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WO2008037047A1 - Composition et procédé pour l'accroissement de la masse musculaire maigre, la réduction de perte musculaire, l'accroissement de la force musculaire et l'amélioration de la performance athlétique - Google Patents

Composition et procédé pour l'accroissement de la masse musculaire maigre, la réduction de perte musculaire, l'accroissement de la force musculaire et l'amélioration de la performance athlétique Download PDF

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Publication number
WO2008037047A1
WO2008037047A1 PCT/CA2006/001566 CA2006001566W WO2008037047A1 WO 2008037047 A1 WO2008037047 A1 WO 2008037047A1 CA 2006001566 W CA2006001566 W CA 2006001566W WO 2008037047 A1 WO2008037047 A1 WO 2008037047A1
Authority
WO
WIPO (PCT)
Prior art keywords
muscle
increasing
phosphate
creatinol
composition
Prior art date
Application number
PCT/CA2006/001566
Other languages
English (en)
Inventor
Marvin Heuer
Shan Chaudhuri
Ken Clement
Original Assignee
Aplodan Formulations Ltd.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Aplodan Formulations Ltd. filed Critical Aplodan Formulations Ltd.
Priority to PCT/CA2006/001566 priority Critical patent/WO2008037047A1/fr
Publication of WO2008037047A1 publication Critical patent/WO2008037047A1/fr

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/66—Phosphorus compounds
    • A61K31/662—Phosphorus acids or esters thereof having P—C bonds, e.g. foscarnet, trichlorfon
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23L—FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
    • A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23L—FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
    • A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
    • A23L33/17—Amino acids, peptides or proteins
    • A23L33/175—Amino acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/385—Heterocyclic compounds having sulfur as a ring hetero atom having two or more sulfur atoms in the same ring
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
    • A23V2002/00—Food compositions, function of food ingredients or processes for food or foodstuffs

