U.S. patent application number 12/504480 was filed with the patent office on 2009-11-12 for palatinose for enhancing dietary supplement and pharmaceutical delivery.
Invention is credited to Bruce W. Kneller.
Application Number | 20090281055 12/504480 |
Document ID | / |
Family ID | 36653516 |
Filed Date | 2009-11-12 |
United States Patent
Application |
20090281055 |
Kind Code |
A1 |
Kneller; Bruce W. |
November 12, 2009 |
PALATINOSE FOR ENHANCING DIETARY SUPPLEMENT AND PHARMACEUTICAL
DELIVERY
Abstract
The present invention is directed to a dietary supplement
comprising palatinose or a derivative thereof. The dietary
supplement may be a nutritional product, a sports performance
product, a weight loss product or a meal replacement product. The
present invention is also directed to a method of increasing the
absorption of a compound into the bloodstream, cells and tissue
comprising administering palatinose, or a derivative thereof, in
combination with the compound. The present invention also relates
to a diluent for parenteral compounds. The diluent comprises
palatinose or a derivative thereof. Another aspect of the present
invention is directed to a method of decreasing the recovery time
to pre-performance levels of total adenosine triphosphate (ATP)
levels in a mammal comprising administering palatinose, or a
derivative thereof, to the mammal. The present invention is further
directed to a method of supplying a compound to a diabetic patient,
burn victim patient or trauma victim patient. The method comprises
administering palatinose, or a derivative thereof, in combination
with the compound.
Inventors: |
Kneller; Bruce W.;
(Randolph, MA) |
Correspondence
Address: |
MORSE, BARNES-BROWN & PENDLETON, P.C.;ATTN: IP MANAGER
RESERVOIR PLACE, 1601 TRAPELO ROAD, SUITE 205
WALTHAM
MA
02451
US
|
Family ID: |
36653516 |
Appl. No.: |
12/504480 |
Filed: |
July 16, 2009 |
Related U.S. Patent Documents
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Application
Number |
Filing Date |
Patent Number |
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11385137 |
Mar 20, 2006 |
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12504480 |
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60663384 |
Mar 19, 2005 |
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Current U.S.
Class: |
514/53 |
Current CPC
Class: |
A61K 31/566 20130101;
A61K 31/7076 20130101; A61K 31/197 20130101; A61K 45/06 20130101;
A61K 31/7016 20130101; A61K 38/05 20130101; A61K 33/00 20130101;
A61K 31/122 20130101; A61K 9/0019 20130101; A61K 31/70
20130101 |
Class at
Publication: |
514/53 |
International
Class: |
A61K 31/7016 20060101
A61K031/7016 |
Claims
1-27. (canceled)
28. A method of decreasing recovery time to pre-performance levels
of total adenosine triphosphate (ATP) levels in a mammal comprising
administering palatinose and one or more of creatine, a creatine
salt, a creatine ester and a creatine chelate to the mammal.
29. A method of increasing the absorption of one or more of
creatine, a creatine salt, a creatine ester and a creatine chelate
in a mammal comprising administering to the mammal palatinose and
one or more of creatine, a creatine salt, a creatine ester and a
creatine chelate.
30. The method of claim 28, wherein administering palatinose and
one or more of creatine, a creatine salt, a creatine ester and a
creatine chelate also reduces fatigue associated with athletic
activity of the mammal.
31. The method of claim 28 or 29, wherein the palatinose and one or
more of creatine, a creatine salt, a creatine ester and a creatine
chelate are administered in a solution with water or saline.
32. The method of claim 28 or 29, further comprising administering
a dietary supplement or nutrient along with said palatinose and one
or more of creatine, a creatine salt, a creatine ester and a
creatine chelate.
33. The method of claim 32 wherein palatinose and/or one or more of
creatine, a creatine salt, a creatine ester and a creatine chelate
are added to a dietary supplement or nutrient formulation prior to
administration.
34. The method of claim 31, wherein the concentration of palatinose
in the solution is between approximately 1% and approximately
85%.
35. The method of claim 31, wherein the concentration of palatinose
in the solution is between about 10% and about 50%.
36. The method of claim 33, wherein the palatinose is added to the
dietary supplement or nutrient formulation prior to administration
and wherein the concentration of palatinose in the dietary
supplement or nutrient formulation is between approximately 1% and
approximately 85%.
37. The method of claim 33, wherein the palatinose is added to the
dietary supplement or nutrient formulation prior to administration
and wherein the concentration of palatinose in the dietary
supplement or nutrient formulation is between about 10% and about
50%.
