U.S. patent application number 12/170946 was filed with the patent office on 2008-10-30 for method of using guava extract and composition including guava extract.
This patent application is currently assigned to Amerilab Technologies, Inc.. Invention is credited to Mary Aldritt, GeMing Lui, Fred Wehling.
Application Number | 20080268081 12/170946 |
Document ID | / |
Family ID | 38232997 |
Filed Date | 2008-10-30 |
United States Patent
Application |
20080268081 |
Kind Code |
A1 |
Wehling; Fred ; et
al. |
October 30, 2008 |
METHOD OF USING GUAVA EXTRACT AND COMPOSITION INCLUDING GUAVA
EXTRACT
Abstract
A method of using guava extract is disclosed that includes
administering alcohol to a mammal, and administering guava extract
within no greater than about 12 hours of administering of the
alcohol. A composition is also disclosed that includes a
pharmaceutically acceptable carrier and guava extract.
Inventors: |
Wehling; Fred; (Greenfield,
MN) ; Aldritt; Mary; (Excelsior, MN) ; Lui;
GeMing; (Honolulu, HI) |
Correspondence
Address: |
ALLISON JOHNSON, P.A.
LAKE CALHOUN EXECUTIVE CENTER, 3033 EXCELSIOR BLVD., SUITE 467
MINNEAPOLIS
MN
55416
US
|
Assignee: |
Amerilab Technologies, Inc.
Plymouth
MN
|
Family ID: |
38232997 |
Appl. No.: |
12/170946 |
Filed: |
July 10, 2008 |
Related U.S. Patent Documents
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Application
Number |
Filing Date |
Patent Number |
|
|
11327586 |
Jan 6, 2006 |
|
|
|
12170946 |
|
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Current U.S.
Class: |
424/774 ;
424/725 |
Current CPC
Class: |
A61K 9/0007 20130101;
A23L 33/105 20160801; A61K 9/0095 20130101; A61K 9/0058 20130101;
A61K 36/61 20130101; A61P 39/02 20180101; A23L 2/40 20130101; A61P
43/00 20180101; A61P 25/32 20180101; A61P 29/00 20180101 |
Class at
Publication: |
424/774 ;
424/725 |
International
Class: |
A61K 36/61 20060101
A61K036/61; A61P 29/00 20060101 A61P029/00 |
Claims
1. A method of using guava extract, said method comprising
administering guava extract to a human feeling a headache.
2. The method of claim 1, wherein said administering comprises
administering at least 250 mg of guava extract to said mammal.
3. The method of claim 1, wherein said administering comprises
administering at least 500 mg of guava extract to said mammal.
4. The method of claim 1, wherein said administering comprises
administering at least about 1000 mg of guava extract to said
mammal.
5. The method of claim 1, wherein said guava extract comprises a
water-soluble extract of guava leaves.
6. The method of claim 1, wherein said guava extract comprises at
least one of an organic solvent soluble extract of guava leaves and
an oil soluble extract of guava leaves.
7. A method of using guava extract, said method comprising
administering guava extract to a human within no greater than 24
hours of said human feeling a headache.
8. The method of claim 7, wherein said administering guava extract
occurs prior to said human feeling a headache.
9. The method of claim 7, wherein said administering guava extract
occurs within about 1 hour of said human feeling a headache.
10. The method of claim 7, wherein said administering guava extract
comprises administering at least 250 mg of guava extract.
11. The method of claim 7, wherein said administering guava extract
comprises administering at least 500 mg of guava extract.
12. The method of claim 7, wherein said administering guava extract
comprises administering at least about 1000 mg guava extract.
13. A method of alleviating a headache in a human, said method
comprising administering guava extract to the human in an amount
sufficient to alleviate the headache.
14. The method of claim 13, comprising administering at least 500
mg of said guava extract.
15. The method of claim 13, comprising administering at least about
1000 mg of said guava extract.
16. A method of using guava extract, said method comprising
administering guava extract to a human who expects to feel a
headache.
Description
CROSS-REFERENCE TO RELATED APPLICATIONS
[0001] This application is a continuation of U.S. application Ser.
No. 11/327,586, filed on Jan. 6, 2006, and incorporated herein.
BACKGROUND
[0002] The invention relates to administering guava extract.
[0003] The guava plant, psidium guajava L., has been used as a
source of nutrition by many cultures; its fruit is eaten as is,
made into juices and jellies, and used in other food products.
Parts of the guava plant have been used by various cultures to
treat diarrhea and sore gums. The guava plant has also been studied
to ascertain its effects on various conditions of the human body
including diabetes and obesity.
[0004] Human beings have been consuming alcohol, in the form of
ethanol, for centuries. After alcohol is ingested it is absorbed
from the stomach and upper gastrointestinal tract. Alcohol that a
person drinks shows up in the person's breath because it is
absorbed from the mouth, throat, stomach and intestines into the
bloodstream. Alcohol is not chemically changed while in the
bloodstream. As the blood passes through the lungs, some of the
alcohol moves across the membranes of the lung's air sacs (alveoli)
into the air, because alcohol is volatile. The concentration of the
alcohol in the alveolar air is related to the concentration of the
alcohol in the blood. By analyzing the breath of an individual, one
can determine the level of alcohol in the individual. Although
alcohol is found in human breath whether or not an individual has
been consuming it, in most circumstances the only possible way to
increase the level of alcohol in the body to a point sufficient to
cause behavioral impairment is to ingest alcohol.
