikely to mediate this effect since it
has been observed in those who use decaffeinated coffee. Caffeic
acid, the hydrolytic product of chlorogenic acid, is known to have
antidiabetic effects in streptozotocin-induced diabetic rats.
Therefore, it is reasonable to expect that chlorogenic acids and/or
caffeic acid in coffee may be responsible for these effects.
[0075] In vivo experiments studying the effects of chlorogenic acid
have shown that it is able to arrest the proliferation of
3T3-preadipocyte cells in the G1 phase of development in a time-
and dose-dependant manner. It is understood by the inventors that
chlorogenic acid administration in vivo would translate into an
inhibition of adipocytes differentiation and proliferation,
resulting in a net reduction in adipose tissue.
[0076] Interestingly, in addition to the inhibitory effects of
chlorogenic acid on preadipocyte proliferation, it has been
suggested that chlorogenic acid decreases the intestinal rate of
glucose absorption. Chlorogenic acid has also been shown to
selectively inhibit hepatic glucose-6-phosphatase (G-6-P), the
rate-limiting step in gluconeogenesis and decrease hepatic
triglyceride levels in mice following 14 days of administration.
Chlorogenic acid may also reduce glucose release from the liver
which is often abnormally high in individuals with obesity,
[0077] It has been shown that about 33% of orally administered
chlorogenic acid is absorbed in the small intestine of humans and
it is understood by the inventors that chlorogenic acid not only
inhibits adipose tissue proliferation but it also inhibits of
glucose absorption.
[0078] Chlorogenic acids, ferulic acid in particular, are also
known to directly act on nitric oxide derived from the vascular
endothelium. It is believed that this will support flow mediated
vasodilation and delivery of nutrients via the systemic circulatory
system.
[0079] According to an aspect of the present invention is the
standardization of the total phenolics, chlorogenic acids, and the
entire plant extract. The standardized extracts have better
batch-to-batch consistency. They may also have higher amounts of at
least one specific chlorogenic acid.
[0080] There is also a need for plant extracts that have been
standardized to the presence of specific markers. Further there is
a need for methods of preparing these extracts, as well as for
compositions containing these extracts. There is also a need for
methods to promote weight loss and/or the treatment of obesity
and/or weight maintenance. According to an aspect of the present
invention is the standardization of the total phenolics,
chlorogenic acids, and the entire extract. The standardized
extracts have better batch-to-batch consistency. They also have
higher amounts of at least one specific chlorogenic acid. The
inventive extracts can be standardized according to at least one
assay. The extracts can be standardized by quantifying the
concentration of total phenolics. The extracts can also be
standardized by quantifying the concentration of specific
chlorogenic acids.
[0081] The present invention further relates to an extract that has
been standardized based on the concentration of individual specific
chlorogenic acids. Specific chlorogenic acids may be assayed using
High Performance Liquid Chromatography ("HPLC"). HPLC is known to
those skilled in the art. Total phenolics can be assayed using the
Folin-Ciocalteu ("FC") method and is known to those skilled in the
art.
[0082] The extraction process may be carried out using methods
known in the art, including but not limited to solvent extraction,
percolation, vat extraction, or countercurrent extraction. The
degree of comminutation of the plant material prior to the
extraction process should provide sufficient particulate surface
for the extraction solvent to contact the material. Extraction may
be at ambient temperature or at elevated temperature. The resulting
extract solution is then dried to substantially remove the
solvent.
[0083] Chlorogenic acids may be extracted from the raw botanical
material according to any known methods. The present invention
further relates to a method of preparing an extract from leaves
which comprises: treating a mass of plant material with a solvent
suitable for extracting at least one chlorogenic acid to yield an
extract solution; concentrating the extract solution to an extent
necessary to provide a minimum desirable concentration of the
active component for promoting weight loss, and; standardizing the
extract to yield a known amount of at least one specific
chlorogenic acid.
[0084] The extraction process according the present invention may
be carried out using suitable solvents selected from water, and
organic solvents with or without water. Suitable organic solvents
include but are not limited to non-toxic aqueous or non-aqueous
monohydric or polyhydric alcohols, hexane, methylene glycol,
glycerin, and similar solvents known to those in the art. Other
extraction methods such as use of super-critical CO.sub.2 may also
be used. Preferably an aqueous solvent having at least 10%
volume/volume ("v/v") of an alcohol is used in the extraction, more
preferably at least 30% v/v of an alcohol, and most preferably at
least 50% v/v of an alcohol. The preferred alcohols are ethanol and
methanol.
[0085] The concentration of total phenolics as well as certain
specific phenolic markers is increased if the plant mass is
freeze-dried after harvesting and before extraction or processing.
In an aspect of the invention, the plant parts such as the bean,
stems, leaves, or flowers are freeze-dried before extraction.
Freeze-drying can be done immediately upon harvesting the plant. Or
the harvested plant can immediately be frozen and then freeze-dried
within at least 30 days.
[0086] The extracts obtained according to an aspect of the present
invention have at least 1% by weight total phenolics, preferably at
least 20% by weight total phenolics, and most preferably at least
40% by weight total phenolics.
[0087] Yacon (Smallanthus sanchifolius) is an Asteraceae from the
Andean areas that grows in zone of not more than 3,000 meters of
altitude and the culture of which has expanded to other latitudes.
In Peru it is found especially in humid temperate areas in Andean
slopes, in dry inter-Andean valleys, as well as in the coast. Both
the tubercle and the leaves improve lipid profile as well as
intestinal absorption of calcium. The tuberous roots of yacon
accumulate almost 10%, based on the fresh weight, of inulin type
fructooligosaccharides (FOSs), which are known as food ingredients
with health benefits, the main saccharide being
beta-1,2-oligofructane.
[0088] Phyllostachys, a genus of bamboo and more particularly,
Phyllostachys edulis, is the largest of all temperate bamboos and
produces edible shoots. The leaves of bamboo have been used in
Asian countries as a food wrapping material to prevent food
deterioration since ancient times. The leaves have been used in the
clinical treatment of hypertension, arteriosclerosis,
cardiovascular disease, and certain forms of cancer.
[0089] In particular, the present invention relates to a
standardized extract of Smallanthus sonchifolius or Phyllostachys
edulis, which comprises at least one specific cholorogenic acid, in
an amount of at least 1% by weight based on the total weight of the
extract. In a preferred embodiment the chlorogenic acid is in an
amount of at least 5% by weight based on the total weight of the
extract. In a more preferred embodiment, in an amount of at least
10% by weight. In a most preferred embodiment of the present
invention, the total phenolics are present in an amount of at least
20% by weight.
[0090] The present invention further relates to a method of
preparing an extract from Smallanthus sonchifolius or Phyllostachys
edulis. This mass is subjected to an extraction process that is
effective in concentrating at least one specific chlorogenic acid.
The extract is then dried. The extract is then standardized
according to the invention. The extract can further be combined
with fillers, excipients, binders and the like to form a
composition suitable for administration for the treatment of
obesity.
[0091] In one specific method leaves of Smallanthus sonchifolius or
Phyllostachys edulis are dried and comminuted and then extracted
first with petroleum ether and next with hot water, until the
extracts contain no more chlorogenic acid. The combined extracts
are concentrated and precipitated with barium acetate. Then the
filtrate is precisely neutralized with sulphuric acid, the excess
barium being removed at the same time. The chlorogenic acid is
separated from the neutral filtrate by means of lead acetate as a
complex, which is washed with hot water and to which hydrogen
sulphide is then added after suspension in hot water. After
standing in a refrigerator for two to three days, the
potassium-caffeine-chlorogenate complex separates from the
concentrated filtrate. Caffeine is removed from the complex by
chloroform and then the free chlorogenic acid is obtained by weak
acidification.