38. The method of claim 28 or 29, wherein the palatinose and one or
more of creatine, a creatine salt, a creatine ester and a creatine
chelate are administered orally or parenterally.
39. The method of claim 28 or 29, wherein the palatinose is
administered in a dose between about 0.5 grams and about 200
grams.
40. A method of increasing the absorption of a compound into the
bloodstream, cells or tissue of a mammal comprising: administering
palatinose and one or more of creatine, a creatine salt, a creatine
ester and a creatine chelate in combination with the compound to
the mammal.
41. The method of claim 40, wherein the compound is a dietary
supplement or a nutrient.
42. A dietary supplement comprising palatinose and one or more
vitamins.
43. The dietary supplement of claim 42, further comprising one or
more compounds selected from the group consisting of a sugar, a
stimulant, an amino acid, and a mineral.
44. A dietary supplement comprising palatinose and one or more
minerals.
45. The dietary supplement of claim 44, further comprising one or
more compounds selected from the group consisting of a sugar, a
stimulant, an amino acid, and a vitamin.
Description
RELATED APPLICATIONS
[0001] This application is a continuation of U.S. application Ser.
No. 11/385,137, filed on Mar. 20, 2006, which claims the benefit of
U.S. Provisional Application No. 60/663,384, filed Mar. 19, 2005.
The entire teachings of the above applications are incorporated
herein by reference.
BACKGROUND OF THE INVENTION
[0002] 1. Technical Field
[0003] The present invention relates to a disaccharide for
therapeutic use. More particularly, the invention relates to the
use of palatinose (6-O-alpha-D-glucopyranosyl-D-fructofuranose) to
increase the efficacy of dietary supplements and
pharmaceuticals.
[0004] 2. Description of Related Art
[0005] Palatinose is a disaccharide consisting of d-glucose and
d-fructose connected by an alpha-1,6-glycosidic linkage. It is also
referred to as 6-O-alpha-D-glucopyranosyl-D-fructofuranose and as
isomaltulose, and is readily produced commercially from sucrose by
enzymatic rearrangement. Palatinose has a taste and appearance
similar to that of sucrose. Because of the rate by which it is
metabolized, it presents potential dietary and therapeutic
uses.
[0006] Most sugars are rapidly absorbed after consumption. Therein,
after oral administration of a significant amount of sucrose
(common table sugar), blood glucose levels rise quickly. This is
followed by a quick rise in insulin levels which brings the blood
glucose level back down. The digestion and absorption of palatinose
is unlike other sugars. It is completely digested and absorbed at a
much slower speed, equivalent to about 1/5 of that for sucrose.
Thus, after oral administration of palatinose, blood glucose and
insulin levels rise more slowly and reach a lower maxima compared
to sucrose. Because of this characteristic, palatinose is well
suited as a sucrose replacement for diabetics and others with
prediabetic dispositions.
[0007] Another benefit of palatinose is its non-cariogenic quality,
i.e., does not promote tooth decay. It is used as a substitute for
other sugars, particularly in the candy and chewing gum industry.
Moreover, it is an improvement over other sugar-substitutes because
it does not cause abdominal discomfort or diarrhea, a side-effect
of many sugar alcohols.
[0008] Many compounds, including nutrients and dietary supplements,
depend on the presence of a sugar for absorption from the
gastrointestinal tract as well as for absorption from the plasma
into various tissues/cells of the body. Studies have demonstrated
that the performance enhancing supplement creatine is better
absorbed into human skeletal muscle when taken with glucose.
Certain amino acids are also more readily absorbed when
administered with glucose. However, sucrose and other sugars are
not ideal for use in combination with nutrient supplements. Sucrose
is rapidly digested and absorbed into the blood stream. This
results in a rapid rise in circulating insulin levels which quickly
lowers circulating glucose levels. As a result, many compounds and
nutrients administered in combination with sucrose may not be
absorbed because of the short duration of the "sugar effect."
[0009] Moreover, excessive amounts of sugar can cause an increase
in body fat, decreased sensitivity to insulin and tooth decay.
Sugar substitutes, which are generally sugar alcohols, are also
inadequate for purposes of aiding absorption. Although they are
hydrolyzed and digested slowly, they often cause abdominal
discomfort and diarrhea. Thus, an improved sugar is needed for use
in the absorption of dietary supplement products as well as other
therapeutic compounds.
SUMMARY OF THE INVENTION
[0010] The present invention solves the above-described problem by
providing a dietary supplement comprising palatinose or a
derivative thereof, a sugar, a stimulant, at least one amino acid
or derivative thereof, and at least one mineral. The dietary
supplement may be a nutritional product, a sports performance
product, a weight loss product, or a meal replacement product.
