WO2008037047A1

WO2008037047A1 - Composition and method for increasing lean muscle mass, decreasing muscle loss, increasing muscle strength and improving athletic performance

Info

Publication number: WO2008037047A1
Application number: PCT/CA2006/001566
Authority: WO
Inventors: Marvin Heuer; Shan Chaudhuri; Ken Clement
Original assignee: Aplodan Formulations Ltd.
Priority date: 2006-09-25
Filing date: 2006-09-25
Publication date: 2008-04-03

Abstract

A dietary supplement and method directed at increasing lean muscle mass, decreasing muscle loss, increasing muscle strength and improving athletic performance. The dietary supplement comprises at least Creatinol-O-Phosphate or derivatives thereof and Alpha Lipoic Acid or derivatives thereof.

Description

COMPOSITION AND METHOD FOR INCREASING LEAN MUSCLE MASS,

DECREASING MUSCLE LOSS, INCREASING MUSCLE STRENGTH AND

IMPROVING ATHLETIC PERFORMANCE

Field of the Invention 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.

Summary of the Invention

The foregoing needs and other needs and objectives that will become apparent for the following description are achieved in the present invention which comprises a dietary supplement and method for increasing lean muscle mass, increasing muscle strength and improving athletic performance A preferred embodiment of the present invention, a composition and method is provided for increasing muscle strength, increasing lean muscle mass, and improving athletic performance. According to an embodiment of the present invention there is provided 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.

Background of the Invention 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. 1995 Feb;95(2):811-9), particularly following exercise (Biolo G, Williams BD, Fleming RY, Wolfe RR. Insulin action on muscle protein kinetics and amino acid transport during recovery after resistance exercise. Diabetes. 1999 May;48(5):949- 57) which is required for increasing muscle mass and associated muscle function, i.e. strength. 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. 1997 Jul;273(l Pt 1):E185-91; Ziegler D, Hanefeld M, Ruhnau KJ, Hasche H, Lobisch M, Schutte K, Kerum G, Malessa R. Treatment of symptomatic diabetic polyneuropathy with the antioxidant alpha-lipoic acid: a 7-month multicenter randomized controlled trial (ALADIN III Study). ALADIN III Study Group. Alpha-Lipoic Acid in Diabetic Neuropathy. Diabetes Care. 1999 Aug;22(8): 1296-301). Likely due to this insulin-like activity, the combination of Alpha Lipoic Acid and Creatine, via supplementation has been shown to result in markedly improved uptake and retention of Creatine by skeletal muscle cells (Burke DG, Chilibeck PD, Parise G, Tarnopolsky MA, Candow DG. Effect of alpha-lipoic acid combined with creatine monohydrate on human skeletal muscle creatine and phosphagen concentration. Int J Sport Nutr Exerc Metab. 2003 Sep;13(3):294-302).

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). 1993 May;84(5):565-71) as well as increasing muscle growth (Volek JS, Duncan ND, Mazzetti SA, Staron RS, Putukian M, Gomez AL, Pearson DR, Fink WJ, Kraemer WJ. Performance and muscle fiber adaptations to creatine supplementation and heavy resistance training. Med Sci Sports Exerc. 1999 Aug;31(8): 1147-56).

Detailed Description of the Invention

In the following description, for the purposes of explanation, numerous specific details are set forth in order to provide a thorough understanding of the present invention. It will be apparent, however, to one of ordinary skill in the art that the present invention may be practiced without these specific details.

While not wishing to be bound by theory, it is understood by the inventors that the beneficial activity of supplemental Creatinol-O-Phosphate, ,is improved through the combination of at least Creatinol-O-Phosphate and Alpha Lipoic Acid in a single dietary supplement wherein an increase in the uptake and retention of Creatinol-O-Phosphate results from the insulin-like activity of Alpha Lipoic Acid.