[0092] In particular, in one embodiment of the invention, the
extraction steps are as follows: a) Smallanthus sonchifolius is
harvested during the early flowering season, when the amount of at
least one specific phenolic marker is at its peak. b) The bean,
stems, flowers, or leaves of the plant are immediately frozen to
prevent fermentation, or are immediately freeze-dried. The frozen
plant mass is freeze dried within one month of harvest.
Freeze-drying is done at minimal heat. c) The freeze-dried material
is pulverized to optimal particle size for percolation extraction.
d) The pulverized material is then extracted and solid material is
removed using the percolation method of extraction, in an
ethanol/water solution wherein the ethanol is preferably 10% v/v,
more preferably 30% v/v, and most preferably 50% v/v. e) The
resulting extract is then dried and concentrated.
[0093] One aspect of the invention is a composition comprising
Smallanthus sonchifolius or Phyllostachys edulis with a substance
for increasing energy. In aspects, the substance for increasing
energy is Lepidium meyenii and/or Ptychopetalum olacoides. Lepidium
meyenii (Brassicaceae), known as Maca or Peruvian ginseng, is a
perennial crop of Peru. For centuries, the Andean Indians have
utilized maca as a food and for its pharmacological properties; for
example to enhance fertility. As a food source, maca displays a
high nutritional value and is rich in sugars, protein, starches and
minerals. It has a fleshy, edible, tuberous root macca that has
been domesticated for at least 2000 years in the Andean Mountains
at an altitude more than 10,000 feet. Dried maca root is rich in
amino acids, iodine, iron, and magnesium. Traditionally maca root
has been used in the Andean region for its supposed aphrodisiac
and/or fertility-enhancing properties and energy-increasing
properties. Another species is Lepidium peruvianum.
[0094] Muira puama (Ptychopetalum olacoides) is a remedy for sexual
impotence as wells as treating neuromuscular problems, rheumatism,
influenza, cardiac and gastrointestinal asthenia and to prevent
baldness. Muira puama also significantly inhibits
anti-cholinesterase activity in vitro in a dose- and time-dependent
manner in rat frontal cortex, hippocampus and striatum suggesting
improvement in facilitate memory retrieval.
[0095] An established component of obesity is abnormal fat
metabolism, specifically, the breakdown of fat, or lipolysis. Body
fat, stored as triglycerides in adipose tissue, is hydrolyzed to
free fatty acids and glycerol through the process of lipolysis. In
fat cells (adipocytes) lipolysis is controlled by adrenergic
signaling and signaling through adenosine receptors. Typically,
stimulation of beta-adrenergic receptors increases lipolysis,
whereas stimulation of adenosine A1 receptors inhibits lipolysis.
The specific effects of stimulation or inhibition of either
adrenergic or adenosine receptors depends on the cell- or
tissue-type involved and the precise panel of receptors expressed
and the downstream signaling connectivity.
[0096] Caffeine is a naturally occurring xanthine alkaloid found in
some plants where it serves as a natural pesticide. In humans,
however, it may have numerous beneficial effects, the most common
of which uses caffeine as a supplement to the central nervous
system. In this capacity, it is used as a stimulant and performance
enhancer. Weight loss related to caffeine supplementation has been
observed in obese women and may be, at least in part, due to
increased lipolysis. Caffeine has additionally been shown to
increase the basal metabolic rate.
[0097] While caffeine is structurally similar to adenosine, it
binds to, but does not activate, adenosine receptors which are
normally activated by adenosine to induce sleep. Thus, caffeine is
a stimulant. By antagonizing certain adenosine receptors, caffeine
has the effect of increasing levels of intracellular cyclic AMP
(cAMP), an important signaling molecule involved in many metabolic
processes including thermogenesis. Caffeine also increases cAMP
levels by inhibiting phosphodiesterases which degrade cAMP. These
actions of caffeine lead to an increase in the release of
epinephrine and norepinephrine. Since epinephrine and
norepinephrine use cAMP for signaling, increased levels of cAMP
will increase adrenergic signaling and thereby inducing
lipolysis.
[0098] In aspects, the caffeine comprises 1,3,7-trimethylxanthine.
In another aspect 1,3-dimethylxanthine or 3,7-dimethylxanthine can
be substituted for 1,3,7-trimethylxanthine.
[0099] Cirsimarin is a flavonoid extracted from several plants
including Microtea debilis (Phytolaccaceae), an herb native to
South America, which is thought to be involved in various
pharmacological activities within the human body. Research suggests
that cirsimarin may be a lipolytic agent due to its antagonist
effects on both adenosine A1 and A2 receptors and inhibitory
effects on the enzyme phosphodiesterase. Phosphodiesterases are the
main enzymes involved in the hydrolysis of the signaling molecule,
cAMP, and have inhibitory effects on lipolysis. It is known that
adenosine receptor activation acts to inhibit lipolysis. Therefore
it will be understood that by inhibiting phosphodiesterase and
inhibiting adenosine receptors, the inhibition of lipolysis is
removed and fat burning is promoted. Use of cirsimarin is
contemplated because it stimulates lipolysis and promote weight
loss by acting as a lipolytic agent due to its antagonism of
adenosine receptors and its inhibition of phosphodiesterase.
[0100] Antioxidants are of great interest because they may help to
protect the body against damage by reactive oxygen species (ROS).
Studies have shown that free radicals present in the human organism
cause oxidative damage to different molecules, such as lipids,
proteins and nucleic acids, and thus are involved in the initiation
phase of some degenerative illnesses. The ROS superoxide anion
radical (O.sub.2), hydrogen peroxide (H.sub.2O.sub.2), hypochlorous
acid (HOCl) and hydroxyl radical (HO.sup.-) have been implicated in
the pathophysiology of various disorders; those antioxidant
compounds, which are capable of neutralizing free radicals or ROS,
may play a major role in the prevention of certain diseases, such
as cancer, diabetes, cataracts, cerebral pathologies and rheumatoid
arthritis.
[0101] Wolfberries, the common name for Lycium barbarum, also
called Goji berries are a nutritionally rich fruit originally grown
in Europe and now cultivated in China. Lycium barbarum contain all
8 essential amino acids, as well as 21 trace minerals and a variety
of vitamins. In traditional Chinese medicine they have been used in
for nearly 2,000 years. In support of these traditional properties
assigned to Lycium barbarum, recent studies indicate that extracts
from Lycium barbarum fruit possess a range of biological
activities, including effects on aging, neuroprotection,
antifatigue/endurance, increased metabolism, glucose control in
diabetics, glaucoma, antioxidant properties, immunomodulation,
antitumor activity, and cytoprotection. Its reddish-orange color is
derived from a group of carotenoids, which make up only 0.03-0.5%
of the dried fruit. The predominant carotenoid is zeaxanthin,
comprising about one-third to one-half of the total
carotenoids.
[0102] Other chemical constituents found in Lycium barbarum fruit
include small molecules such as betaine, cerebroside,
beta-sitosterol, p-coumaric acid, and various vitamins. Other minor
components include glutamine; asparagine; stigmasterol;
cholest-7-enol; campesterol; cholestanol; 24-methylene cholesterol;
28-isofucosterol; 24-methylcholesta-5,24-dienol;
24-ethylcholesta-5,24-dienol; 31-norcycloartanol;
31-norcycloartenol; cycloeucalenol; obtusifoliol;
4a,14a,24-trimethylcholesta-8'24-dienol; 4a-methylcholest-8-enol;
4-methylcholest-7-enol; 24-ethyllophenol; 4,24-methyllophenol;
gramisterol; citrostadienol;
4a-methyl-24-ethylcholesta-7,24-dienol; lanost-8-enol;
cycloartanol; lanosterol; b-amyrin; lupeol;
24-methylenelanost-8-enol; 24-methylenecycloartanol; taurine and
-aminobutanoic acid.