Palatinose enhances absorption of the dietary supplement components
into the bloodstream, cells and tissue.
[0011] More particularly, the dietary supplement may comprise
palatinose or a derivative thereof; amylose; glucose; a
methylxanthine such as caffeine or theobromine or both; arginine or
a salt, ester or chelate thereof; creatine or a salt, ester or
chelate thereof; disodium adenosine triphosphate; calcium
carbonate; sodium bicarbonate; and glucuronolactone. This dietary
supplement formulation increases the athletic performance of a
mammal during an approximately one to three hour period.
[0012] Still more particularly, the dietary supplement of the
present invention may comprise palatinose or a derivative thereof;
trehalose; amylose; amylopectin; L-carnosine; calcium carbonate;
sodium bicarbonate; sulbutiamine or fursultiamine; disodium
adenosine triphosphate; orotic acid; vinpocetine or rhodiola rosea;
and cellulose or another undigestible bulk forming starch. This
dietary supplement formulation increases the athletic performance
of a mammal during an approximately three to eight hour period.
[0013] Another aspect of the present invention is directed to a
method of increasing the absorption of a compound into the
bloodstream, cells and tissue. The method includes administering
palatinose or a derivative thereof in combination with the
compound.
[0014] More particularly, the compound may be a dietary supplement,
a nutrient, a pharmaceutical, or a vaccine. If the compound is a
dietary supplement formulation, the method may comprise adding
palatinose or a derivative thereof to the dietary supplement
formulation prior to administration. If the compound is a
pharmaceutical formulation, the method may comprise adding
palatinose or a derivative thereof to the pharmaceutical
formulation.
[0015] Still, another aspect of the present invention is directed
to a diluent for parenteral compounds, wherein the diluent
comprises palatinose or a derivative thereof. The parenteral
compound may be a dietary supplement, a nutrient, a pharmaceutical,
or a vaccine.
[0016] Yet, another aspect of the present invention is directed to
a method of decreasing recovery time to pre-performance levels of
total adenosine triphosphate (ATP) levels in a mammal comprising
administering palatinose, or derivative thereof, to the mammal. The
palatinose or derivative thereof may be administered orally or
parenterally. Preferably, the alatinose or derivative thereof is
administered in a dose between about 0.5 grams and about 200
grams.
[0017] The present invention is also directed to a method of
supplying a compound to a diabetic patient, burn victim patient or
trauma victim patient. The method includes administering
palatinose, or a derivative thereof, in combination with the
compound. The compound may be a nutrient, dietary supplement, or
pharmaceutical. The compound and palatinose or derivative thereof,
may be administered orally or parenterally. In addition, the
palatinose or derivative thereof is preferably administered in a
dose between about 0.5 grams and about 200 grams.
[0018] Other features and advantages of the present invention will
become apparent upon reading the following detailed description of
embodiments of the invention, when taken in conjunction with the
appended claims.
DETAILED DESCRIPTION
[0019] Studies have demonstrated that the presence of sugar
directly enhances nutrient absorption into various tissues and
cells. For example, a mixture of arginine and glucose is more
efficiently absorbed into the vascular endothelium than arginine
alone. Other studies have shown that nutrients and ergogenic sports
performance products depend on the indirect presence of sugar for
absorption wherein increased levels of insulin enhance the
absorption of nutrients into the tissues and cells.
[0020] Palatinose offers an improvement over other sugars,
including glucose, in that it is metabolized much slower by the
gastrointestinal tract thereby extending the time that the "sugar
effect," both direct and indirect, can have on the absorption of
dietary supplements, nutrients, pharmaceuticals or vaccines. Rather
than enter the blood stream, rapidly rise and fall, palatinose
leads to gradual increases and sustained levels of glucose and
insulin. This allows greater time and opportunity for the
absorption of various compounds. With respect to dietary
supplements, the end result may be greater energy, alertness,
athletic performance and/or muscle development.
[0021] Moreover, replacing common sugars with palatinose presents
other advantages. Preventing surges in blood glucose and insulin
levels may help in the management and prevention of obesity,
diabetes and cardiovascular disease. Recent studies have also
provided evidence that palatinose may also have a positive effect
on mental concentration. And unlike other sugars, palatinose does
not promote tooth decay.
[0022] The Dietary Supplement Health and Education Act of 1994,
commonly referred to as DSHEA, defines "dietary supplement" as any
product (except tobacco) that contains at least one of the
following: (1) a vitamin, (2) a mineral, (3) an herb or botanical,
(4) an amino acid, (5) a dietary substance "for use to supplement
the diet by increasing total dietary intake," or (6) any
concentrate, metabolite, constituent, extract, or combination of
any of the aforementioned ingredients. Examples of dietary
supplements include, but are not limited to nutritional products;
sports performance products, including ergogenic sports performing
products; weight loss products; and meal replacement products.
