Note: Descriptions are shown in the official language in which they were submitted.
CA 02246014 1998-08-21
The present invention is directed to food supplements which comprise lipoic
acid or derivative thereof and creative or a derivative thereof, and to
methods far
supplementing the diet of an attdete and methods for enhancing an athlete's
muscle
size or strength, which methods employ these food supplements.
Creative (atso lmown as N-methyl-N-guavyl glycine or (alpha meth~rl
guanido) acetic acid) is an amino acid compound produced naturally in the
liver and
kidneys and obtained from food such as meat and fish. Food supplements
containing creative, typically creative tnonohydrate, are commonly used by
athletes
to allow them to train harder and enhance muscle size and strengfih. Various
commercial products comaining creative monohydrate are available.
Lipoic acid (also known as alpha lipoic acid, thioctic acid or 6,$-difbio
octanoic acid) is a nutrient that the human body makes in minute quantities
and may
1 S be obtained from yeast and liver, Studies have shown that ligoic acid can
significantly increase the body's utilization of blood sugar iv type a
diabetics and
tbat lipoic acid may increase the metabolic clearance rate of glucose by 50 %
in
diabetics. In LGUrope, lipoic acid has been used as a substitute for insulin
in the
treatment of Type iT diabetes.
Food supplements for enhancing an athlete's muscle size and strength have
become popular substitutes for steroids and other drugs in various sports and
body
CA 02246014 1998-08-21
building regimes. However, as athletes continually strive for improved
performance, there is a canting need for non-steroid containing aids for
improving muscle size and strength.
Accordingly, it is an object of the present invention to provide new food
supplements, It is a more specific object of the invention to provide food
supplements particularly adapted for supplementing the diet of an athlete. Tt
is
another object to provide food supplements which may enhance an athlete's
muscle
size or strength. It is a farther object of the invention to provide non-
steroid
containing food supplements and to provide food supplem,eats which zaay be
conveniently administered to the diet of an athlete,
These and additional objects are provided by the food supplements and
methods according to the present invention. The food supplements comprise
lipoic
acid or a derivative thereof, for example a salt or ester thereof, and
crcatine or a
derivative thereof, for example a hydrate, salt ar ester thereof. The food
supplements may optionally, and preferably, further comprise dextrose. It has
been
determined that such food supplement compositions are advantageous for
supplementing the diet of an athlete and may provide surprising enhancement of
an
athlete's muscle size or strength when administered to an athlete's diet.
'these and
additional objects and advantages will be more fully apparent in view of the
following detailed description.
2
CA 02246014 1998-08-21
The food supphment compositions of the present invention comprise lipoic
acid or a derivative thereof and creative or a derivative thereof. Creative
and
hydrates thereof, partzculaxiy creative monohydrate, are kvowti to improve
and/or
enhance muscle size andlor strength. The food supplements anti methods of the
present invention may provide further and significant muscle size and strength
enhancement or improvement as compared with supplements and methods
employing only creative or a hydrate thereof. Although the present invernion
is not
to be limited by any theoretical explanation, it is believed that insulin is a
primacy
factor that stimulates glucose and creative transport into the muscle cells
and that the
lipoic acid both mimics and enhances the actions of insult in glucose and
creative
transport into the muscle cells. In preferred embodiments, the compositions
further
include dextrose which has been shown to stimulate insulin action.
The food supplements comprise lipoic acid or a derivative thereof, for
example a salt or ester thereof. Suitable salts include, but are not limited
to, alkali
and alkalise earth meral salts, for example sodium, potassium or calcium
salts,
while suitable esters include, but are not limited to, alkyl esters, for
example,
methyl, ethyl or propyl esters, or lactone esters.
The food supplement compositions further comprise creative or a derivative
thereof, for example a hydrate, salt or ester thereof. Commercially available
creative derivatives include creative monohydrate, other creative hydrates,
creative
citrate and creative pyruvate. The creatirLe which is employed in the food
supplement compositions of the present invention preferably comprises creative
CA 02246014 1998-08-21
monohydrate, commercially available from various sources. It is similarly
preferred
that the creative, creative monohydrate or other creative derivative is a
pharmaceutical-grade material. As set forth above, the food supplement
compositions also preferably further conagrise dextrose (glucose), with
pbarmaceutical~grade dextrose being preferred.
The food supplement COInpOSltIOnS of the present invention may be provided
in liquid or powder form, with powders suitable for mixiag with water or other
liquids being preferred. The food supplement compositions in powder ox
granular
form may be provided in accordance with customary processing techniques, for
example as spray dried powders, or the like. Owing to the lipoic acid
component,
the food supplement compositions generally exhibit an acidic pH value.