[0103] It is understood that the polysaccharide extracts which
contain six monosaccharides (Ara, Rha, Xyl, Man, Gal, and Glc),
galacturonic acid, and 18 amino acids, and share a Glycan-O-Ser
glycopeptide structure, provides benefits such as enhancing the
immune system function, improving eyesight, protecting the liver,
boosting sperm production, and improving circulation in an
individual. The use of Lycium barbarum polysaccharides in the
treatment of age-related oxidative stress in mice has been shown to
improve the total antioxidant capacity as well as improved immune
function. Furthermore, the same study also illustrated that the
antioxidant activity of the wolfberries could be increased with
co-treatment of vitamin C.
[0104] Acerola (Malpighia emarginata) one of the richest sources of
vitamin C (L-ascorbic acid) an is also known as Barbados cherry,
West Indian cherry, Puerto Rican cherry, Antilles cherry, cereso,
cereza, cerisier, and semeruco is a fruit which has been used to
treat dysentery, diarrhea, and liver disorders. Other
ethnobotanical uses include as an astringent and for fever. Acerola
is also used for preventing heart disease, "hardening of the
arteries" (atherosclerosis), blood clots, and cancer.
[0105] Vitamin C, or L-ascorbic acid, is an essential nutrient
required in small amounts in order to allow a range of essential
metabolic reactions in animals and plants. Since the body does not
make or store vitamin C, humans are required to ingest it in their
daily diets. Ascorbic acid is a strong antioxidant and protects the
body from oxidative stress, as well as acting as a coenzyme in
necessary enzymatic reactions. As a strong antioxidant and
anti-inflammatory molecule, ascorbic acid has been shown to protect
against the common cold.
[0106] Cactus pear (Opuntia ficus-indica) fruit contains vitamin C
and characteristic betalain pigments, the radical-scavenging
properties and antioxidant activities. Consumption of cactus pear
fruit positively affects the body's redox balance, decreases
oxidative damage to lipids, and improves antioxidant status in
healthy humans. Supplementation with vitamin C at a comparable
dosage enhances overall antioxidant defense.
[0107] Blueberries are a group of flowering plants in the genus
Vaccinium. The species are native to North America and eastern Asia
and contain a high amount of anthocyanins, potent antioxidants.
[0108] Anthocyanins are the colorful flavonoids concentrated in
brightly colored berries and fruit ("anthos" means "flower" and
"cyan" means "blue") being most concentrated in bilberries,
blueberries, cranberries, elderberries, purple grapes, red wine and
hawthorn berries. Flavonoids have been reported to demonstrate
their benefits in lowering oxidative stress and also have
beneficial effects on cardiovascular and chronic inflammatory
diseases.
[0109] Anthocyanin extracts are important for the health of the
micro-blood vessel network and prevent blood platelet stickiness
better than aspirin. Anthocyanins bind to and stabilize collagen
and elastin; they stabilize the phospholipids of endothelial cells
and increase synthesis of collagen and mucopolysaccharides, which
give the arterial walls structural integrity.
[0110] Anthocyanins also inhibit the proliferation of human cancer
cell lines in vitro, an effect attributed to their antioxidant
activity. Anthocyanins induce the secretion of insulin from rodent
pancreatic .beta.-cells, the cells normally responsible for insulin
secretion, which are the cells compromised in diabetes. Ingested
anthocyanins have been shown to be detectable in the plasma and
brain as intact molecules 10 minutes after ingestion by rats and to
be excreted in the urine of both rats and humans. Antioxidant
supplementation can reduce the markers of cellular damage.
Therefore, supplemental with antioxidants should benefit any
nutritional and exercise program.
[0111] Bilberries, Vaccinium myrtillus [Fam. Ericaceae], otherwise
known as European blueberries, huckleberry or whortleberry are rich
in anthocyanins. Bilberry has traditionally been used in herbal
medicine as an astringent to help relieve diarrhea. Bilberry
anthocyanin extracts are beneficial for the cardiovascular system
have strong antiplatelet aggregating activity. Bilberry leaf
constituents prevent the release and synthesis of pro-inflammatory
compounds such as histamine, prostaglandins, and leukotrienes and
bilberry anthocyanins also support the lymphatic system and prevent
bacteria from adhering to the bladder wall. Bilberry extracts also
exert potent protective action on LDL particles during
copper-mediated oxidation.
[0112] Blueberries, Vaccinium corybosum and other and other
blueberry species including Vaccinium alaskensis, Vaccinium
membranaceum and Vaccinium ovalifolium [Fam. Ericaceae], are also
rich anthocyanins.
[0113] Carotenoids are isoprenic compounds that are naturally
occurring in plants. There are over 600 known carotenoids split
into two classes: xanthophylls and carotenes. The 6 major
carotenoids are: alpha-carotene, beta-carotene, lycopene
(carotenes); beta-cryptoxanthin, zeaxanthin and lutein
(xanthophylls). Zeaxanthin is found in many vegetables and fruits,
particularly green leafy vegetables such as kale and spinach.
Zeaxanthin is widely known as a nutrient for protecting ocular
function. It has long been thought that carotenoid intake also
reduces the risk of certain forms of cardiovascular disease,
stroke, and cancer. Zeaxanthin and its stereoisomer lutein, may
prevent cellular damage in these conditions by quenching singlet
oxygen or neutralizing photosensitizers.
[0114] Acai berries (Euterpe oleracea) are a rich source of
anthocyanin and polyphenolic compounds, essential fatty acids, and
vitamins. Cyanidin-3-glucoside is the main anthocyanin (1,040 mg/L
of acai berry juice), as well as 16 other polyphenolics at levels
ranging from 4 to 212 mg/L. Total anthocyanin content is 3.2 mg/g
freeze-dried acai berry samples on a dry weight basis where
cyanidin-3-glucoside and cyanidin-3-rutinoside are the predominant
anthocyanins. Resveratrol, albeit at very low levels, fatty acids,
mainly oleic and palmitic acids can also be found in acai berry.
Plasma antioxidant capacity of 2.3- and 3-fold is observed for acai
juice and pulp after the consumption.
[0115] Gentian root and rhizome, Gentiana lutea L. [Fam.
Gentianaceae], otherwise known as Bitter Root may have
anti-inflammatory activity in addition to antioxidant activities
such as hydroxyl radical scavenging.
[0116] Schisandrin B is a dibenzocyclooctadiene compound that is
isolated from Schisandrae chinensis. Schisandrin has been used to
enhance the detoxification of xenobiotics in the liver and assist
in liver regeneration. Recent studies have shown that schisandrin
can protect various organs from free-radical induced damage.
[0117] Furthermore, it is known that oxidized low density
lipoprotein (LDL) is a key factor in the initiation of
atherosclerosis, one of the pathological processes involved in
cardiovascular and cerebrovascular disease. LDL expresses numerous
adhesion molecules that appear to enhance the binding of monocytes
to aortic endothelium, where they may become transformed into foam
cells and initiate atherosclerosis. Research has shown that
zeaxanthin can inhibit thickening of the walls of carotid arteries
and LDL-induced migration of monocytes to human artery cell walls.
It is believed that carotenoids for the ability to scavenge free
radicals and inhibit lipid peroxidation in cardiovascular and
cerebrovascular disease.
[0118] Phytosterols have cholesterol-lowering properties by
reducing cholesterol absorption in intestines. The most abundant
phytosterols (beta-sitosterol, campesterol, and stigmasterol)
differ from cholesterol only in the identity of one side chain or
the presence of an extra double bond. Cholesterol and phytosterol
are very similar and the human body is not able to distinguish
between them and therefore, phytosterols compete with cholesterol
for absorption in the small intestine. A non-limiting list of
phytosterols includes sitosterol, campesterol, sigmasterol,
brassicasterol, sitostanol and campestanol.