Dietary supplements may exist in various forms, including, but not
limited to tablets, capsules, caplets, powders, drinks including
shakes, solid food items including snack bars, etc.
[0023] In one embodiment, the dietary supplement of the present
invention includes palatinose or a derivative thereof, a sugar, a
stimulant, at least one amino acid or derivative thereof, and at
least one mineral. For example, a dietary supplement designed to
increase the athletic performance of a mammal during a one to three
hour sports activity period, preferably comprises palatinose or a
derivative thereof; amylose; glucose; a methylxanthine such as
caffeine or theobromine or both; arginine or a salt, ester or
chelate thereof; creatine or a salt, ester or chelate thereof;
disodium adenosine triphosphate; calcium carbonate; sodium
bicarbonate; and glucuronolactone.
[0024] Alternatively, the dietary supplement of the present
invention may comprise palatinose or a derivative thereof;
trehalose; amylose; amylopectin; L-carnosine; calcium carbonate;
sodium bicarbonate; sulbutiamine or fursultiamine; disodium
adenosine phosphate; orotic acid; vinpocetine or rhodiola rosea;
cellulose or another undigestible bulk forming starch; and perhaps
at least one B vitamin. This dietary supplement formulation
increases the athletic performance of a mammal during an
approximately three to eight hour period.
[0025] Other preferred dietary supplement formulations of the
present invention may comprise palatinose or a derivative thereof,
and any or all of the following: water; carbon dioxide; creatine or
a salt, ester or chelate thereof; camitine or a salt, ester or
chelate thereof; taurine or a salt, ester or chelate thereof;
arginine or a salt, ester or chelate thereof; citrulline or a salt,
ester or chelate thereof; carnosine or a salt, ester or chelate
thereof; pyruvate or a salt, ester or chelate thereof; ribose;
amylase; amylopectin; tyrosine or a salt, ester or chelate thereof;
tyramine or a salt, ester or chelate thereof; histidine or a salt,
ester or chelate thereof; alanine or a salt, ester or chelate
thereof; phenylalanine or a salt, ester or chelate thereof;
adenosine mono, di or triphosphate, or a salt, ester or chelate
thereof; alpha lipoic acid, or a salt, ester or chelate thereof;
4-hydroxy-isoleucine; d-pinitol; ornithine or a salt, ester or
chelate thereof; sodium or any salt thereof; potassium or any salt
thereof; zinc or any salt thereof; magnesium or any salt thereof;
iron or any salt thereof; chromium or any salt thereof; calcium or
any salt thereof; vitamin B-1; vitamin B-2; vitamin B-3; vitamin
B-6; vitamin B-12; pantothenic acid; folic acid; vitamin C;
7-keto-DHEA, or any ester or ether thereof; 7-hydroxy-DHEA or any
ester thereof; caffeine; octopamine; norsynephrine; synephrine;
ephedrine; hordenine; theobromine; evodiamine; phenylephrine;
insulin; metformin; corosolic acid; glucuronolactone; ginger;
ginseng; ginko biloba; rhodiola rosea; fenugreek; epicatechin;
epicatechin-3-gallate; epigallocatechin; epigallocatecin-3-gallate;
glutamine; branched chain amino acids or any salts or esters
thereof; any chelate of any amino acid; 6-methyluracil;
phosphocreatinine; orotic acid; 5-hydroxytryptophan; vinpocetine;
sucralose; fructose; galactose; maltodextrin; glucose; DMAE; DMG;
TMG; coenzyme Q-10, sulbutiamine; fursultiamine; octotiamine;
adrafanil; choline; phosphatidylcholine; and
phosphatidylserine.
[0026] Due to the presence of palatinose, or derivative thereof, in
the dietary supplements of the present invention, these dietary
supplements increase athletic performance, energy, strength,
percent fat-free muscle mass, muscle development, mental
concentration and alertness, and stamina in mammals.
[0027] It should be understood that palatinose may be added to any
dietary supplement formulation to enhance the effects of and
improve the absorption of the dietary supplement, and the present
invention is intended to encompass such improved formulations. It
should also be understood that use of the palatinose in any of the
embodiments or methods of the present invention may be substituted
by any derivative of palatinose.