[0005] Blood Alcohol Content, which is also referred to as Blood
Alcohol Concentration, (both of which are referred to as "BAC") can
be determined by breath analysis for the volatile organic compound
ethanol. BAC is a measure of the mass of alcohol (i.e., ethanol) in
a given volume of blood and is reported in milligrams (mg) ethanol
per 100 milliliters (mL) blood. A BAC measurement of 0.04%, for
example, translates to a concentration of 40 mg of alcohol in 100
mL of blood. Breath analysis alcohol content (BrAC) in the United
States is specified as BAC/2100. At 34.degree. C. (i.e., 93.degree.
F.) ethanol is in equilibrium in blood at a ratio of roughly 2100:1
based on the distribution of ethanol in equilibrium with the blood
in the deep part of the lungs. In other words, 2100 ml of air in
the deep parts of the lungs contain the same amount of ethanol that
is present in 1 ml of blood. Because the ethanol concentration in
the breath is related to that in the blood, the BAC can be
calculated from the breath alcohol measurement. The ratio of breath
alcohol to blood alcohol is 2,100:1. This means that 2,100
milliliters (ml) of alveolar air will contain the same amount of
alcohol as 1 ml of blood.
[0006] Consuming too much alcohol can cause a variety of negative
effects in the body including impairing motor skills and reaction
times. When people who have consumed too much alcohol operate a
motor vehicle, they can pose a danger to themselves and other
motorists. As a result, legal standards for permissible blood
alcohol content for operating a motor vehicle have been developed.
For many years, the legal standard for permissible blood alcohol
content across the United States was a BAC measurement of 0.10%,
but many states have now adopted the 0.08% standard. The federal
government has pushed states to lower the legal limit. The American
Medical Association takes the position that a person can become
impaired when the blood alcohol level hits 0.05%.
[0007] Consuming too much alcohol can also result in a hangover,
which is often accompanied by a variety of symptoms including at
least one of headache, nausea, lack of appetite, shakiness,
fatigue, dry mouth, an overall feeling of being unwell, and
decreased occupational, cognitive, or visual-spatial skill
performance. The negative effects of alcohol consumption are due in
large part to the toxic effects of acetaldehyde. Although a portion
of the alcohol is eliminated in urine and breath, a majority of the
alcohol is oxidized, primarily in the liver. The liver converts
ethanol to acetaldehyde by alcohol dehydrogenases. Acetaldehyde is
processed by the liver at a fixed rate, regardless of how much
alcohol is in the bloodstream. Acetaldehyde is then oxidized to
acetic acid by acetaldehyde dehydrogenases, which is rapidly
metabolized to carbon dioxide and water.
[0008] Acetaldehyde provokes disturbances in bodily processes by,
for example, forming adducts with hemoglobin and proteins of plasma
of the brain and other organs, and inhibiting the transfer of
reducing agents along the mitochondrial respiratory chain.
Acetaldehyde also accumulates in the cerebellum causing headache by
contracting cerebral blood vessels thereby decreasing blood flow
resulting in pain.
SUMMARY
[0009] In one aspect, the invention features a method of
administering guava extract to a mammal (including, e.g., a human
being, a chimp, a monkey, a dog, a pig, a rat, and a mouse). In one
embodiment, the method includes treating a mammal having an
elevated (i.e., greater than normal due to alcohol consumption)
blood alcohol content by administering guava extract to the mammal.
In another embodiment, administering the guava extract includes
administering an amount of guava extract sufficient to decrease the
blood alcohol content of the mammal. In some embodiments, the
mammal has a blood alcohol content of at least 0.05% prior to the
administering. In other embodiments, the administering includes
administering at least 250 mg of guava extract to the mammal. In
some embodiments, the administering includes administering at least
500 mg, at least about 1000 mg, at least about 1500 mg, or even at
least about 2000 mg of guava extract to the mammal.
[0010] In another embodiment, the administering includes
administering guava extract in an amount sufficient to decrease the
blood alcohol content of the mammal by at least about 20%. In other
embodiments, the administering includes administering guava extract
in an amount sufficient to decrease the blood alcohol content of
the mammal by at least 0.02 units.
[0011] In another aspect, the invention features a method of
decreasing the aldehyde content in a mammal experiencing elevated
levels of aldehyde by administering guava extract to the mammal. In
some embodiments, the administering includes administering at least
500 mg, at least about 1000 mg, at least about 1500 mg, or even at
least about 2000 mg of guava extract to the mammal. In one
embodiment, the method inhibits, alleviates or prevents the
feelings associated with a hangover.
[0012] In other aspects, the invention features a the method of
using guava extract includes administering alcohol to a mammal and
administering guava extract within no greater than about 12 hours
of the administering of the alcohol. In one embodiment, the
administering guava extract occurs within about 1 hour of the
administering alcohol. In another embodiment, the guava extract
includes a water-soluble extract of guava leaves. In other
embodiments, the guava extract includes at least one of an organic
solvent soluble extract of guava leaves and an oil soluble extract
of guava leaves.
[0013] In some embodiments, the administering guava extract occurs
prior to the consuming alcohol.
[0014] In other embodiments of the methods disclosed herein, the
administering includes administering least 250 mg, at least 500 mg,
at least about 1000 mg, at least about 1500 mg, or even at least
about 2000 mg of guava extract to the mammal.
[0015] In another aspect, the invention features a composition that
includes at least 500 mg guava extract and a pharmaceutically
acceptable carrier. In one embodiment, the carrier includes water,
oil, binder, lubricant, or a combination thereof. In other
embodiments, the carrier includes an aqueous liquid that includes
carbonation.
[0016] In some embodiments, a composition disclosed herein is a
formulation in the form of a powder, liquid, tablet, pill, capsule,
gel cap, a chewing gum or a combination thereof.
[0017] In another embodiment, a composition disclosed herein is a
formulation in the form of a suspension, a solution, an emulsion, a
syrup or a combination thereof.