[0119] Olive leaf comes from the olive tree (Olea europaea).
Although olives and olive oil are used as foods, olive leaf is
primarily used medicinally or as a tea. Olive leaf helps to
maintain a healthy metabolism as well as lowering cholesterol and
blood pressure in people with mild hypertension. According to an
aspect of the invention, olive corresponding to about 500 mg to
about 1 g dried plant is used. Preferably, olive corresponding to
450 mg dried plant is used.
[0120] Alfalfa (Medicago sativa) [Fam. Leguminosae] may have
cholesterol-lowering effects. Alfalfa is also extremely rich in
antioxidants, including one powerful antioxidant called tricin, and
is a source of chlorophyll and carotene.
[0121] Oat bran, Avena sativa L. [Fam. Gramineae], is rich in
protein, approximately 30%, and contains all the essential amino
acids along with chlorophyll, flavonoids, lecithin and enzymes.
This abundance of nutrients has made it popular for treating
debility. It is also extremely rich in antioxidants, including
polyphenols and one powerful antioxidant called tricin. It also
contains beta-glucan, which has been shown to stimulate immune
functions.
[0122] Angelica (Angelica archangelica) belongs to the family
Umbelliferae. Angelica is said to be `ginseng` for women and is
recommended by many as a daily beauty tonic, to prevent hormonal
imbalances and treat menstrual difficulties (Amenorrhea) and is
recommended for the prevention of vascular disease. Angelica root
is a source of bitters and aromatics that stimulate gastric and
pancreatic secretion. Polysaccharide extract from the root Angelica
has been studied for its liver protective effect in rodents and has
been found to prevent liver toxicity caused by acetaminophen in
mice without reducing the serum acetaminophen concentration. It
also normalized enzyme activities and levels including alanine
transferase (ALT), hepatic nitric oxide synthase (NOS) and
glutathione in the liver.
[0123] Evening primrose oil [Gen. Oenothera] has been shown to
decrease the risk of heart disease by lowering cholesterol and by
decreasing the risk of blood clots (decreased platelet
aggregation).
[0124] The flowers of calendula, Calendula officinalis [Fam.
Asteraceae], contain high concentrations of colorful orange
xanthophylls, carotenoids and other flavonoids that are powerful
antioxidants and the flavonoid extract has been shown
scientifically to be effective against inflammation, fever and to
stimulate bile flow for aiding digestion and cleansing the
liver.
[0125] Choline is a constituent of phosphatidylcholine (PC), which
is a component of cell walls and membranes. It is involved in fat
and cholesterol metabolism and transport. In this form, choline
aids in fat metabolism and transport away from the liver.
[0126] Ginseng (American ginseng, Asian ginseng, Chinese ginseng,
Korean red ginseng, Panax ginseng) appears to have antioxidant
effects that may benefit patients with heart disorders. Studies
suggest that ginseng also reduces oxidation of low-density
lipoprotein (LDL or "bad") cholesterol and brain tissue. Several
studies report that ginseng may boost the immune system, improve
the effectiveness of antibiotics in people with acute bronchitis,
and enhance the body's response to flu vaccines.
[0127] Pomegranate (Punica granatum) delivers approximately 40% of
an adult's daily vitamin C requirement and is high in polyphenolic
compounds. Juice of the pomegranate was effective in reducing heart
disease risk factors, including LDL oxidation, macrophage oxidative
status, and foam cell formation all of which are believed to be
involved in atherosclerosis and cardiovascular disease. Consumption
of pomegranate juice for two weeks was shown to reduce systolic
blood pressure by inhibiting serum angiotensin-converting enzyme
(ACE).
[0128] Inosine (also known as hypoxanthine riboside,
hypoxanthosine, 2,3-diphosphoglycerate, 6-9
dihydro-9-B-D-ribofuranosyl-1H-purin-6-one,
9-B-D-ribofuranosylhypoxanthine) and primarily used in the
treatment for various forms of heart disease. Inosine monophosphate
is a precursor for adenine, a nucleotide and purine base that
reacts with ribose to form adenosine. Adenosine is a nucleoside
that can be phosphorylated to produce adenosine monophosphate
(AMP), the diphosphate (ADP), the triphosphate (ATP) and cyclic
adenosine monophosphate (cAMP).
[0129] Gamma oryzanol is a mixture of ferulic acid esters of
sterols and triterpene alcohols extracted from rice bran oil and
other grain oils such as corn and barley. Ferulic acid compounds
also are present in many foods, including oats, berries, citrus
fruits, tomatoes, olives, and vegetables. Gamma oryzanol is an
important antioxidant within plant cells.
[0130] Turmeric (Curcuma longa), a perennial herb and member of the
Zingiberaceae (ginger) as is used as an anti-inflammatory and for
the treatment of flatulence, jaundice, menstrual difficulties,
hematuria, hemorrhage and colic. The active constituents of
turmeric are the flavonoid curcumin (diferuloylmethane) and various
volatile oils, including tumerone, atlantone, and zingiberone.
Other constituents include sugars, proteins, and resins. There is
about 0.3-5.4 percent of curcumin in raw turmeric. Water- and
fat-soluble extracts of turmeric and its curcumin component exhibit
strong antioxidant activity, comparable to vitamins C and E.
Turmeric has been found to have a hepatoprotective characteristic
similar to silymarin. Turmeric's hepatoprotective effect is
primarily due to its antioxidant properties, as well as its ability
to decrease the formation of pro-inflammatory cytokines.
[0131] Turmeric's protective effects on the cardiovascular system
include lowering cholesterol and triglyceride levels, decreasing
susceptibility of low density lipoprotein (LDL) to lipid
peroxidation and inhibiting platelet aggregation. Turmeric
extract's effect on cholesterol levels may be due to decreased
cholesterol uptake in the intestines and increased conversion of
cholesterol to bile acids in the liver. Inhibition of platelet
aggregation by turmeric's constituents is thought to be via
potentiation of prostacyclin synthesis and inhibition of
thromboxane synthesis.
[0132] Ficus carica has antioxidant properties and is used to treat
constipation, bronchitis, high cholesterol, eczema, psoriasis
(chronic skin disease) and vitiligo (white skin patches).
[0133] Sunflower (Helianthus annuus) (Asteraceae) oil is rich in
linoleic acid (omega-6), oleic acid (omega-9) and Vitamin E.
[0134] Bayberry (Myrica cerifera) (Myricaceae) stimulates lymphatic
drainage and encourages the healing of mucus membranes. The primary
chemical constituents of bayberry include essential oils,
triterpenes (taraxerol, taraxaxerone, myricadol), flavonoids
(myricitrin), phenols, starch, myrica wax (palmitic acid, stearic
acid, myristic acid) lignin, albumin, gum, tannins and gallic acid.
Bayberry is also been shown to alleviate arthritic pain.
[0135] Inulin (Cichorium intybus) is a type of naturally occurring
fructose-containing oligosaccharide present in various fruits and
vegetables such as onions, garlic, wheat, leeks, garlic, bananas,
asparagus, and artichokes. Typically, inulin contains 2 to 150
fructose units which are linked by beta-(2-1) glycosidic bond with
a terminal glucose. Inulin is resistant to digestion in the upper
gastrointestinal tract and is fermented by the colonic bacteria,
promoting intestinal bacteria and possibly acting as a mild
laxative. In the colon, inulin is metabolized into short-chain
fatty acids-acetate, propionate, and butyrate, lactic acids, and
gases (e.g., hydrogen sulfide, carbon dioxide, and methane). Inulin
is also reported to possess anti-tumor, antimicrobial,
hypolipidemic, hypoglycemic, and antiosteoporotic effects and
enhance mineral absorption and balance. Inulin from roots of
chicory and Jerusalem artichokes are marketed as nutritional
supplements and functional foods. Nutritionally, it is considered a
form of soluble fibre. It is herein understood that inulin will act
to benefit digestion by enhancing nutrient absorption, by promoting
intestinal bacteria, and by mild laxative activity.