[0028] Preferably, the concentration of palatinose, or derivative
thereof, in the dietary supplement is between approximately 1% and
approximately 85%. More preferably, the concentration of palatinose
in the dietary supplement is between approximately 10% and
approximately 50%. Furthermore, the palatinose present in the
dietary supplement is desirably administered in a dose between
about 0.5 grams and about 200 grams.
[0029] The present invention is also related to a method of
increasing the absorption of a compound into the bloodstream, cells
and tissue by administering palatinose, or a derivative thereof, in
combination with the compound. Palatinose may be used to increase
the absorption of any compound in the method of the present
invention, including compounds used to treat any disease or
illness. Exemplary compounds for use in the present invention
include, but are not limited to a dietary supplement, a nutrient, a
pharmaceutical, or a vaccine. When palatinose is used to increase
the absorption of particular compounds, including dietary
supplements and nutrients, the fatigue associated with an athletic
performance of a mammal is reduced.
[0030] In addition, because palatinose maintains a more constant
elevation of blood sugar levels as opposed to other sugars, an
optimal maximum rate of adenosine triphosphate (ATP) synthesis in
cells can be maintained for several hours. Most sugars, including
glucose, peak in the plasma about 45 to 60 minutes post absorption
and then an insulin spike drives this level down rapidly, leading
to pre-prandial (or lower) levels of plasma sugar. When the plasma
sugar levels decrease, ATP synthesis also decreases. Palatinose
maintains a slightly heightened plasma sugar level for a longer
period of time. As a result, mitochondria have access to optimal
levels of carbohydrates for approximately 6 to 8 hours, thereby
allowing for heightened and continued ATP synthesis. Accordingly,
the administration of palatinose, or a derivative thereof, to a
mammal decreases the recovery time to pre-activity performance
levels of total ATP in the mammal. Preferably, palatinose is
administered prior to the sports performance.
[0031] The method of the present invention may include adding
palatinose, or a derivative thereof, to a dietary supplement
formulation, pharmaceutical formulation or vaccine formulation
prior to administering the respective compounds. Preferably, the
concentration of palatinose or derivative thereof, in the dietary
supplement, pharmaceutical, vaccine or other formulation, is
between approximately 1% and approximately 85%. More preferably,
the concentration of palatinose or derivative thereof, in the
dietary supplement, pharmaceutical, vaccine or other formulation,
is between approximately 10% and approximately 50%. Furthermore,
the palatinose, or derivative thereof, is desirably administered in
a dose between about 0.5 grams and about 200 grams.
[0032] Additional examples of compounds that may be used in the
method of the present invention include, but are not limited to
phosphatidyserine; S-adenosyl-methionine; nicotinamide adenine
dinucleotide; any cephalosporin antibiotic; any macrolide
antiobiotic; any aminoglycoside; antibiotic; any penicillin
antibiotic; any fluroquinolone antibiotic; any tetracycline
antibiotic; chloramphenicol; any protease inhibitor antiviral; any
nucleoside analog antiviral; any reverse transcriptase inhibitor
antiviral; any polyene or membrane active antimycotic; any azole or
inhibitor of ergosterol biosynthesis antimycotics; griseofulvin;
flucytosine; capsofungin; mycafungin; any pneuraminidase inhibitor
antiviral; any polymerase inhibitor antiviral; any class of
interferon; any class of interleukin; any type of human growth
hormone; any type of insulin growth factor or insulin like growth
factor; any type of anti-vascular endothelial growth factor
antibodies; any alkylating agent including those used to treat
cancer of any type; any antimetabolite agent including those used
to treat cancer of any type; any plant alkaloid agent including
those used to treat cancer of any type; doxorubicin or any salt,
ester, or chelate thereof; mitoxantrone or any salt, ester or
chelate thereof; bleomycin or any salt, ester, ether or chelate
thereof; platinum or any salt, ester, ether or chelate thereof;
paclitaxel; docetaxel; epoeitin alfa; and darboepoeitin alfa.
[0033] The compound and palatinose may be administered by any
method known to those having skill in the art including, but not
limited to oral and parenteral administration. The compound and
palatinose may also be administered in a solution of water or
saline, wherein the saline is hypotonic, hypertonic or normotonic
saline. Palatinose, or a derivative thereof, may also be used as a
diluent for any parenteral compound, including, but not limited to
dietary supplements, nutrients, pharmaceuticals and vaccines.
[0034] Palatinose is particularly useful for supplying any
compound, including nutrients and pharmaceuticals, to patients,
such as diabetic, burn victim, and trauma victim patients.
[0035] It should be understood that the foregoing relates to
exemplary embodiments of the invention and that modifications may
be made without departing from the spirit and scope of the
invention as set forth in the following claims.
* * * * *