[0018] In one embodiment, the composition is a solid effervescent
composition that includes at least 500 mg guava extract and a
pharmaceutically acceptable carrier that includes an effervescent
agent that includes an acid and a base. In some embodiments, the
composition is in the form of a tablet and the carrier further that
includes from 10% by weight to about 60% by weight binder and from
1% by weight to about 15% by weight lubricant. In some embodiments,
the composition further includes an ice tea flavor agent, FD&C
red dye number 40 or a combination thereof.
[0019] In other embodiments, the formulation is in the form of
chewing gum and the carrier further includes a gum base that
includes a water-soluble bulk portion, and a water-insoluble
chewable gum base portion.
[0020] In some embodiments of the methods disclosed herein, the
administering includes administering at least 500 mg, at least
about 1000 mg, at least about 1500 mg, or even at least about 2000
mg of guava extract to the mammal.
[0021] The guava extract is provided in an easy to ingest dosage
form that is palatable and is relatively quick acting. In some
cases the guava extract alleviates the effects of a hangover
including improving at least one of the overall feeling of the
mammal, headache, nausea, dry mouth, lack of appetite, shakiness,
and fatigue. In some cases the guava extract reduces the breath
alcohol content of a mammal, the aldehyde content in a mammal, at
least one negative physical feeling associated with a hangover or a
combination thereof.
[0022] Other features and advantages will be apparent from the
following description of the preferred embodiments and from the
claims.
GLOSSARY
[0023] In reference to the invention, these terms have the meanings
set forth below:
[0024] As used herein the term "an effective amount of guava
extract" means an amount that causes a decrease in the amount of
alcohol expired through the lungs based on the measured breath
alcohol content, a decrease in the level of alcohol in the blood, a
decrease in aldehyde content, or a combination thereof.
[0025] As used herein, the term "unit dose" or "unit dosage" refers
to physically discrete units that contain a predetermined quantity
of active ingredient calculated to produce a desired therapeutic
effect.
[0026] As used herein the term "oral dosage form" is used in a
general sense to reference a product that is administered
orally.
[0027] As used herein the term "carrier" means a substance used in
association with guava extract for aiding in the administration of
guava extract.
[0028] The term "pharmaceutically acceptable" when used herein as
an adjective, means substantially non-toxic and substantially
non-deleterious to the recipient.
DETAILED DESCRIPTION
[0029] The method includes administering (e.g., administering to
others or to one's self including, e.g., ingesting)) guava extract
to a mammal before, during or after consumption of alcohol.
Preferably the guava extract is administered at a time and provided
in an amount sufficient to alleviate at least one effect of a
hangover including such effects as dehydration, headache, nausea,
lack of appetite, shakiness, fatigue, dry mouth, and an overall
feeling of being unwell.
[0030] The administration of guava extract also preferably occurs
in an amount sufficient to reduce the mammal's blood alcohol
content, breath alcohol content, aldehyde (e.g., formaldehyde,
acetaldehyde and combinations thereof) content, or a combination
thereof. The guava extract is preferably administered in an amount
and at a time sufficient to decrease the blood alcohol content of
the mammal by at least about 10%, by at least about 20%, or even by
at least about 30%, by at least 0.02 units, by at least 0.03 units,
or even by at least 0.05 units as measured based on breath alcohol
content.
[0031] The guava extract can be administered at any suitable time
including, e.g., within no greater than 24 hours, no greater than
12 hours, no greater than 5 hours, no greater than 3 hours, no
greater than 2 hours, no greater than 1 hour, no greater than 0.5
hour, just after or before, or even simultaneously while consuming
alcohol. Alternatively or in addition, the guava extract can be
administered to a mammal that is feeling the effects of a hangover
or expects to feel the effects of a hangover at any suitable time
including, e.g., within no greater than 24 hours, no greater than
12 hours, no greater than 5 hours, no greater than 3 hours, no
greater than 2 hours, no greater than 1 hour, no greater than 0.5
hour, after, before, or even simultaneously with the feelings of a
hangover. Alternatively or in addition, the guava extract can be
administered to a mammal having a blood alcohol content of at least
0.03%, at least 0.04%, at least 0.05%, at least 0.06%, at least
0.08%, at least 0.1% or even greater than 0.15%.
[0032] The effective amount of guava extract will vary depending on
a number of factors including, e.g., the physical characteristics
of the individual (e.g., height, weight, age, and physical health),
the amount of alcohol consumed or to be consumed by the individual,
and the means used to administer the dosage. The guava extract is
preferably provided in a unit dosage form and can be administered
in a single dose or in multiple doses. The effective dose for a
given individual is usually set by the judgment of the individual.
The guava extract is generally effective over a wide dosage range.
Amounts that have been found to be useful include at least about
250 mg/dose, at least about 500 mg/dose, at least about 800
mg/dose, at least about 1000 mg/dose, at least about 1500 mg/dose,
at least about 2000 mg/dose, at least about 3000 mg/dose, at least
about 5000 mg/dose, or even at least about 10,000 mg/dose.
[0033] The dose of guava extract can include neat guava extract,
i.e., the dose is free of other components, or it can include
components in addition to guava extract including, e.g., a variety
of carriers. The dose preferably includes from 0.1% to 100% by
weight, at least about 10% by weight, at least about 20% by weight,
at least about 25% by weight, at least about 30% by weight, at
least about 40% by weight guava extract.