The lipoic acid or salt, ester or other derivative thereof is employed in the
food supplement compositions according to the present invention in an amount
sufficient to increase creative transport into the muscle cells. In a
preferred
embodiment, the food supplement compositions comprise from about 0.1 mg to
about i0 mg lipoic acid or derivative thereof per gram of supplement and from
about 0.01 g to about 0.5 g of creative, preferably creative monohydrate, or
derivative thereof, per gram of supplement. In further preferred embodiments,
the
food supplement compositions comprise from about 0.5 mg to about 5 mg lipoic
acid derivative thereof per gram of supplement and fmm about 0.05 g to about
0.25
g of create or derivative thereof per gram of supplevzevr. Even mare
preferably
the food supplement compositions comprise fTOm about 1 mg to about 3 mg lipoic
acid, salt, ester or other derivative thereof per gram of supplement and from
about
4
CA 02246014 1999-O1-28
! ,
0.05 g to about 0.2 g of creatine, cxeatine monohydrate or other derivative
thereof
per gram of supplement. Food supplement compositions further comprising
deztrose preferably include the deztrose in an amount sufficient to stimulate
insulin
secretion and preferably the food supplement compositions comprise from about
0.1
g to about 0.9 g dextrose per gram of supplement. In fitrther preferred
erabodiments, the food supplement compositions cotuprise from about 0.4 g to
about
0.9 g dextrose per dram of supplement, and more preferably comprise from about
0.5 g to about 0.$ g dextrose per Gram of supplement. Most preferably, the
food
supplement compositions comprise about 0.75 g dextrose per gram of supglt,
The food supplemem compositions according to the present invention may
further contain additional camponents to further increase the speed at or ease
with
which creative enters the bloodstream and subsequernly the muscle tissue, or
to
otherwise enhance the effec~s of the creative in the body. For example,
additional
amino acids may be included in the food supplement compositions. Suitable
amino
acids include, but are not limited to, glutamine, aIanine, taurine, carnitine,
acetyl-~._
carnitine, and the like. These additional amino acids may stimulate cell
volumization and protein synthesis and therefore provide further advantages to
increasing muscle strength andlor size. These amino acids may be employed
individually or in various combinations and in amounts customary in the art,
for
example in the range of from about 0.01 mg to about 100 mg per p am of food
supplement.
In a further preferred embodiment, the food supplement compositions also
include a ehromiurn campound. Again, while not intending to be limited by
theory,
5
CA 02246014 1998-08-21
various studies have indicated that chromium supplementing will improve
glucose
tolerance in insulyn-sensitive individuals by up to 50 ~ and thereby maximize
insulin
efficiency. Chromium is a~coustituent of a biologically active compound, the
glucose tolerance factor (CrTF), found in foods such as organ meats, whale
grains,
cheese, mushrooms and brewer's yeast. Various chromium compounds may be
included in the food supplement compositions, and in amounts effective to
improve
insulin efficiency. A preferred chromium compound is chromium picolinate,
which
may be included, for example in an amount of from about SO to about 500
micrograms get 100 grams of supplement. Additional components for the food
supplement compositions include additional minerals such as magnesium,
potassium,
phosphorous, salts thereof, or mixtures thereof in amounts conventional in the
art,
for example, from about 0.01 mg to about 100 mg per gram of food supplement.
The food supplement compositions also preferably contain ascorbic acid
(vitamin
C), for example is amounts equal to or exceeding the recommended minimum daily
requirements. Another component for use in the food supplements comprises beta-
hydroxy, beta-methyl butyrate (H1V1H), in amounts known in the art.
The food supplement compositions may further comprise natural and/or
artificial flavoring components, dyes or other coloring additives,
preservatives and
other conventional food supplement additives ltnown in the art.
The food supplements according to the present invention may be employed in
methods for supplementing the diet of an athlete, andlar for enhancing an
athlete's
muscle size or strength. The food supplement compositions of the present
invention
are particularly advantageous for creating an increased anabolic environment
and
CA 02246014 1998-08-21
obtaining extra growth in lean muscle mass and strength. The amount of the
food
supplement composition which is administered to the diet of the athlete may
vary
depending on the desired effect, the body weight and characteristics of the
athlete,
and the like. >~or example, in preferred methods for supplementing the diet of
an
S athlete andlor for enhancing an athlete's muscle size or strength, from
about 10 mg
to about 1,000 mg of Iipoic acid, salt, ester or other derivative thereof and
from
about 1 g to about 50 g of creative, creative monohydrate, or other derivative
thereof are administered to the diet of the athlete on a daily basis. In more
preferred
embodiments of these methods, from about 50 mg to about 500 zng of lipoic acid
or
derivative thereof and from about 5 g to about 25 g of creative, creative
monohydrate or other derivative thereof are administered to the diet of the
athlete on
a daily basis. The food supplement may be administered in a single serving or
in
multiple servings spaced throughout the day. In alternate preferred
embodiments,
from about I00 mg to about 300 mg of lipoic acid or derivative thereof and
from
about 5 g to about 20 g of creative, creative monohydrate or other derivative
thereof
are administered to the diet of the athlete on a daily basis.