[0136] Inulin type fructooligosaccharides can be found in other
plants. Smallanthus sonchifolius is also cultivated for its tubers,
which are consumed mainly as a "fruit". In contrast with most
edible roots, Smallanthus sonchifolius stores its carbohydrates in
the form of beta-(2-1) fructooligosaccharides (FOS). FOS are sugars
found naturally in many types of plants but never in concentrations
as high as in Smallanthus sonchifolius roots. FOS are able to
resist the hydrolysis of enzymes in the upper part of the human
gastrointestinal tract. For this reason, they have a low caloric
value for humans.
[0137] Smallanthus sonchifolius FOS are completely fermented in the
colon by bacteria that form part of the intestinal microflora.
These bacteria (especially of the genus Bifidus and Lactobacillus)
improve the gastrointestinal function. In this regard, FOS
functions as a prebiotic. Prebiotics are an alternative for
probiotics or their cofactors. As non-digestible or low-digestible
food ingredients that benefit the host organism by selectively
stimulating the growth or activity of one or a limited number of
probiotic bacteria in the colon. This role is played by fermentable
carbohydrates, which are not digested or poorly digested in the
small intestine and stimulate, preferentially, the growth of
bifidobacteria and some Gram-positive bacteria, belonging to the
probiotic bacteria administered to humans.
[0138] Smallanthus sonchifolius tubers show an important effect by
producing a positive balance of calcium and magnesium, and thus
obtaining a greater osseous mineral retention. FOS aid in digestion
and prevent and control constipation. The sub-chronic use for 4
months of yacon root flour in male rats was well tolerated and did
not show adverse effects or toxicity at a daily dose of 340 mg and
6800 mg FOS. Under these conditions, the triglyceride levels
decreased, although no effects on glycemia were observed. It does
not appear that the hypoglycemic effect of yacon is due to a lower
intestinal absorption of glucose.
[0139] In one specific method yacon tubers are frozen (-20.degree.
C.) immediately after harvest. The frozen tubers are then cut into
smaller parts and homogenized in a homogenizer for 30 s. Ten grams
of yacon tubers are transferred into a 100 mL volumetric flask and
filled with water. The extraction mixtures is ultrasonicated for 15
min and filtered. Three milliliters of the filtrates may be
pipetted into 10 mL volumetric flasks and filled with methanol.
Saccharide analysis of the tubers can be performed using techniques
familiar to those skilled in the art. For example, extracts of
yacon tubers can be analyzed for sugar content using
high-performance thin-layer chromatography (HPTLC).
[0140] According to an aspect of the present invention is a syrup
composition obtained from the tubers of Smallanthus sonchifolius.
The syrup may be obtained from Smallanthus sonchifolius tubers
according to methods known to those skilled in the art. For
example, harvested tubers which contain about 40 to 70% FOS, 5 to
15% sucrose, 5 to 15% fructose and less than 5% glucose are juiced
and filtered. The juice generally has an initial concentration of
sugars in the range from 8 to 13.degree. Brix. Removal of water via
evaporation and concentration can increase the concentration to
about 50 to 70.degree. Brix.
[0141] In addition to prebiotics such as inulin and FOS, the use of
probiotics is also contemplated. Probiotics are defined as
selected, viable microbial dietary supplements beneficially affect
the organism through their effects in the intestinal tract. Some
strains of Lactobacillus, Bifidobacterium and Saccharomyces, for
example have been promoted in food products because of their
reputed health benefits.
[0142] The physiological effects related to probiotic bacteria
include the reduction of gut pH, production of some digestive
enzymes and vitamins, production of antibacterial substances, e.g.,
organic acids, bacteriocins, hydrogen peroxide, restoration of
normal intestinal microflora after diarrhea, antibiotic therapy and
radiotherapy, reduction of cholesterol level in the blood,
stimulation of immune functions, suppression of bacterial
infections and removal of carcinogens.
[0143] Psyllium is a water-soluble fiber derived from the husks of
ripe seeds from Plantago ovata. Psyllium is widely used as a fiber
supplement for the treatment of constipation. Psyllium husk is
obtained by milling the seed of P. ovata to remove the hulls.
Psyllium husk contains a high proportion of hemicellulose, composed
of a xylan backbone linked with arabinose, rhamnose, and
galacturonic acid units (arabinoxylans). The seed consists of
35-percent soluble and 65-percent insoluble polysaccharides
(cellulose, hemicellulose, and lignin). Psyllium is classified as a
mucilaginous fiber due to its powerful ability to form a gel in
water. This ability comes from its role as the endosperm of the P.
ovata seed, where it functions to retain water in order to prevent
the seed from drying out. Psyllium also has hypocholesterolemic
effects, although the exact mechanism by which psyllium husk brings
about a reduction of cholesterol is not totally clear. Animal
studies have shown psyllium increases the activity of cholesterol 7
alpha-hydroxylase (the rate-limiting enzyme in bile acid synthesis
also referred to as cytochrome 7A [CYP7A]) more than twice that of
cellulose or oat bran. Psyllium may also have an effect on
appetite.
[0144] Caralluma is a cactus-like plant that grows abundantly in
areas of Asia, the south Mediterranean, and parts of Africa.
Caralluma is a cactus that has historical use as an appetite
suppressant during times of famine in India and Africa. In India,
the plant is boiled and eaten whole but elsewhere only the green
follicles are consumed. The name of the plant varies between
regions and in addition to caralluma, it is also known as:
Ranshabar, Maked shenguli, and Shindala makad.
[0145] Caralluma is reported to have anti-inflammatory,
anti-nociceptive, anti-hyperglycemic, anti-ulcer, cytoprotective
and appetite suppressant properties. In addition to the
anti-hyperglycemic and appetite suppressant properties, caralluma
or an extract thereof may have other activities conducive to
maintaining or reducing weight such as the blocking the activity of
the fat synthesis enzyme, citrate lyase. The phytochemical
constituents of caralluma include various glycosides (pregnane,
flavone and megastigmane glycosides), bitter principles, saponins
and various flavanoids.
[0146] There are a number of species of caralluma including but not
limited to: C. fimbriata, C. indica, C. attenuata, C. tuberculata,
C. edulis, C. adscendens, C. stalagmifera, C. umbellata, C.
penicillata, C. russeliana, C. retrospiciens, C. arabica and C.
lasiantha.
[0147] It is herein understood that inclusion of Caralluma or an
extract thereof in a composition will support the maintenance or
reduction of body weight in a subject by at least reducing
appetite. It is further understood that Caralluma may further
support the maintenance or reduction of body weight in a subject by
antagonizing fat synthesis by blocking citrate lyase.
[0148] Cumin (Cuminum cyminum) is native from the eastern
Mediterranean area to eastern India. It is used as a medicinal herb
and in cooking throughout the Middle East, North Africa, South
Asia, and parts of southern Europe. Evidence suggests that cumin
may have antibacterial properties and has been used as a diuretic
(increases urine production), dyspeptic (relieves indigestion),
carminative (prevents gas), stimulant, astringent and eases
digestion. According to an aspect of the invention, cumin
corresponding to about 500 mg to about 1 g dried plant is used.
Preferably, cumin corresponding to 384 mg dried plant is used.
[0149] Lady's mantle (Alchemilla vulgaris) is a perennial herb
found in Europe, North America, and Asia that has been used
medicinally since the Middle Ages. It helps maintain body weight.
According to an aspect of the invention, lady's mantle
corresponding to about 500 mg to about 1 g dried plant is used.