[0034] Useful sources of guava extract include extracts of various
parts of the plant psidium guajava L. including the fruit, leaves,
stems, and roots thereof. Preferably the guava extract is obtained
from guava leaves. The guava extract can be obtained through a
solvent extraction process wherein at least a portion of the guava
plant is contacted with a liquid including, e.g., an organic
solvent (e.g., methanol, ethanol, butanol and isopropanol), water
(e.g., tap water, room temperature water, elevated temperature
water (e.g., boiling water) and combinations thereof), oil (e.g.,
mineral oil, elevated temperature oil, vegetable oils, animal oils
and combinations thereof), and combinations thereof. The resulting
extract is then gathered for use. The guava plant or a portion
thereof can also be treated prior to extraction. Useful treatments
include, e.g., drying, lyophilizing, freeze drying, humidifying,
and combinations thereof.
[0035] Useful carriers for the guava extract include, e.g.,
excipients, diluents, binders, lubricants, disintegrants, coloring
agents, sweetening agents, and combinations thereof including,
e.g., carbohydrates, waxes, water soluble and/or swellable
polymers, hydrophilic materials, hydrophobic materials, gelatin,
oils, organic solvents, water, and combinations thereof. The
selection of the carrier will depend upon the means by which the
guava extract is to be administered.
[0036] The dose of guava extract can optionally include wetting
agents, lubricating agents, emulsifiers, suspending agents,
preservatives, sweeteners, stabilizers, flavoring agents, coloring
agents, and combinations thereof, useful examples of which are set
forth below.
[0037] The dose of guava extract can be provided in a variety of
packages including metal foil pouches, tubes (e.g., plastic and
metal tubes), ampoules, in multidose containers. The packaging
preferably is air tight and impermeable to moisture.
[0038] The dose of guava extract can be administered in any
convenient manner including, e.g., by oral, intravenous,
subcutaneous, intramuscular and subcutaneous routes, and
combinations thereof. Oral administration can be by any suitable
dosage form including, e.g., powder (e.g., effervescent powders,
and powdered drink mixes), tablet (e.g., quick dissolve tablets),
granulations (e.g., effervescent granulations, chewable
granulations), pill, capsule, gel caps, composite (e.g., a layered
tablet construction, a construction that includes a continuous
phase and a discontinuous phase), chewable dosage forms including
chewing gum and chewable tablets, wafer (e.g., disintegrating
tablets and dissolving tablets), and liquid formulations (e.g.,
solutions and dispersions), e.g., beverages, e.g., canned and
bottled beverage, a dry or liquid aerosol that can be inhaled or
sprayed, and combinations thereof. The guava extract can be
provided in the form of a sterile solution by direct injection into
the bloodstream of the individual to be treated. The guava extract
is preferably formulated into a dosage form that provides an easily
controllable dose of guava extract, is easy to ingest, and is easy
to handle.
[0039] One example of a useful solid effervescent composition for
guava extract includes guava extract and an effervescent agent that
includes an acid and a base. The guava extract is preferably dried
and sieved to a suitable particle size (e.g., using a number 12
sieve) prior to combining with the other ingredients of the
effervescent composition. The effervescent composition preferably
includes guava extract in an amount of at least about 250 mg, at
least about 500 mg, at least about 800 mg, at least about 1000 mg,
at least about 1500 mg, or even at least about 2000 mg.
[0040] The effervescent agent is activated when contacted with an
aqueous liquid, e.g., water (e.g., when the powder or tablet is
placed in a glass of water). The water liberates the acid and base
and enables the acid and base to react with each other to produce
carbon dioxide gas, which imparts carbonation to the aqueous
composition. Examples of useful acids include citric acid, ascorbic
acid, aspartic acid, malic acid, adipic acid, tartaric acid,
fumaric acid, succinic acid, sodium acid pyrophosphate, lactic
acid, hexamic acid, amino acids, and acid salts and acid anhydrides
thereof, and mixtures thereof. Examples of useful acid anhydrides
include citraconic anhydride, glucono-D-lactone, and succinic
anhydride. Examples of useful acid salts include potassium
bitartrate, acid citrate salts, sodium dihydrogen phosphate,
disodium dihydrogen phosphate, sodium acid sulfite, and
combinations thereof. Preferably acid is present in the
effervescent composition in an amount of from 10% by weight to
about 60% by weight, from about 15% by weight to about 50% by
weight, or even from about 25% by weight to about 40% by
weight.
[0041] The base preferably is capable of generating a gas such as
carbon dioxide. Examples of suitable carbonate bases include sodium
bicarbonate, sodium carbonate, sodium sesquicarbonate, potassium
carbonate, potassium bicarbonate, calcium carbonate, magnesium
carbonate, magnesium oxide, sodium glycine carbonate, L-lysine
carbonate, arginine carbonate, zinc carbonate, zinc oxide, amino
acid carbonates, and mixtures thereof. The effervescent composition
preferably includes base in an amount of from 10% by weight to
about 60% by weight, from about 15% by weight to about 50% by
weight, or even from about 25% by weight to about 40% by
weight.
[0042] The effervescent composition can optionally include a
variety of additional active agents including, e.g., vitamins,
amino acids, pharmaceutical agents, minerals, dietary supplements,
and combinations thereof. Suitable vitamins include, e.g., ascorbic
acid (vitamin C), aspartic acid, thiamin, riboflavin, nicotinic
acid, pantothenic acid, pyridoxine, biotin, folic acid, niacin,
vitamin B12, lipoic acid, vitamin A, vitamin D, vitamin E and
vitamin K and coenzymes thereof, choline, camitine, and alpha,
beta, and gamma carotenes. Examples of coenzymes include thiamine
pyrophosphates, flavin mononucleotide, flavin adenine dinucleotide,
nicotinamide adenine dinucleotide, nicotinamide adenine
dinucleotide phosphate coenzyme A pyridoxal phosphate, biocytin,
tetrahydrofolic acid, coenzyme B12, lipoyllysine, 11-cis-retinal,
and 1,25-dihydroxycholecalciferol and mixtures.