Definitions

  • the present invention relates to the composition of a dietary supplement directed towards increasing lean muscle mass, and improving athletic performance. Through oral administration of the composition, a method for producing the same is also provided.
  • a composition and method for increasing muscle strength, increasing lean muscle mass, and improving athletic performance.
  • a composition and method comprising at least a combination of Creatinol-O-Phosphate and Alpha Lipoic Acid directed towards increasing muscle strength, increasing lean muscle mass, and improving athletic performance.
  • Insulin is involved in the carbohydrate-induced uptake of glucose by cells. The release of glucose from cells is also concomitantly inhibited by insulin and its storage as glycogen and triglycerides is promoted (Khan AH, Pessin JE. Insulin regulation of glucose uptake: a complex interplay of intracellular signalling pathways. Diabetologia. 2002 Nov;45(l l): 1475-83). Additionally, insulin has also been shown to stimulate the uptake of amino acids by muscle cells and stimulate protein synthesis (Biolo G, Declan Fleming RY, Wolfe RR. Physiologic hyperinsulinemia stimulates protein synthesis and enhances transport of selected amino acids in human skeletal muscle. J Clin Invest.
  • Alpha Lipoic Acid has been shown to have insulin-like activity in terms of glucose metabolism (Streeper RS, Henriksen EJ, Jacob S, Hokama JY, Fogt DL, Tritschler HJ. Differential effects of lipoic acid stereoisomers on glucose metabolism in insulin-resistant skeletal muscle. Am J Physiol.
  • Creatine use has been thoroughly studied and it is well-establish as a beneficial dietary supplement for replenishing energy stores in working muscle cells (Greenhaff PL, Bodin K, Soderlund K, Hultman E. Effect of oral creatine supplementation on skeletal muscle phosphocreatine resynthesis. Am J Physiol. 1994 May;266(5 Pt l):E725-30), thereby increasing strength, reducing fatigue resulting from high-intensity exercise (Greenhaff PL, Casey A, Short AH, Harris R, Soderlund K, Hultman E. Influence of oral creatine supplementation of muscle torque during repeated bouts of maximal voluntary exercise in man. Clin Sci (Lond).
  • the present invention is directed to increasing muscle strength, increasing lean muscle mass, and improving athletic performance.
  • the present invention comprises at least Creatinol-O-Phosphate or derivatives thereof and Alpha Lipoic Acid or derivatives thereof. Creatinol O-Phosphate
  • Creatinol O-Phosphate also known by the synonyms, (N-methyl-N-(beta-hydroxyethyl) guanidine O-phosphate, COP, and (CAS: 6903-79-3), is a phosphoric ester derivative of creatine.
  • Creatinol O-Phosphate has been shown to be well tolerated and without side effects (Melloni GF, Minoja GM, Lureti GF, Merlo L, Pamparana F, Brusoni B. Acute clinical tolerance of creatinol O-phosphate. Arzneiffenbachforschung. 1979, 29(9a): 1447-9).
  • Creatinol-O-Phosphate Early studies of Creatinol-O-Phosphate explored its use as a treatment for heart lesions and also its ability to restore reduced cardiac contractile function. As a result of these early studies, Creatinol-O- Phosphate has been successfully used to improve cardiac parameters in patients with inadequate coronary blood flow (Barlattani M, Guglielmi G, Mammarella A. Creatinol O-phosphate therapy in patients with inadequate coronary circulation. Double-blind clinical trial. Arzneistoffforschung. 1979;29(9a): 1483-5).
  • Creatinol-O-Phosphate hypothesized that the cardioprotective effect of Creatinol-O-Phosphate was due to action on anaerobic glycolysis (Godfraind T, Saleh MM. Action of creatinol-O- phosphate on the contractility changes evoked by hypoxia and ischemia in rat isolated heart. Arzneistoffforschung. 1984;34(9):968-72).
  • Creatinol-O-Phosphate is an effect in the electrophysiological properties of the cell membrane as shown by other investigators (Botti G, Bonatti V. Preliminary report on electrophysiological effectiveness of creatinol O-phosphate (COP) in human subjects. Arzneistoffaria. 1979;29(9a): 1491 -4).
  • Creatinol-O-Phosphate in addition to its cardio-protective effects, has been has also been shown to improve muscle development and increase the capacity of a muscle to perform physical activity.
  • hand-grip strength was improved by Creatinol-O-Phosphate administration and while remaining unaffected in a placebo group (Nicaise J. Creatinol O-phosphate (COP) and muscular performance: a controlled clinical trial. Curr Ther Res Clin Exp. 1975, 17(6):531-4).
  • Creatinol-O- Phosphate improved muscular performance as compared to controls (Cavalieri U, Quadri A, Ghirardi F.
  • Creatinol-O-Phosphate functions in a similar to that of Creatine, which is well known is in art, in addition to possibly possessing unique properties. Creatinol-O-Phosphate administration has been found to increase urine levels of creatinine (Melloni GF, Minoja GM, Lureti GF, Merlo L, Pamparana F, Brusoni B. Acute clinical tolerance of creatinol O-phosphate. Arzneiffenbachaba.
  • Creatinol-O-Phosphate may therefore enhance athletic performance and muscle growth in a manner similar to that of creatine, aiding in the rapid rephosphorylation of ATP to provide energy to a given muscle (Greenhaff PL, Bodin K, Soderlund K, Hultman E. Effect of oral creatine supplementation on skeletal muscle phosphocreatine resynthesis. Am J Physiol.
  • a dietary supplement includes Creatinol-O-Phosphate or derivatives thereof.