Preferably, Lady's mantle corresponding to 690 mg dried plant is
used.
[0150] Wild mint (Mentha longifolia) is known for the treatment of
colic, menstrual disorders, indigestion, flatulence, pulmonary
infection and congestion, headache, fever, cough, colds and urinary
tract infections. It also stimulates the flow of bile to the
stomach and relaxes the digestive tract muscles. According to an
aspect of the invention, wild mint corresponding to about 500 mg to
about 1 g dried plant is used. Preferably, wild mint corresponding
to 324 mg dried plant is used.
[0151] A water extract of the common white kidney bean (Phaseolus
vulgaris) inhibits digestive enzyme alpha-amylase in vitro.
Alpha-amylase, secreted in saliva and by the pancreas, is
responsible for breaking down starch to simple sugars that are
absorbed in the small intestine. Blocking this digestive enzyme may
prevent the digestion of complex carbohydrates, allowing them to
pass through the digestive system. The end result of blocking
alpha-amylase would logically be a decrease in the number of
calories absorbed, potentially promoting weight loss.
[0152] Chromium, an essential trace mineral and cofactor to
insulin, enhances insulin activity and has been the subject of
studies assessing its effects in carbohydrate, protein, and lipid
metabolism. Reported effects include an increase in lean body mass,
a decrease in percentage body fat, and an increase in the basal
metabolic rate. Chromium picolinate is an organic compound of
trivalent chromium and picolinic acid, a naturally occurring
derivative of tryptophan
[0153] Calcium carbonate is a colorless or white crystalline
compound, CaCO.sub.3, occurring naturally as chalk, limestone,
marble, and other forms and used in a wide variety of manufactured
products including dentifrices and medicines.
[0154] Although the present invention is not to be limited by any
theoretical explanation, it is believed that increased calcium
intake has a significant effect on body weight and body fat.
Studies show a consistent effect of higher calcium intakes,
expressed as lower body fat and/or body weight, and reduced weight
gain at midlife. Specifically, calcium may assist in weight loss,
weight management, regulation of metabolism, and the breakdown of
fat. Studies show that increasing dietary calcium speeds up weight
and fat loss. In a comparison trial, both the diets, either high in
calcium or low in calcium, produced significant weight and fat
loss. Weight and fat loss with respect to the high dairy diet were
approximately 2-fold higher (p<0.01), and loss of lean body mass
was markedly reduced (p<0.001) compared with the low dairy diet.
This study purports to show that employing calcium-rich foods in
isocaloric diets reduced adiposity and improved metabolic profiles
in obese African Americans. Additionally, calcium carbonate
facilitates the prevention and treatment of calcium deficiencies,
and thereby facilitates bone formations and maintenance.
[0155] Furthermore, it is known that that an isocaloric
substitution of yogurt (diary) for other foods can significantly
reduce central adiposity during energy restriction and therefore
augment fat loss. This was purportedly shown by the use of control
subjects (400-500 mg Ca/day), or yogurt diet (1100 mg Ca/day) with
the dairy macronutritents controlled to the United States average
values. After 12 weeks, fat loss was markedly increased in the
yogurt group, and mean tissue loss was also increased in the yogurt
group by 31%. Compared to the control group, an 81% increase in
trunk fat loss was also purported to be seen in the yogurt group,
this resulted in decrease in waist diameter in yogurt group. It has
been shown that calcium and dairy supplementation accelerated fat
and weight loss during a 24 week controlled study. Subjects on
high-dairy diet (1200-1300 mg Ca/day) reportedly lost 70% more
weight than those on the standard diet of 400-500 mg Ca/day and
subjects on the calcium enriched, but non-dairy diet lost on 26%
more weight than those on the standard diet. Therefore, this study
purports to show that calcium supplementation significantly
increases weight loss and that calcium supplementation from diary
sources exerts a substantially greater effect of the weight and fat
loss.
[0156] It is believed that a high calcium diet in the form of dairy
products or as calcium carbonate may be useful in inducing the loss
of adipose tissues via stimulating lipolysis, inhibiting
lipogenesis, and increasing the expression of uncoupling protein 2
in white adipose tissue.
[0157] Vitamin D is a steroid hormone, known to have an important
role in regulating body levels of calcium and phosphorus, and in
mineralization of bone. Vitamin D is particularly important for the
absorption of calcium from the stomach and for the functioning of
calcium in the body. Thus, vitamin D is particularly important for
strong bones and teeth. Vitamin D is also known as cholecalciferol,
which is generated in the skin of animals when light energy is
absorbed by a precursor molecule 7-dehydrocholesterol.
Cholecalciferol is used as a dietary supplement to treat and/or
prevent low levels of vitamin D in the body. Although the present
invention is not to be limited by any theoretical explanation, it
is believed that vitamin D is highly involved in mineral
metabolism, as well as bone growth and function. It has been shown
that vitamin D effectively facilitates intestinal absorption of
calcium, and stimulates absorption of phosphate and magnesium ions.
In the absence of vitamin D, dietary calcium may not be absorbed
efficiently. Vitamin D stimulates the expression of a number of
proteins involved in transporting calcium from the lumen of the
intestine, across the epithelial cells and into blood.
[0158] Vitamin B3 (Niacin) also known as or nicotinic acid is one
of several water-soluble B-family vitamins. Niacin is often
consumed as a nutritional dietary supplement in the form of a
multi-vitamin/mineral complex to improve general health. As a
supplement in itself, niacin has long been successfully used to
improve blood lipid profiles. Xanthinol nicotinate is one of
several forms of Niacin (vitamin B3) and is considered the most
potent form of Niacin. Xanthinol nicotinate is classified as a
vasodilator. In patients with peripheral arterial obliterative
disease, xanthinol nicotinate was found to have anti-platelet and
thrombolytic actions accompanied by an increase in the release of
NO. Xanthinol nicotinate may also have the effects of enhancing
cellular metabolism and increasing oxygen supply which may be the
mechanism of improvements in both short- and long-term memory.
[0159] Compositions of the present invention may be formulated for
administration to any suitable subject to promote weight loss. In a
preferred embodiment, the subject is a mammal and even more
preferably, the mammal is a human.
[0160] The administration may be by any conventional route such as
oral, rectal, or nasal. Thus the composition may be a tablet,
capsule, suspension, emulsion, solution, suppository or spray. The
compositions may take the form of, for example, tablets or capsules
prepared by conventional means with pharmaceutically acceptable
excipients such as binding agents (e.g., pregelatinized maize
starch, polyvinyl pyrrolidone or hydroxypropyl methylcellulose);
fillers (e.g., lactose, microcrystalline cellulose or calcium
hydrogen phosphate); lubricants (e.g., magnesium stearate, talc or
silica); disintegrants (e.g., potato starch or sodium starch
glycolate); or wetting agents (e.g., sodium lauryl sulphate).
Non-limiting examples of binders include starch, and sugars such as
sucrose, glucose and dextrose. Non-limiting examples of
disintegrators include corn and potato starch, methylcellulose,
agar, and bentonite. Non-limiting examples of coloring agents
include any of the approved certified water-soluble FD&C dyes
and mixtures of the same.
[0161] Tablets provided in accordance with the present invention
may be uncoated or they may be coated by known techniques. In a
preferred embodiment, the pharmaceutical composition may take the
form of a capsule or powder to be dissolved in a liquid for oral
consumption. Preparations for oral administration may be suitably
formulated to give controlled release of the active compound.
[0162] Formulations for oral use include tablets or capsules which
contain the active ingredients mixed optionally with
pharmaceutically acceptable inert excipients.