[0043] Suitable amino acids include, e.g., L-tyrosine, isoleucine,
omithine, glutamine, phenylalanine, leucine, lysine, methionine,
threonine, taurine, tryptophan, valine, alanine, glycine, arginine,
histidine, cysteine, asparagine, proline and serine, and mixtures
thereof.
[0044] Examples of minerals include iron, zinc, selenium, copper,
iodine, phosphorus, chromium and mixtures thereof.
[0045] Suitable dietary supplements include, e.g., bee pollen,
bran, wheat germ, kelp, cod liver oil, ginseng, and fish oils,
amino-acids, proteins, vitamins, minerals
alpha-glycerylphosphorylcholine, acetyl-L-carnitine and salts
thereof, docosahexaenoic acid, cranberry extract, chondroitin,
methylsulfonylmethane, and mixtures thereof.
[0046] The effervescent composition can also include other
ingredients including, e.g., flavor agents, fillers, surfactants
(e.g., polysorbate 80 and sodium lauryl sulfate), color agents
including, e.g., dyes and pigments, sweeteners, and flow
agents.
[0047] Useful flavor agents include natural and artificial flavor
agents including, e.g., volatile oils, synthetic flavor oils,
flavoring aromatics, oils, liquids, oleoresins and extracts derived
from plants, leaves, flowers, fruits, stems and combinations
thereof. Useful flavor agents include, e.g., citric oils, e.g.,
lemon, orange, grape, lime and grapefruit, fruit essences
including, e.g., apple, pear, peach, grape, strawberry, raspberry,
cherry, plum, pineapple, apricot, and other fruit flavors, ice tea
flavoring, and combinations thereof. Other useful flavor agents
include, e.g., aldehydes and esters (e.g., benzaldehyde (cherry,
almond)), citral, i.e., alpha-citral (lemon, lime), neral, i.e.,
beta-citral (lemon, lime), decanal (orange, lemon), aldehyde C-8
(citrus fruits), aldehyde C-9 (citrus fruits), aldehyde C-12
(citrus fruits), tolyl aldehyde (cherry, almond),
2,6-dimethyloctanal (green fruit), 2-dodedenal (citrus, mandarin),
and mixtures thereof. Preferably the effervescent composition
includes at least about 100 mg, at least about 200 mg, no greater
than about 500 mg or even no greater than about 400 mg flavor
agent.
[0048] Useful color agents include, e.g., food, drug and cosmetic
(FD&C) colors including, e.g., dyes (e.g., FD&C red no.
40), lakes, and certain natural and derived colorants. Useful lakes
include dyes absorbed on aluminum hydroxide and other suitable
carriers.
[0049] Useful sweetening agents include stevia, sugars such as
sucrose, glucose, invert sugar, fructose, ribose, tagalose,
sucralose, malitol, erythritol, xylitol, and mixtures thereof,
saccharin and its various salts (e.g., sodium and calcium salt of
saccharin), cyclamic acid and its various salts, dipeptide
sweeteners (e.g., aspartame), acesulfame potassium,
dihydrochalcone, glycyrrhizin, and sugar alcohols including, e.g.,
sorbitol, sorbitol syrup, mannitol and xylitol, and combinations
thereof.
[0050] The solid effervescent composition can be provided in a
variety of forms including, e.g., powder, granulation, tablet,
capsule, pellet and composite. Preferred effervescent tablets have
a hardness of at least 3 kilopounds (Kp), preferably at least 5 Kp,
from about 5 Kp to about 10 Kp, or even from about 5 Kp to about 8
Kp, as measured on a standard hardness tester fitted with a strain
gauge.
[0051] When in the form of a tablet, the effervescent composition
preferably also includes binder, lubricant, and combinations
thereof. Examples of suitable binders include, e.g., starches,
natural gums, cellulose gums, microcrystalline cellulose,
methylcellulose, cellulose ethers, sodium carboxymethylcellulose,
ethylcellulose, gelatin, dextrose, lactose, sucrose, sorbitol,
mannitol, polyethylene glycol, polyvinylpyrrolidone, pectins,
alginates, polyacrylamides, polyvinyloxoazolidone,
polyvinylalcohols and mixtures thereof. Preferably the binder is
water soluble.
[0052] Where present, the binder of the effervescent composition is
present in an amount sufficient to assist in holding the components
of the composition together in the form of a tablet. When present,
the composition preferably includes binder in an amount from 10% by
weight to about 60% by weight, from about 15% by weight to about
50% by weight, or even from about 20% by weight to about 40% by
weight, or even 20% by weight to 30% by weight.
[0053] Various lubricants are suitable for use in the effervescent
composition including water dispersible, water soluble, water
insoluble lubricants and combinations thereof. Preferred lubricants
are water soluble. Some lubricants also provide a binder function
and vice versa. Examples of useful water soluble lubricants include
sodium benzoate, polyethylene glycol, L-leucine, adipic acid, and
combinations thereof. The composition can also include water
insoluble lubricants including, e.g., stearates (e.g., magnesium
stearate, calcium stearate and zinc stearate), oils (e.g., mineral
oil, hydrogenated and partially hydrogenated vegetable oils, and
cotton seed oil) and combinations thereof. Other water insoluble
lubricants include, e.g., animal fats, polyoxyethylene
monostearate, talc, and combinations thereof.
[0054] The effervescent composition preferably includes a
sufficient amount of lubricant to enable the composition to be
formed into tablets and released from a high speed tableting press
in the form of a tablet. When present, the composition preferably
includes lubricant in an amount of from 1% by weight to about 15%
by weight, from about 1% by weight to about 12% by weight, from
about 2% by weight to about 10% by weight, or even from about 3% by
weight to about 8% by weight.
