EP1187600A1 - Procede destine a augmenter une concentration stable de creatine cellulaire - Google Patents

Procede destine a augmenter une concentration stable de creatine cellulaire

Info

Publication number
EP1187600A1
EP1187600A1 EP99933496A EP99933496A EP1187600A1 EP 1187600 A1 EP1187600 A1 EP 1187600A1 EP 99933496 A EP99933496 A EP 99933496A EP 99933496 A EP99933496 A EP 99933496A EP 1187600 A1 EP1187600 A1 EP 1187600A1
Authority
EP
European Patent Office
Prior art keywords
creatine
combination
effervescent
tablet
amount
Prior art date
Legal status (The legal status 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 status listed.)
Withdrawn
Application number
EP99933496A
Other languages
German (de)
English (en)
Inventor
Joseph W. Carnazzo
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Fortress Systems LLC
Original Assignee
Fortress Systems LLC
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 Fortress Systems LLC filed Critical Fortress Systems LLC
Priority claimed from PCT/US1999/012597 external-priority patent/WO2000074647A1/fr
Publication of EP1187600A1 publication Critical patent/EP1187600A1/fr
Withdrawn legal-status Critical Current

Links

Definitions

  • TITLE METHOD FOR ENHANCING STABLE
  • Creatine oral supplementation has been used in the prior art to increase creatine and creatine phosphate (also called phosphocreatine) stores, which are needed for high energy phosphorus metabolism. Creatine, along with dietary carbohydrates, fats, proteins, and other compounds, is a central component of the metabolic system, and is involved in the provision of energy for work and exercise performance. Phosphocreatine helps provide Adenosine TriPhosphate (ATP) during short bursts of high intensity exercise, and it has been found that the depletion of phosphocreatine has been associated with the onset of fatigue. It has been recently discovered that the phosphocreatine pool in skeletal muscle is expandable. This has led to the oral supplementation of creatine and phosphocreatine to increase the levels of these components in muscle, to thereby enhance exercise performance during intermittent activities which require strength and power.
  • ATP Adenosine TriPhosphate
  • Creatine is synthesized from amino acids in the liver, pancreas and kidney, by the transfer of the guanidine moiety of arginine to glycine, which is then methylated to form creatine. Creatine, which is synthesized in the liver, pancreas and kidney, is released into the bloodstream and actively taken up by the muscle cells, using the Na+ gradient. Oral creatine is absorbed, unchanged, from the intestinal lumen and passes directly into the bloodstream. The cellular creatine concentration is determined by specific transporters, which transport creatine into the cell against its concentration gradient.
  • the creatine transport protein has an increased affinity for creatine and concentrates creatine within the cell. Once inside the cell, very little creatine is lost (approximately 2 grams per day in a 70 kg male). Based upon this information, it follows that small increases of plasma creatine (which can occur with creatine supplementation) result in increased transport activity.
  • the loss of creatine from skeletal muscle is typically about 3% per day, which closely matches the amount of creatinine produced non-enzymatically by living human muscle.
  • the main mechanism by which creatine is lost is the conversion of creatine to creatinine, which is an irreversible non-enzymatic process.
  • creatine lost from a cell is considered to be negligible, and the concentration of creatine in the cell is not at risk of depletion by virtue of exercise.
  • the main advantage of creatine administration is in the fact that cellular creatine concentration is stable and not prone to being lost.
  • creatine monohydrate The most commonly used creatine supplement for oral consumption is creatine monohydrate. Creatine monohydrate supplementation at a dosage of 20 grams per day for a 5 day period has been the standard used during most studies in humans. Conventionally, creatine monohydrate is dissolved in approximately 300 milliliters of warm to hot water, the increased water temperature thereby increasing the solubility of creatine monohydrate. It has been found that creatine is not decomposed in the alimentary tract after oral administration, since there is no appreciable increase in urinary urea or ammonia. The results obtained for the conversion of retained creatine to creatinine have led researchers to believe that creatine is completely absorbed from the alimentary tract, then carried to the tissues, and thence either stored in the tissues or immediately rejected and eliminated by way of the kidneys.
  • Still another object is to provide a creatine oral supplement which is highly soluble, absorbable, and provides consistent, uniform, and accurate delivery of the creatine to the human cells.
  • the method for enhancing a stable concentration of cellular creatine in a human includes dissolving an effervescent containing an acidic edible salt form of creatine in water. Once the tablet has completely dissolved, the solution is ingested, and an effective amount of creatine is absorbed.
  • the effervescent is in tablet form and contains creatine in the form of an edible salt, a mixture of acids and sodium bicarbonate, which release carbon dioxide when dissolved in the water.
  • creatine may be uniformly and accurately dispensed when completely dissolved in liquid. More specifically, the creatine has been created in the form of an effervescent in tablet or granular powder form which reduces the pH of water to thereby increase the solubility of the creatine in the liquid.
  • Creatine monohydrate as used in the prior art, has a neutral pH which does not readily dissolve in water or other neutral pH liquids.
  • the increase in solubility gives a much more uniform absorption of the creatine after ingestion.
  • an effervescent tablet, or packet of premeasured effervescent powder assures complete and uniform dispersal of the creatine in the water, by virtue of the lowering of the pH of the liquid, and the effervescence of the liquid.
  • the soluble effervescent will contain mixtures of acids (including but not limited to citric acid and/or tartaric acid) and sodium bicarbonate, which releases carbon dioxide when dissolved in water.
  • the chemical formula of creatine is C4 H9 N3 02, and has a molecular weight 131.13.
  • Prior art powder forms of creatine utilize creatine monohydrate in water, having a chemical formula of C4 H9 N3 02 H20.
  • Creatine monohydrate becomes anhydrous at 100°F, and has a neutral reaction to litmus.
  • One gram of creatine monohydrate dissolves in 75 ml of water, about 9 liters of alcohol, and is insoluble in ether.
  • creatinine is formed. While aqueous and alkaline solutions contain an equilibrium mixture of creatine and creatinine, it has been found that in an acid solution, the formation of creatinine is complete.
  • the method of the present invention relies upon the combination of creatine within an effervescent to create an acid solution which is ingested by the consumer.
  • the effervescent lowers the pH to form an acid solution, whereby the creatine will completely and uniformly dissolve.
  • the invention includes a soluble effervescent containing creatine, an acid, or mixture of acids, and a bicarbonate for releasing carbon dioxide when dissolved in a neutral pH liquid, such as water.
  • creatine citrate is utilized, while other acidic edible salt forms of creatine may be utilized, including creatine phosphate (C4 H10 N3 05P, which may include either a sodium salt or a calcium salt) or creatine monohydrate.
  • the effervescent ingredients preferably utilize a mixture of acids, including citric acid and/or tartaric acid. Either sodium bicarbonate or potassium bicarbonate may be utilized for the release of carbon dioxide.
  • Either sodium bicarbonate or potassium bicarbonate may be utilized for the release of carbon dioxide.
  • starch cellulose, alginic acid or other disintegrating agents
  • stearic acid or other lubricants for tablet compression
  • flavoring agents either natural or synthetic
  • the effervescent is preferably in the form of a tablet, it may also be utilized in granular/powder form.
  • the effervescent must be stored in a tightly closed container or other moisture-proof package, since water or other liquids will activate the effervescent. This is beneficial, because it permits a predetermined, premeasured amount of creatine and effervescent to be meted out within a package. In this way, the consumer will always receive the exact dosage of creatine desired, whether in tablet form or granular/powder form.
  • creatine which has been found to accomplish the objectives of the present invention is manufactured in a 2.59 tablet with creatine citrate, with the following composition: sodium carbonate 50.0 mg sodium bicarbonate 1000.0 mg citric acid 1200.0 mg dextrose 1200.0 mg creatine citrate 2500.0 mg sodium laurel sulfate 5.0 mg stevia (herbal sweetener) 25.0 mg magnesium stearate 10.0 mg natural orange flavor 125.0 mg
  • the amounts of bicarbonate and carbonate may vary by as much as
  • the initial step in the method of the invention is to open a moisture-proof package containing the effervescent creatine and dispense it into a glass of water or other pH neutral liquid. Once the effervescent creatine has completely dissolved, the solution should be swallowed immediately. As noted above, an acidic aqueous solution will eventually cause the creatine to completely convert to creatinine. While this conversion typically takes a number of hours, the longer the consumer waits to ingest the solution, the smaller the amount of beneficial creatine (and the greater the amount of undesirable creatinine) that will be present in the solution.
  • the solution is ingested within 15 minutes of being completely dissolved in the liquid.