The present invention, according to various embodiments thereof, 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. As a supplement, 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. Arzneimittelforschung. 1979, 29(9a): 1447-9). 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. Arzneimittelforschung. 1979;29(9a): 1483-5). Additionally, early investigators of the properties of 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. Arzneimittelforschung. 1984;34(9):968-72). Furthermore, an additional or alternative possible mechanism hypothesized in regard to 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. Arzneimittelforschung. 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. In one study, 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). Moreover, in another study conducted in elderly subjects, it was found that Creatinol-O- Phosphate improved muscular performance as compared to controls (Cavalieri U, Quadri A, Ghirardi F. Effects of creatinol o-phosphate on the muscle function of elderly people. The Therapeutic Clinic. 1974, 69: 215-223). 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. Arzneimittelforschung. 1979, 29(9a): 1447-9), the end metabolite and degradation product of creatine and phosphocreatine, which diffuses out of cells for later excretion by the kidneys. This metabolism to Creatinol-O-Phosphate may be due to phosphodiesterases contained within the body. 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. 1994, 266(5 Pt l):E725-30). In various embodiments of the present invention which are set forth in greater detail below in the examples below, 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

Alpha Lipoic Acid (ALA) 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. 1999 Feb;13(2):411-8) in rats supplemented with ALA, thereby indicating its protective effects in these parameters. As such, the antioxidant activity of ALA is likely involved in the prevention of cell death due to an improvement in oxidative stress (Arivazhagan P, Juliet P, Panneerselvam C. Effect of dl-alpha-lipoic acid on the status of lipid peroxidation and antioxidants in aged rats. Pharmacol Res. 2000 Mar;41(3):299-303). Furthermore, ALA has been linked to a beneficial increase in high-density lipoproteins (Wollin SD, Wang Y, Kubow S, Jones PJ. Effects of a medium chain triglyceride oil mixture and alpha-lipoic acid diet on body composition, antioxidant status, and plasma lipid levels in the Golden Syrian hamster. J Nutr Biochem. 2004 Jul;15(7):402-10) possibly due to its known effects as an antioxidant. Further to its insulin-like activity, 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. Effect of alpha-lipoic acid combined with creatine monohydrate on human skeletal muscle creatine and phosphagen concentration. Int J Sport Nutr Exerc Metab. 2003 Sep;13(3):294-302) thereby enhancing the effects of Creatinol-O-Phosphate or derivatives thereof through an increase in retention.

In an embodiment of the present invention, which is set forth in greater detail in the examples below, 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

Acid or derivatives thereof. The preferred dosage of a serving of the dietary supplement comprises about 0.010 g of Alpha Lipoic Acid or derivatives thereof.

In a preferred embodiment of the present invention, the dietary supplement comprises at least a combination of Creatinol-O-Phosphate or derivatives thereof and Alpha Lipoic Acid or derivatives thereof.

It is understood by the inventors that advantageously, the combination of ALA and Creatinol-O-Phosphate subsequent co-administration in the form of a dietary supplement will enhance the retention of Creatinol-O-Phosphate in the body.

According to various embodiments of the present invention, the dietary supplement may be consumed in any form. For instance, 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.

Furthermore, 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. Additionally, 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.

Preferably, the dietary supplement of the present invention is consumed by an individual in accordance with the following method: As a dietary supplement, 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.

Although the following example 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, supplied in caplet form, 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. Example 2

The ingredients of the dietary supplement, supplied in tablet form, 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. Example 3

The ingredients of the dietary supplement, supplied in caplet form, 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. Example 4

The ingredients of the dietary supplement, supplied in tablet form, 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. Example 5

The ingredients of the dietary supplement, supplied in tablet form, 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. Example 6

The ingredients of the dietary supplement, supplied in caplet form, 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. Extensions and Alternatives

In the foregoing specification, the invention has been described with specific embodiments thereof however, it will be evident that various modifications and changes may be made thereto without departing from the broader spirit and scope of the invention.

Claims

ClaimsWhat is claimed:

1. A dietary supplement comprising at least Creatinol-O-Phosphate or derivatives thereof and Alpha Lipoic Acid or derivatives thereof.

2. A method of increasing lean muscle mass in an individual comprising at least the step of consuming the composition of claim 1.

3. A method of increasing muscle strength in an individual comprising at least the step of consuming the composition of claim 1.

4. A method of improving athletic performance in an individual comprising at least the step of consuming the composition of claim 1.

5. A composition comprising: about 1.0 g of Creatinol-O-Phosphate or derivative thereof; about 0.01Og of Alpha Lipoic Acid or derivative thereof.

6. A method of increasing lean muscle mass in an individual comprising at least the step of consuming the composition of claim 5.

7. A method of increasing muscle strength in an individual comprising at least the step of consuming the composition of claim 5.

8. A method of improving athletic performance in an individual comprising at least the step of consuming the composition of claim 5.