[0055] The components of the effervescent composition are
preferably dried and sieved as necessary prior to formulating.
[0056] The effervescent composition is preferably stored in a
moisture-proof package including, e.g., sealed metal foil pouches,
blister packs, and desiccant capped tubes. Useful packaging
materials further include metal foil, plastic films, and blister
packaging.
[0057] The effervescent composition can be administered by adding
the composition to excess water or vice versa, e.g., an eight ounce
glass of tap water, to form an aqueous composition, followed by
ingestion. After addition of the effervescent composition to an
aqueous liquid, the composition optionally can be stirred to
facilitate dispersion and/or dissolution of the composition in the
aqueous liquid.
[0058] The effervescent composition for tableting is well suited to
the mass production of effervescent tablets that are free from
picking, die wall etching, capping and lamination. Any suitable
tablet mass production equipment and processes can be used.
Examples of useful tableting processes for effervescent
compositions are described in Pharmaceutical Dosage Forms, Vol. 1,
(Herbert A. Lieberman et al. eds, 2.sup.nd ed. 1989) and
incorporated herein. The tablets can then be manufactured in an
automated process in which multiple dies of a tablet press are
filled sequentially or simultaneously with the effervescent
composition, two punches compress the effervescent composition to
form the tablet(s), and then the tablet(s) is ejected from the die.
The tablet is then placed in packaging material, which is then
sealed to form an air tight sealed package. The packaged tablet can
be further processed by conveying it to other processing stations
including, e.g., additional packaging stations for further
packaging, e.g., boxing and bagging.
[0059] The tablet manufacturing and initial packing operations are
preferably performed in a controlled environment in which the
temperature and humidity are controlled. Preferably the controlled
environment has less than 18 grains, less than 16 grains, or even
less than 15 grains of moisture.
[0060] Other useful methods of making effervescent tablets, as well
as coated tablets, sustained release tablets, coated particles, and
chewable tablets, are disclosed in Pharmaceutical Dosage Forms,
Vols. 1-3, (Lieberman et al. eds. 2 ed. 1989) and incorporated
herein. A useful method of making quick dissolve tablets is
disclosed in U.S. Pat. No. 6,368,625 and incorporated herein.
[0061] One example of a suitable chewing gum formulation includes
guava extract and a chewing gum base. A useful chewing gum base
includes a water-soluble bulk portion, a water-insoluble chewable
gum base portion, and, optionally, a flavor agent. The
water-soluble portion dissipates with a portion of the flavoring
agent over a period of time during chewing. The gum base portion is
retained in the mouth throughout the chew. Useful water-insoluble
gum bases include, e.g., elastomers, resins, fats, oils, softeners,
inorganic fillers, and combinations thereof. The water-insoluble
gum base may optionally include wax. The chewing gum preferably
includes from about 5% by weight to about 95% by weight, from about
10% by weight to about 50% by weight, or even from about 25% by
weight to about 35% by weight water-insoluble gum base.
[0062] An example of a useful water-insoluble gum base includes
from about 20% by weight to about 60% by weight synthetic
elastomer, from about 0% by weight to about 30% by weight natural
elastomer, from about 5% by weight to about 55% by weight
plasticizer, from about 4% by weight to about 35% by weight filler,
from about 5% to about 35% by weight softener, and optionally minor
amounts (i.e., no greater than about 1% by weight) of additives
including, e.g., coloring agents, antioxidants, flavor agents, and
combinations thereof.
[0063] Useful synthetic elastomers include, e.g., polyisobutylene
(e.g., polyisobutylene having a weight average molecular weight of
from about 10,000 to about 95,000, or even from about 50,000 to
80,000), isobutylene-isoprene copolymer (butyl elastomer),
styrene-butadiene, copolymers of styrene-butadiene wherein the
styrene to butadiene ratio is from about 1:3 to about 3:1, or even
from about 1:1 to about 1:3, polyvinyl acetate (e.g., polyvinyl
acetate having a weight average molecular weight of from about
2,000 to about 90,000, or even from about 10,000 to about 65,000),
polyisoprene, polyethylene, vinyl acetate-vinyl laurate copolymers
(e.g., vinyl laurate copolymers having a vinyl laurate content from
about 5% by weight to about 50% by weight, or even from about 10%
by weight to about 45% by weight), and combinations thereof.
[0064] Useful natural elastomers include, e.g., natural rubber
(e.g., smoked latex, liquid latex, and guayule), natural gums
(e.g., jelutong, lechi caspi, perillo, sorva, massaranduba balata,
massaranduba chocolate, nispero, rosindinha, chicle, gutta hang
kang, and combinations thereof), and combinations thereof.
[0065] Useful elastomer plasticizers include, e.g., natural rosin
esters (e.g., glycerol esters of partially hydrogenated rosin,
glycerol esters of polymerized rosin, glycerol esters of partially
dimerized rosin, glycerol esters of rosin, pentaerythritol esters
of partially hydrogenated rosin, methyl and partially hydrogenated
methyl esters of rosin, pentaerythritol esters of rosin), synthetic
plasticizers including, e.g., terpene resins derived from
alpha-pinene, beta-pinene, d-limonene, and combinations thereof,
and combinations thereof.
[0066] Useful fillers and texturizers include, e.g., magnesium
carbonate, calcium carbonate, ground limestone, silicates (e.g.,
magnesium silicate and aluminum silicate), clay, alumina, talc,
titanium oxide, mono-, di- and tri-calcium phosphate, cellulose
polymers, and combinations thereof.