To facilitate such administration, preferred embodiments of the food
supplement of the invention comprise from about 0. I mg to about IO mg lipoic
acid
or derivative thereof per gram of supplement and fzom about O.pI g to about
O.S g
of creative, creative monohydrate, or other derivative thereof per gram of
supplemem, and the supplement is administered in as amount of from about I0 g
to
about 500 g per day, In additional embodiments, such supplements are
administered
7
CA 02246014 1998-08-21
in an amount of from about 50 g to about 300 g per day, in one or multiple
servings
throughout the day.
rn additional embodiments wherein the supplement furtheZ comprises
dextrose, from about 10 mg to about 1,000 mg of upoic acid or derivative
thereof,
from about 1 g to about 50 g of creative, creative monohydrate or other
derivative
thereof, and from about 10 g to about 300 g of dextrose are administered to
the diet
of the athlete on a daily basis, In further preferred embodiments, from about
50 mg
to about 500 mg of lipoic acid or derivative thereof, from about S g to about
25 g of
creative, creative monohydrate, or other derivative thereof, and. from about
50 g to
about 200 g of dextrose administered to the diet of the athlete on a daily
basis.
Most preferably, each supplement serving comprises from about 100 mg to about
300 mg lipoic acid or a derivative thereof, from about 5 g to about 20 g of
creative,
creative monohydrate or other derivative thereof, and ixom about SO g to about
90
g, more preferably about 75 g, of dexanse.
When the food supplement further comprises dextrose, a supglement
comprising from about 0.1 mg to about 10 mg lipoic acid or derivative thereof
per
gram of supplement, from about 0.01 g to about 0.5 g of creative or derivative
thereof ger gram of supplement, and from about 0.1 g to about 0.9 g dextrose
per
gram of supplement, preferably from about 0.5 g to about 0.8 g dextrose per
gram
of supplement, may be administered in an amount of from about 10 g to about
S00
g, more preferably from about 50 g to about 300 g, per day.
rn one embodiment of the methods according to the present invemion,
increased servings of the food supplement according to the present invention
may be
CA 02246014 1998-08-21
initially administered to the athlete's diet in order to increase ox enhance
the
athlete's muscle size or strength, followed by a maintenance period in which
decreased servings of the food supplement may be administered. The initial
period
may be at least several days and may extend up to several woks as desired.
Once a
desired muscle strength andlor size has been obtained, lower servings of the
food
supplement may be administered to the athlete's diet in ordez to maintain the
increased muscle size andlor strength. These features will be discussed in
further
detail in the examples. Additionally in order to maximize the effects of the
food
supplement in enhancing muscle size andlor snength, it is preferred that the
food
supplement is administered to the diet of the athlete immediately following an
exercise period. On non-warlcout days, the food supplement may be administered
anytime during the day, although administering the food supplement ugon
awakening or otherwise during the morning hours is preferred.
The food supplement compositions and methods of the invention are further
illusarated in the following examples. In the examples and throughout the
present
specification, parts and percentages are by weight unless otherwise specif ed.
In this example, an athlete consumes two servings of the food supplement as
described herein daily, are in the morning and the other twelve hours later or
immediately after hislher exercise workout. This regime is continued for 8ve
days
in order to enhance muscle size andlor strength. Each serving of the food
supplemem is approximately 100 g and contains the follpwing;
9
CA 02246014 1998-08-21
Lipoic Acid 200 mg
Creatine Monohydrate 10 g
Dextrose 75 g
S Taurine 2000 mg
Vitamin C 250 mg
Magnesium 70 mg
Potassium 150 mg
Phosphorous 100 mg
Chromium Picolinate 300 mcg
Each approximate I00 gram serving is mixed with 12 ounces of cold water to
provide a liquid drink. An additional 8 ounces of water is consumed aftex the
food
supplement litncid drink is consumed.
The muscle size alullor strength enhancing regime of Example 1 is modified
so that the athlete consumes four servings of the food supplement daily, with
each
serving being approximately 50 g of the supplement and comprising:
Com ~nent,
Lipoic Acid 100 mg
Creative Monohydrate 5 g
Dextrose 37.5 g
Taurine 1000 mg
Vitamin C 125 mg
Magnesium 35 mg
Potassium 75 mg
Phosphorous 50 mg
Chromium Plcolinate 150 mcg
Each supplement serving is mixed with 12 ounces of cold water and the servings
are
administered at approximately evcnly spaced times through the day, with one
serving being consumed immediately after the athlete's exercise workout,
CA 02246014 1998-08-21
Once the regime described in Example 1 is completed, the athlefie cont~s
with a maintenance regime wherein one serving of the food supplement
composition
described in Example I is consumed on a daily basis. The serving is consumed
im~diately after an exercise workout or, on non-workout days, upon awakening
or
otherwise in the morning hours, As described i~t F.xampIe I, the approximate
I00
gram serving is mixed with cold water to form a liquid drink, Alternatively,
the
food supplement is be combined with other liquid drinks or foods as desired.
This
maintenance regime is co~inued for at least eight weeps to mairnain enhanced
muscle size andlor strength.
1 ~ The servings set forth in these examples are designed for a 2004 calorie
diet.
Daily values may be increased or decreased depending on the calorie needs of
individual athletes, andlor body weights of individual athletes.
The examples and embodiments set forth in the present application are
provided only to illustrate various aspects of the invention and additional,
embodiments and advantages of the food supplements and methods of the present
invention will be apgarent to those skilled in the art_
11