  • a serving of the dietary supplement may include from about 0.250 g to about 5.0 g of Creatinol-O-Phosphate or derivatives thereof.
  • the preferred dosage, in a serving of said dietary supplement comprises about 1.0 g of Creatinol-O-Phosphate or derivatives thereof.
  • Alpha Lipoic Acid is an enzyme found in the cellular energy-producing structures, the mitochondria. Moreover, ALA works in synergy with vitamins C and E as an antioxidant in both the water- and fat- soluble environments. Negative age-related changes in mitochondrial function, accumulated oxidative damage and metabolic rate were all improved (Hagen TM, Ingersoll RT, Lykkesfeldt J, Liu J, Wehr CM, Vinarsky V, Bartholomew JC, Ames AB. (R)-alpha-lipoic acid-supplemented old rats have improved mitochondrial function, decreased oxidative damage, and increased metabolic rate. FASEB J.
  • Alpha Lipoic Acid may enhance the uptake and retention of supplemental Creatinol-O-Phosphate or derivatives thereof in a manner similar to that of the enhanced Creatine retention induced by Alpha Lipoic Acid with respect muscle cells (Burke DG, chilibeck PD, Parise G, Tarnopolsky MA, Candow DG.
  • a dietary supplement may include Alpha Lipoic Acid or derivatives thereof.
  • a serving of the dietary supplement may include from about 0.005 g to about 0.1 g of Alpha Lipoic
  • the preferred dosage of a serving of the dietary supplement comprises about 0.010 g of Alpha Lipoic Acid or derivatives thereof.
  • the dietary supplement comprises at least a combination of Creatinol-O-Phosphate or derivatives thereof and Alpha Lipoic Acid or derivatives thereof.
  • the dietary supplement may be consumed in any form.
  • the dosage form of the diet supplement may be provided as, e.g., a powder beverage mix, a liquid beverage, a ready-to-eat bar or drink product, a capsule, a liquid capsule, a tablet, a caplet, or as a dietary gel.
  • the preferred dosage form of the present invention is as a caplet or tablet.
  • the dosage form of said dietary supplement may be provided in accordance with customary processing techniques for dietary supplements in any of the forms mentioned above.
  • the dietary supplement set forth in the example embodiments herein may contain any appropriate number and type of excipients, as is well-known in the art.
  • the present dietary supplement or those similarly envisioned by one of ordinary skill in the art may be utilized in compositions and methods for increasing lean muscle mass,, increasing muscle strength and improving athletic performance.
  • the dietary supplement of the present invention is consumed by an individual in accordance with the following method:
  • a serving of said dietary supplement may be administered by means of consumption in conjunction with a liquid medium at least one (1) time daily wherein each serving is comprised of at least one (1) caplet or tablet.
  • Said dietary supplement may be consumed immediately post-workout, pre-workout, or in the morning upon waking on non-workout days. In this manner, the dietary supplement may increase lean muscle mass, increase muscle strength and improve athletic performance.
  • Example 1 illustrates the practice of the present invention in one of its embodiments, the example should not construed as limiting the scope of the invention. Other embodiments will be apparent to one of ordinary skill in the art from consideration of the specifications and example. Examples Example 1
  • the ingredients of the dietary supplement may be consumed with 8 ounces of water.
  • the composition of the dietary supplement includes Creatinol-O- Phosphate (1.0 g) and Alpha Lipoic Acid (0.010 g).
  • the dietary supplement may be consumed at least one (1) time daily wherein said serving isconsumed immediately following exercise.
  • the ingredients of the dietary supplement may be consumed with 8 ounces of water.
  • the composition of the dietary supplement includes Creatinol-O- Phosphate (1.0 g) and Alpha Lipoic Acid (0.010 g).
  • the dietary supplement may be consumed at least one (1) time daily wherein said serving is consumed immediately following exercise.
  • the ingredients of the dietary supplement may be consumed with 8 ounces of water.
  • the composition of the dietary supplement includes Creatinol-O- Phosphate (1.0 g) and Alpha Lipoic Acid (0.010 g).
  • the dietary supplement may be at least one (1) time daily wherein said serving is consumed prior to exercise.
  • the ingredients of the dietary supplement may be consumed with 8 ounces of water.
  • the composition of the dietary supplement includes Creatinol-O- Phosphate (1.0 g) and Alpha Lipoic Acid (0.010 g).
  • the dietary supplement may be at least one (1) time daily wherein said serving is consumed prior to exercise.
  • the ingredients of the dietary supplement may be consumed with 8 ounces of water.
  • the composition of the dietary supplement includes Creatinol-O- Phosphate (1 g) and Alpha Lipoic Acid (0.010 g).
  • the dietary supplement may be consumed at least one (1) time daily wherein said serving is consumed upon waking in the morning.
  • the ingredients of the dietary supplement may be consumed with 8 ounces of water.
  • the composition of the dietary supplement includes Creatinol-O- Phosphate (1.0 g) and Alpha Lipoic Acid (0.010 g).
  • the dietary supplement may be consumed at least one (1) time daily wherein said serving is consumed upon waking in the morning.