[0067] Useful softeners and emulsifiers include, e.g., tallow,
hydrogenated tallow, hydrogenated and partially hydrogenated
vegetable oils, cocoa butter, glycerol monostearate, glycerol
triacetate, lecithin, mono-, di- and triglycerides, acetylated
monoglycerides, fatty acids (e.g. stearic, palmitic, oleic and
linoleic acids), and combinations thereof.
[0068] Useful coloring agents including whiteners include, e.g.,
FD&C-type dyes and lakes, fruit and vegetable extracts,
titanium dioxide, and combinations thereof.
[0069] The gum base can optionally include wax. An example of a
wax-free gum base is disclosed in U.S. Pat. No. 5,286,500, the
disclosure of which is incorporated herein by reference.
[0070] The water soluble bulk portion can include bulk sweeteners,
high intensity sweeteners, flavoring agents, softeners,
emulsifiers, colors, acidulants, fillers, antioxidants, and
combinations thereof.
[0071] Softeners are added to the chewing gum in order to optimize
the chewability and mouth feel of the gum. The softeners, which are
also known as plasticizers and plasticizing agents, generally
constitute from about 0.5% by weight to about 15% by weight of the
chewing gum. Suitable softeners include, e.g., glycerin, lecithin,
and combinations thereof. Aqueous sweetener solutions such as those
containing sorbitol, hydrogenated starch hydrolysates, corn syrup,
and combinations thereof, can also be used as softeners and binding
agents in chewing gum.
[0072] Bulk sweeteners include both sugar and sugarless components.
The chewing gum can include from about 5% by weight to about 95% by
weight, from about 20% by weight to about 80% by weight, or even
from about 30% by weight to about 60% by weight bulk sweetener.
Sugar sweeteners generally include saccharide-containing components
including, e.g., sucrose, dextrose, maltose, dextrin, dried invert
sugar, fructose, levulose, glactose, corn syrup solids, and
combinations thereof. Sugarless sweeteners include, e.g., sugar
alcohols such as sorbitol, mannitol, xylitol, hydrogenated starch
hydrolysates, maltitol, and combinations thereof.
[0073] The gum can optionally include artificial sweeteners
including, e.g., sucralose, aspartame, N-substituted APM
derivatives such as neotame, salts of acesulfame, altitame,
saccharin and its salts, cyclamic acid and its salts,
glycyrrhizinate, dihydrochalcones, thaumatin, monellin, and
combinations thereof. In order to provide longer lasting sweetness
and flavor perception, it may be desirable to encapsulate or
otherwise control the release of at least a portion of the
artificial sweetener. Such techniques as wet granulation, wax
granulation, spray drying, spray chilling, fluid bed coating,
coacervation, and fiber extension may be used to achieve the
desired release characteristics.
[0074] Combinations of sugar and sugarless sweeteners may be used
in chewing gum. Additionally, the softener may also provide
additional sweetness such as with aqueous sugar or alditol
solutions.
[0075] Useful low calorie bulking agents include, e.g.,
polydextrose, Raftilose, Raftilin, fructooligosaccharides,
palatinose oligosaccharide, guar gum hydrolysate, indigestible
dextrin, and combinations thereof.
[0076] A variety of flavoring agents can are also suitable
including, e.g., essential oils, synthetic flavors or mixtures
thereof including, but not limited to, oils derived from plants and
fruits such as citrus oils, fruit essences, peppermint oil,
spearmint oil, other mint oils, clove oil, oil of wintergreen,
anise and the like. Artificial flavoring agents and components may
also be used. Natural and artificial flavoring agents may be
combined in any sensorially acceptable fashion. The flavor agent
can be present in the gum in amounts of from about 0.1% by weight
to about 15% by weight gum, or even from about 0.2% by weight to
about 5% by weight.
[0077] Useful methods of manufacturing chewing gum base and the
chewing gum end product are disclosed in, e.g., U.S. Pat. No.
6,949,264 (McGrew et al.), U.S. Pat. No. 3,995,064 (Ehrgott et al.)
and U.S. Pat. No. 4,459,311 (DeTora et al.) U.S. Pat. No. 5,045,325
(Lesko et al.), and U.S. Pat. No. 4,555,407 (Kramer et al.), U.S.
Pat. No. 4,968,511 (D'Amelia et al.), U.S. Pat. Nos. 5,543,160,
5,800,847, 5,397,580, 5,523,097, 5,419,919 and 5,571,543, European
Publication No. 0,273,809 (General Foods France), French
Publication No. 2,635,441 (General Foods France) and incorporated
herein.
[0078] The invention will now be described by way of the following
examples.
EXAMPLES
Test Procedures
[0079] Test procedures used in the examples include the
following.
Breath Alcohol Content (BAC) Test Method I
[0080] An individual inserts the mouthpiece of a ALCOHAWK portable
digital breath alcohol content tester (Q3 Innovations, LLC) into
his or her mouth and exhales into the device in accordance with the
device instructions until a reading appears on the device. The
value on the display is recorded in units of % BAC (blood alcohol
content).
Example 1
[0081] A base effervescent powder formulation is prepared by
combining 1000 mg sorbitol powder, 650 mg sodium bicarbonate
powder, and 2000 mg dried wild guava leaf extract (boiling water
soluble extract), in a plastic bag and shaking the bag until a
visually uniform granulation is obtained. All of the ingredients
are sieved in a number 12 sieve prior to combining.
[0082] To 3650 mg of the base, 1300 mg citric acid, 20 mg
sucralose, 20 mg VELTOL ULTRA flavor agent (Danisco, St. Louis
Mo.), 130 mg natural orange flavor, 20 mg natural tangerine flavor,
20 mg natural peach flavor, and 20 mg natural grapefruit flavor are
added. The ingredients are placed in a plastic bag and shaken until
a uniform granulation is obtained as determined by visual
observation.