[0163] Such excipients include for example: inert diluents such as
calcium carbonate, sodium chloride, lactose, calcium phosphate,
sodium phosphate, dicalcium phosphate, calcium sulfate, mannitol,
sorbitol, and the like, etc.; granulating and disintegrating
agents, for example, potato starch, alginic acid, etc.; binding
agents, for example, starch, gelatin or acacia, etc.; and
lubricating agents for example, magnesium stearate, stearic acid or
talc. Non-limiting examples of lubricants include talc, starch,
paraffin, stearic acid, magnesium stearate, and calcium
stearate.
[0164] Other pharmaceutically acceptable excipients include
colorants, flavoring agents, plasticizers, humectants, etc. In
certain embodiments, the active ingredient(s) may be delivered in a
soft or hard gel capsule by mixing the active ingredient with water
or oil such as peanut oil, or olive oil and enclosing the resulting
formulation in a capsule. Suitable colorants include dyes that are
generally suitable for food, drug and cosmetic applications, i.e.,
those known as F.D.&C. dyes.
[0165] The extracts of the present invention can be processed in
the usual way for the preparation of the compositions, including
but not limited to tablets, controlled-release products, capsules,
caplets, solutions, and the like. The composition can also be
formulated as confections including but not limited to gums,
lozenges, troches and the like. One preferred composition is as a
tablet containing between 50-300 mg of the extract or the raw plant
material, and more preferably containing 100-200 mg of the extract
or the raw plant material.
[0166] The preparation may be in liquid form, for example,
solutions, syrups or suspensions, or may be presented as a powdered
product for reconstitution with water, beverage or other suitable
vehicle before use. Such liquid preparations may be prepared by
conventional means with pharmaceutically acceptable additives such
as suspending agents (e.g., sorbitol syrup, cellulose derivatives
or hydrogenated edible fats); emulsifying agents (e.g., lecithin or
acacia); non-aqueous vehicles (e.g., almond oil, oily esters, or
fractionated vegetable oils); and preservatives (e.g., methyl or
propyl-p-hydroxybenzoates or sorbic acid).
[0167] The composition can be formulated to provide a homogenous
mixture, or the composition can be formulated so that the
components are non-homogenous.
[0168] The dosage may also be administered as an oral liquid dosage
form by suspending the active ingredients or extracts thereof in an
aqueous solution in admixture with a dispersing or wetting agent,
suspending agent and one or more preservatives. Suitable dispersing
or wetting agents are, for example, naturally occurring
phosphatides, for example, lecithin, or condensation products of
ethylene oxide, fatty acids, long chain aliphatic acids, or a
partial ester derived from fatty acids and a hexitol or hexitol
anhydrides, for example, polyoxyethylene stearate, polyoxyethylene
sorbitol monooleate, polyoxyethylene sorbitan monooleate, etc.
Suitable suspending agents are, for example, sodium
carboxymethylcellulose, methylcellulose, sodium alginate, etc.
[0169] The solubility the acids in water can be improved by
providing them in the form of a pharmaceutically acceptable salt,
and their physiological effectiveness can be enhanced. Examples of
a basic substance used for forming such a salt include inorganic
bases such as alkali metal or alkaline earth metal hydroxides, for
example, such as lithium hydroxide, sodium hydroxide, potassium
hydroxide, magnesium hydroxide and calcium hydroxide; and ammonium
hydroxide; and organic bases, such as basic amino acids such as
arginine, lysine, histidine and ornithine; and monoethanolamine,
diethanolamine and triethanolamine, with the alkali metal or
alkaline earth metal hydroxides being particularly preferred. The
agents according to the present invention may be formulated either
by preparing such a salt and adding the salt to other components,
or by separately adding a salt-forming component and a component to
be formed into a salt to other components to react them in the
formulation system.
[0170] For buccal administration, the compositions may take the
form of tablets or lozenges formulated in conventional manner.
Lozenges will typically be shaped solids containing the extract in
a candy or glycerinated base.
[0171] Alternatively, the active ingredients of the present
invention may be delivered over an extended time period by delaying
disintegration and absorption in the gastrointestinal tract to
provide a sustained release effect. A time delay material such as
glyceral monostearate or glycerol distearate may be employed for
this purpose. Extended release formulations that may be employed to
deliver the active ingredients of the invention are well known in
the art.
[0172] If the composition is water-soluble, then it may be
formulated in an appropriate buffer, for example, phosphate
buffered saline or other physiologically compatible solutions.
Alternatively, if the resulting composition has poor solubility in
aqueous solvents, then it may be formulated with a non-ionic
surfactant such as Tween or polyethylene glycol. Thus, the
compositions and their physiologically acceptable solvates may be
formulated for administration by inhalation or insufflation (either
through the mouth or the nose), oral, buccal, parenteral, or rectal
administration.
[0173] For rectal applications, suitable formulations for
compositions according to the present invention include
suppositories (emulsion or suspension type), and rectal gelatin
capsules (solution or suspensions). In a typical suppository
formulation, the active ingredients are combined with an
appropriate pharmaceutically acceptable suppository base such as
cocoa butter, esterified acids, glycerinated gelatin, and various
water soluble or dispersable bases like polyethylene glycols and
polyoxyethylene glycols and polyoxyethylene sorbitan fatty acid
esters.
[0174] The compositions may, if desired, be presented in a pack or
dispenser device which may comprise one or more unit dosage forms
comprising the active ingredient. The pack may for example comprise
metal or plastic foil, such as a blister pack. The pack or
dispenser device may be accompanied by instructions for
administration.
[0175] The composition can also be formulated as a confection such
as a gum, lozenge, troche, and the like. Components that may be
incorporated into a confection include but are not limited to
sweeteners, coloring agents, flavoring agents, preservatives,
diluents, emulsifying agents, excipients, and the like.
[0176] Suitable sweeteners may be readily selected by those skilled
in the art, and the amount of sweetener to be determined by taste.
The sweetener may be naturally occurring or synthetic, and may be
nutritive or non-nutritive. Examples of such sweeteners include,
but are not limited to, the saccharides, sugar alcohols such as
alcohol and mannitol, water-soluble artificial sweeteners such as
soluble saccharine salts, and dipeptide-based sweeteners such as
L-aspartyl-L-phenylalanine methyl ester. Flavorings may include
natural or artificial flavors such as mint oils, citrus oils, and
the like.
[0177] The composition may be prepared as a gum using conventional
means. The "gum base" may be one a number of types of compositions,
typically prepared by heating and blending various ingredients,
e.g., natural gums, synthetic resins, waxes, and the like. Waxes,
including natural and synthetic waxes, petroleum waxes, paraffin
waxes and microcrystalline waxes may also be incorporated into the
gum base.
[0178] A preferred composition is a controlled-release formulation.
Controlled-release formulations may employ alginates,
microcrystalline cellulose, cellulose ethers, vegetable gums, and
polymer complexes to sustain the extract in the system. Physical
means such as coating, microencapsulation, and embedding in complex
matrices may be employed for this purpose. A preferred physical
means is microencapsulation.
[0179] Other techniques known in the art can also be used to
produce a controlled release composition. The controlled release
composition yields an immediate release of effective dosage, and a
sustained release such as to yield an effective dosage duration
ranging from 3-6 hours, preferably 3.5 to 4.5 hours.
[0180] In addition to the foregoing, compositions of the present
invention include formulations further comprising additional active
ingredients and/or inactive ingredients, including solvents,
diluents, suspension aids, thickening or emulsifying agents,
sweeteners, flavorings, preservatives, solid binders, lubricants
and the like, as suited to the particular dosage form desired.
Remington's Pharmaceutical Sciences, Sixteenth Edition, E. W.
Martin (Mack Publishing Co., Easton, Pa., 1980) discloses various
carriers used in formulating pharmaceutically acceptable
compositions and which may also be suitable for use in formulations
of the present invention.