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Polymers & Plastics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Mycology (AREA)
  • Engineering & Computer Science (AREA)
  • Food Science & Technology (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nutrition Science (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

La présente invention concerne un supplément diététique et un procédé destinés à l'accroissement de la masse musculaire maigre, la réduction de perte musculaire, l'accroissement de la force musculaire et l'amélioration de la performance athlétique. Le supplément diététique comporte au moins du créatinol-O-phosphate ou ses dérivés et de l'acide alpha-lipoïque ou ses dérivés.
PCT/CA2006/001566 2006-09-25 2006-09-25 Composition et procédé pour l'accroissement de la masse musculaire maigre, la réduction de perte musculaire, l'accroissement de la force musculaire et l'amélioration de la performance athlétique WO2008037047A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
PCT/CA2006/001566 WO2008037047A1 (fr) 2006-09-25 2006-09-25 Composition et procédé pour l'accroissement de la masse musculaire maigre, la réduction de perte musculaire, l'accroissement de la force musculaire et l'amélioration de la performance athlétique

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/CA2006/001566 WO2008037047A1 (fr) 2006-09-25 2006-09-25 Composition et procédé pour l'accroissement de la masse musculaire maigre, la réduction de perte musculaire, l'accroissement de la force musculaire et l'amélioration de la performance athlétique

Publications (1)

Publication Number Publication Date
WO2008037047A1 true WO2008037047A1 (fr) 2008-04-03

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Family Applications (1)

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PCT/CA2006/001566 WO2008037047A1 (fr) 2006-09-25 2006-09-25 Composition et procédé pour l'accroissement de la masse musculaire maigre, la réduction de perte musculaire, l'accroissement de la force musculaire et l'amélioration de la performance athlétique

Country Status (1)

Country Link
WO (1) WO2008037047A1 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2276494A4 (fr) * 2008-04-09 2011-10-19 John H Owoc Compositions aqueuses stables comprenant des espèces bioactives de créatine

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6136339A (en) * 1998-08-21 2000-10-24 Gardiner; Paul T. Food supplements and methods comprising lipoic acid and creatine
US20050192183A1 (en) * 2004-03-01 2005-09-01 Thomas Gastner Use of guanidine compounds as physiological strengthening agents in the form of nutritional supplements, animal feed additives, in cosmetic preparations and as plant stimulants
WO2006034586A1 (fr) * 2004-09-29 2006-04-06 Aplodan Formulations Ltd. Composition nutritive favorisant la performance musculaire et agissant comme bloqueur d'hydrogene (h+)

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6136339A (en) * 1998-08-21 2000-10-24 Gardiner; Paul T. Food supplements and methods comprising lipoic acid and creatine
US20050192183A1 (en) * 2004-03-01 2005-09-01 Thomas Gastner Use of guanidine compounds as physiological strengthening agents in the form of nutritional supplements, animal feed additives, in cosmetic preparations and as plant stimulants
WO2006034586A1 (fr) * 2004-09-29 2006-04-06 Aplodan Formulations Ltd. Composition nutritive favorisant la performance musculaire et agissant comme bloqueur d'hydrogene (h+)

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
2 March 2007 (2007-03-02), Retrieved from the Internet <URL:http://www.muscletech.com/PRODUCTS/APLODAN/index.shtml> *

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2276494A4 (fr) * 2008-04-09 2011-10-19 John H Owoc Compositions aqueuses stables comprenant des espèces bioactives de créatine
US8372821B2 (en) * 2008-04-09 2013-02-12 Jack H. Owoc Stable aqueous compositions comprising bioactive creatine species
US9114150B2 (en) 2008-04-09 2015-08-25 Jho Intellectual Property Holdings, Llc Stable aqueous compositions comprising bioactive creatine species

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