Landscapes

  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

L'invention concerne un procédé destiné à augmenter une concentration stable de créatine cellulaire chez un être humain. Ce procédé consiste à dissoudre un corps effervescent dans l'eau, ledit corps contenant une forme de sel comestible acide de créatine. Une fois ce corps effervescent entièrement dissous, on ingère immédiatement la solution, d'où l'absorption d'une quantité efficace de créatine. Le corps effervescent se présente de préférence sous forme d'un comprimé contenant de la créatine sous la forme d'un sel comestible, d'un mélange d'acides et de sodium.
EP99933496A 1999-06-07 1999-06-07 Procede destine a augmenter une concentration stable de creatine cellulaire Withdrawn EP1187600A1 (fr)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/US1999/012597 WO2000074647A1 (fr) 1997-03-31 1999-06-07 Procede destine a augmenter une concentration stable de creatine cellulaire

Publications (1)

Publication Number Publication Date
EP1187600A1 true EP1187600A1 (fr) 2002-03-20

Family

ID=22272903

Family Applications (1)

Application Number Title Priority Date Filing Date
EP99933496A Withdrawn EP1187600A1 (fr) 1999-06-07 1999-06-07 Procede destine a augmenter une concentration stable de creatine cellulaire

Country Status (3)

Country Link
EP (1) EP1187600A1 (fr)
JP (1) JP2003501374A (fr)
AU (1) AU4954199A (fr)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW200538738A (en) 2004-02-20 2005-12-01 Univ California Molecular flux rates through critical pathways measured by stable isotope labeling in vivo, as biomarkers of drug action and disease activity
JP2014526685A (ja) 2011-09-08 2014-10-06 ザ・リージェンツ・オブ・ザ・ユニバーシティ・オブ・カリフォルニア 代謝流量測定、画像化、および顕微鏡法
ES2668678T3 (es) * 2011-12-07 2018-05-21 Glaxosmithkline Llc Procedimiento de determinación de la masa muscular esquelética corporal total

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE19537494C2 (de) * 1995-09-25 1997-10-02 Desitin Arzneimittel Gmbh Kreatin zum Schutz von neuralem Gewebe

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See references of WO0074647A1 *

Also Published As

Publication number Publication date
AU4954199A (en) 2000-12-28
JP2003501374A (ja) 2003-01-14

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