[0181] In accordance with an aspect of the present invention, the
extract can be included in the preparation of pharmaceutical
compositions containing a sufficient concentration of the extract
to achieve a desirable pharmaceutical effect within an acceptable
dosage regimen. All the compositions can be standardized for total
phenolics, chlorogenic acids and specific chlorogenic acids by
varying the amount of standardized extract added during the
compounding process.
[0182] The present invention provides a method for promoting weight
loss. The composition may be provided 1 to 7 times daily in
conjunction with proper diet and physical exercise. The exact
dosage and dosage forms will vary according to the individual to be
treated and will depend on such factors such as requirements of the
individual, the severity of the disorder or condition being treated
and the age and health of the person being treated, as well as use
of other medications and herbal remedies. The determination of
optimum dosages can be made for a particular patient by one skilled
in the art. An example of an effective amount of the Smallanthus
sonchifolius extract of the present invention is between about 5 to
5000 mg, and especially between about 10 to 500 mg, a day per adult
(weight: 60 kg).
[0183] The magnitude of the therapeutic dose of an active
ingredient in the acute or chronic management of a disorder or
condition will vary with the severity of the disorder or condition
to be treated and the route of administration. The dose, and
perhaps the dose frequency, may vary according to age, body weight,
response, and the past medical history of the consumer or patient.
Suitable dosing regimens can be readily selected by those skilled
in the art with due consideration of such factors.
[0184] Except insofar as any conventional carrier medium is
incompatible with the ingredients of the invention, such as by
producing any undesirable effect or otherwise interacting in a
deleterious manner with any other ingredient(s) of the formulation,
its use is contemplated to be within the scope of this
invention.
Examples
Example 1
Example 1
[0185] It has now been shown that a dietary supplement prepared
according to the following specification in caplet form promote and
support weight loss; help reduce body mass index (BMI); help reduce
waist measurements; increase metabolism; increase thermogenesis and
increase energy.
TABLE-US-00001 Dietary Ingredient Name Active % caffeine
Smallanthus sonchifolius extract, leaves Chlorogenic acids 45
5-caffeoylquinic acid 10 Phyllostachys edulis extract Lepidium
meyenii
Example 2
[0186] A serving of the dietary supplement was prepared and
comprises the following ingredients in powder form.
TABLE-US-00002 Actives Dietary Ingredient Name % Anhydrous caffeine
Smallanthus sonchifolius extract Chlorogenic acids 45
5-caffeoylquinic acid 10 Goji Extract (Lycium barbarum) std to
polysaccaharides 3 Acerola Extract (Malpighia glabra), fruit
Zeaxanthin Blueberry Powder (Vaccinum corymbosum), fruit
Pomegranate powder (Punica granatum), fruit Bilberry Extract
(Vaccinium myrtillus), fruit Vitamin C 95% std to Ascorbic Acid 95
Vitamin D3 100,000 IU/g
Example 3
[0187] A serving of the dietary supplement was prepared and
comprises the following ingredients in powder form.
TABLE-US-00003 Dietary Ingredient Name Psyllium powder (Plantago
ovata), seed Smallanthus sonchifolius extract Oat Bran (Avena
sativa) Inulin (Cichorium intybus), root
Example 4
[0188] A serving of the dietary supplement was prepared and
comprises the following ingredients in caplet form.
TABLE-US-00004 Active Stan. Dietary Ingredient Name (%) Smallanthus
sonchifolius extract, Chlorogenic acids 45 5-caffeoylquinic acid 10
Goji extract (Lycium barbarum), fruit Std to Polysaccharides 3
Acerola concentrate 4-5:1 (Malpighia glabra), fruit Supplying
bioflavonoids Vitamin C - Ascorbic acid Std to Ascorbic acid 95
Blueberry powder (Vaccinium corymbosum), fruit Supplying flavonoids
Pomegranate powder (Punica granatum), fruit & seed Bilberry
extract 4:1 (Vaccinium myrtillus), fruit Supplying Anthocyanins
Zeaxanthin Supplying Zeaxanthin 5 Vitamin D3 (as cholecalciferol)
beadlets - 1,000,000 IU
Example 5
[0189] A serving of the dietary supplement was prepared and
comprises the following ingredients in powder form.
TABLE-US-00005 Active Stan. Dietary Ingredient Name (%) Caffeine
Anhydrous Smallanthus sonchifolius extract inosine L-Histidine
Muira Puama Powder(Ptychopetalum Uncinatum/Olacoides), Bark Taurine
L-glutamine L-ornithine hcl Gamma -Oryzanol Phytosterol Complex
Total phytosterols 90 Beta-sitosterol 40 Campesterol 20
Stigmasterol 14 Buffalo Herb (Medicago sativa) Mycozyme ( Fungal
Amylase 1000 Units/Gram) DL-Malic Acid
Example 6
[0190] A serving of the dietary supplement was prepared and
comprises the following ingredients in caplet form.
TABLE-US-00006 Active Stan. Dietary Ingredient Name (%) Vitamin C -
Ascorbic acid Std to Ascorbic acid Natural caffeine extract (Coffea
94 arabica) 50:1, bean/seed Std to Caffeine 90 Smallanthus
sonchifolius extract Std to Chlorogenic acid 45 Std to
5-coffeoylquinic acid 10 Std to Caffeine 2 White kidney powder
(Phaseolus vulgaris), bean/seed Acerola juice powder 5:1 (Malpighia
glabria), fruit Asian ginseng powder (Panax ginseng), root Opuntia
ficus-indica powder, leaf Schizandra chinensis powder, fruit
Turmeric powder (Curcuma longa), root Vitamin H Biotin 1 Choline
bitartrate - encapsulated Choline bitartrate 88 Goji extract 6:1
(Lychium barbarum), fruit Std to Polysaccharide 3 Pomegranate
powder (Punica granatum), fruit & seed (whole fruit) Vitamin B3
- nicotinamide Vitamin B6 - Pyridoxine HCl granular Pyridoxine HCl
96 Pyridoxine 82 Vitamin D3 (as cholecalciferol) beadlets -
1,000,000 IU Chromium picolinate (Chromax) Chromium 12.18
Example 7
[0191] A serving of the dietary supplement was prepared and
comprises the following ingredients in capsule form.
TABLE-US-00007 Active Stan. Dietary Ingredient Name (%) Calcium
carbonate Calcium 39 Natural caffeine dry concentrate extract
(Coffea arabica), seed/bean Std to Caffeine 90 Smallanthus
sonchifolius extract, Chlorogenic acid 45 5-caffeoylquinic acid 10
Caffeine 2 White kidney bean powder (Phaseolus vulgaris), bean
Isoleucine Threonine Inositol Angelica archangelica powder, root
Bayberry powder (Myrica cerifera), bark Bilberry powder (Vaccinium
myrtillus), fruit Gentiana lutea powder, root Niacin (as nicotinic
acid) Calendula officinalis powder, aerial parts/herb top Ficus
carica powder, fruit Sunflower oil powder (Helianthus annuus), seed
L-glutamic acid hydrochloride Evening primrose oil (Oenothera
biennis), seed Std to Gamma-linoleic 10 Folic acid Folic acid 10
Vitamin D3 - 1,000,000 IU/g (liquid) Chromium picolinate Chromium
12.68
Example 8
[0192] A comestible composition is prepared according to following
proportions: 198 mg of an extract of Smallanthus sonchifolius and 2
mg of vitamin C.
Example 9
[0193] A serving of the dietary supplement was prepared and
comprises Smallanthus sonchifolius, Lepidium meyenii and caffeine
in syrup form providing between 0.07 g and 0.21 g FOS/kg/day.
[0194] In the foregoing specification, the invention has been
described with specific embodiments thereof; however, it will be
evident that various modifications and changes may be made thereto
without departing from the broader spirit and scope of the
invention.
* * * * *