[0083] The resulting composition is expected to be a dark brown
liquid with sediment on the bottom of the glass.
Example 2
[0084] To 3650 mg of the base of Example 1, 1400 mg citric acid, 20
mg sucralose, 20 mg VELTOL ULTRA flavor agent, and 100 mg
artificial ice tea flavor are added. The ingredients are placed in
a plastic bag and shaken until a uniform granulation is obtained as
determined by visual observation.
[0085] The granulation of Example 2 is placed in a number of air
tight sealed metal foil pouches. The stability of the packaged
granulations of Example 2 at room temperature (RT), 40.degree. C.
at 75% relative humidity and 45.degree. C. is studied for four
weeks and the expected results are set forth in Table 1. No puffing
is expected.
TABLE-US-00001 TABLE 1 Example 1 Week 2 Weeks 3 Weeks 4 Weeks 2 RT
40.degree. C. 45.degree. C. RT 40.degree. C. 45.degree. C. RT
40.degree. C. 45.degree. C. RT 40.degree. C. 45.degree. C. Puffing?
No No No No No No No No No No No No
Example 3
[0086] An effervescent tablet is prepared by combining the
following ingredients with manual mixing until uniform to form a
base: 900 mg sorbitol instant, 850 mg No. 5 sodium bicarbonate, 100
mg sodium carbonate grade 50, and 1000 mg dried wild guava leaf
extract (boiling water soluble extract). Each of the ingredients is
sieved through a number 12 sieve prior to combining.
[0087] To 2850 mg of the base is added 1500 mg citric acid
anhydrous fine granular, 30 mg mineral oil, 25 mg sucralose, 150 mg
natural orange flavor, 35 mg natural tangerine flavor, 25 mg
natural grapefruit flavor, and 15 mg natural peach flavor.
[0088] The composition is then formed into tablets using a tablet
press to an average mass of 4.64 g, average thickness of 0.261 in
and average hardness of 8 kP. The tablets are expected to
disintegrate in one minute 40 seconds in room temperature tap water
to a black suspension of guava. Some sediment is expected on the
bottom of the glass. The taste is expected to be good.
Example 4
[0089] To 2850 mg of the base prepared above in Example 3 is added
1500 mg citric acid anhydrous fine granular, 30 mg mineral oil, 25
mg sucralose, 150 mg natural orange flavor, 35 mg natural tangerine
flavor, 25 mg natural grapefruit flavor, 15 mg natural peach
flavor, and 5 mg FD&C Red food coloring number 40.
[0090] The composition is then formed into tablets using a tablet
press to an average mass of 4.74 g, average thickness of 0.272 in
and average hardness of 7.1 kP. The tablets are expected to
disintegrate in two minutes in room temperature tap water to a
dispersion having black foam on the surface includes particulate
suspended throughout, and a deep red purple color.
Dosing Study
[0091] Group I
[0092] Each test subject in a first test group consumed a beverage
that included an approximately 5 g tablet prepared according the
method of Example 4 dissolved in approximately 8 ounces of tap
water. The test subjects then consume alcoholic beverages for a
period of approximately one hour. Most test subjects consume three
or more alcoholic beverages.
[0093] After one hour of drinking each test subject is tested
according to the Breath Alcohol test method set forth above. The
expected results are reported in Table 2.
TABLE-US-00002 TABLE 2 BAC Volunteer Gender Age Height Weight
Reading 1 M 25-29 5'8-6' >200 0.06 2 M 25-29 5'8-6' >200 0.02
3 M 40-49 5'8-6' >200 0.05 4 M 30-39 5'8-6' 176-200 0.08 5 F
25-29 5'3-5'7 176-200 0.08 6 F 25-29 5'8-6' 151-175 0.07 7 F 40-49
5'3-5'7 136-150 0.12 8 F 30-39 5'3-5'7 136-150 0.10 9 F 30-39
.ltoreq.5'2 136-150 0.06 10 F 25-29 5'3-5'7 110-135 0.06
Group II
[0094] Each test subject in a second test group consumes alcoholic
beverages for a period of approximately one hour. Most test
subjects consume three to five alcoholic beverages. Each test
subject is tested according to the Breath Alcohol Content test
method (the results are identified as BAC Reading 1). Each test
subject then consumes a tablet prepared according to Example 4 and
then rests for 25 minutes. Each test subject is then tested again
according to the Breath Alcohol Content test method (the results
are identified as BAC Reading 2). The expected results are reported
in Table 3.
[0095] Note that test subject 11 consumes 5 drinks and is re-tested
twenty minutes after the first test conducted at the original 25
minute interval. His blood alcohol is expected to register a drop
from 0.14 to 0.10.
TABLE-US-00003 TABLE 3 Sub- Gen- No. of BAC BAC ject der Age Height
Weight Drinks Reading 1 Reading 2 11 M 30-39 5'8-6' >200 5 0.14
0.12 12 F 30-39 5'8-6' 176-200 Un- 0.10 0.08 known 13 M 40-49
5'8-6' 176-200 4 0.15 0.09 14 M 40-49 5'8-6' 176-200 3 0.13 0.14 15
M 25-29 5'8-6' 176-200 4 0.11 0.10 16 F 40-49 5'3-5'7 151-175 3
0.13 0.07 17 M 40-49 5'8-6' 151-175 3 0.08 0.12 18 F 25-28 5'3-5'7
151-175 3 0.12 0.03 19 F 30-39 5'3-5'7 136-150 5 0.16 0.10
[0096] Other embodiments are within the claims.
* * * * *