Source: https://www.lens.org/lens/patent/166-772-551-323-755/fulltext
Timestamp: 2019-05-25 07:40:08
Document Index: 171377452

Matched Legal Cases: ['application No. 12', 'Application No. 95', 'Application No. 95', 'Application No. 95', 'Application No. 95', 'Application No. 95', 'Application No. 95', 'Application No. 95', 'Application No. 95', 'Application No. 95', 'Application No. 95', '§371', '§119', 'Application No. 60']

US 8394402 B2 - Compositions And Methods For The Sustained Release Of Beta-alanine - The Lens - Free & Open Patent and Scholarly Search
US 8394402 B2
166-772-551-323-755
*US08394402B2*
US008394402B2
(12) United States Patent (10) Patent No.: US 8,394,402 B2
et al. (45) Date of Patent: Mar. 12, 2013
(21) Appl. No.: 13/646,184
(22) Filed: Oct. 5, 2012
US 2013/0030052 A1 Jan. 31, 2013
Division of application No. 12/064,005, now Pat. No. 8,329,207 .
(51) Int. Cl. A61K 047/00 (20060101); A61K 031/195 (20060101)
(52) U.S. Cl. 424/439; 514/561
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WO WO-9/3/04690 A1 3/1993
WO WO-9/8/06278 A1 2/1998
WO WO-2/007/073398 A3 9/2007
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Primary Examiner —Robert A Wax
Assistant Examiner —Jessica Worsham
[0001] This application is a divisional of U.S. application Ser. No. 12/064,005, filed Apr. 30, 2009, which is a National Stage application under 35 U.S.C. §371, which claims benefit under 35 U.S.C. §119(a) of International Application No. PCT/US2006/020104, filed May 23, 2006, which claims benefit of U.S. Provisional Patent Application No. 60/683,985, filed May 23, 2005, all of which are herein incorporated by reference.
[0004] In addition, in the sporting and athletic community, natural food supplements which specifically improve athletic ability are increasingly important, such as supplements that promote or enhance physical prowess for leisure or employment purposes. In another example, anaerobic (e.g., lactate producing) stress can cause the onset of fatigue and discomfort that can be experienced with aging. Anaerobic stress can also result from prolonged sub-maximal isometric exercise when the local circulation is partially or totally occluded by the increase in intra-muscular pressure (e.g., during rock climbing) or from exercise involving prolonged breath holding (e.g., free diving, or synchronized swimming) Excessive lactate production can result in the acidification of the intracellular environment.
[0011] The pharmaceutical composition can include about 0.1-200.0; about 1.0-9.0; about 2.0-8.0; about 3.0-7.0; or about 4.0-6.0 grams (g) of free beta-alanine or the equivalent amount of a biological source thereof. The pharmaceutical composition can be formulated for humans and can include about 0.1-200.0; about 1.0-9.0; about 2.0-8.0; about 3.0-7.0; or about 4.0-6.0 g of free beta-alanine or the equivalent amount of a a biological source thereof.
[0046] The concentrations of free beta-alanine or a biological source thereof in the compositions disclosed herein are effective for increasing the anaerobic working capacity of a tissue by providing an amount of free beta-alanine to blood or blood plasma effective to increase the synthesis of beta-alanylhistidine peptides, particularly carnosine, in muscle and other tissues. A sustained release formulation of beta-alanine is administered in an amount effective to attenuate the metabolic acidosis encountered during high-intensity exercise and thus delay the onset of fatigue during anaerobic exercise without inducing symptoms of parasthesia.
[0059] In addition, coating agents may be used to create or enhance the sustained release features of a pharmaceutical composition. For example, plasticizers that are useful as coating agents include, but are not limited to, citric and tartaric acid esters (acetyl-triethyl citrate, acetyl tributyl-, tributyl-, triethyl-citrate); glycerol and glycerol esters (glyceroldiacetate, -triacetate, acetylated monoglycerides, castor oil); phthalic acid esters (dibutyl-, diamyl-, diethyl-, dimethyl-, dipropyl-phthalate), di-(2-methoxy- or 2-ethoxyethyl)-phthalate, ethylphthalyl glycolate, butylphthalylethyl glycolate and butylglycolate; alcohols (propylene glycol, polyethylene glycol of various chain lengths); adipates (diethyladipate, di (2-methoxy- or 2-ethoxyethyl)-adipate; benzophenone; diethyl- and diburylsebacate; dibutylsuccinate; dibutyltartrate; diethylene glycol dipropionate; ethyleneglycol diacetate, -dibutyrate, -dipropionate; tributyl phosphate, tributyrin; polyethylene glycol sorbitan monooleate; polysorbates such as Polysorbar 50; and sorbitan monooleate.
[0072] In another embodiment, dietary supplements containing free-beta alanine or a biological source of beta-alanine are food products wherein the free beta-alanine or a biological source of beta-alanine is suspended in an edible supporting matrix to form an edible suspension. The term “suspension” is intended to mean compositions containing free beta-alanine or a biological source of beta-alanine as provided herein, comprise flee beta-alanine in solid form (e.g. as crystals, power or the like), distributed within an edible viscous liquid or semi-liquid, or a solid, supporting matrix, typically such that settling (under the influence of gravity) of the solid beta-alanine is inhibited or prevented.
[0077] Other ingredients that can be included in the presently disclosed sustained release beta-alanine compositions can include, for example, anti-oxidants, alpha-lipoic acid, tocotrienols, N-acetylcysteine, co-enzyme Q-10, extracts of rosemary such as camosol, botanical anti-oxidants such as green tea polyphenols, grape seed extract, COX-1 type inhibitors such as resveratrol, ginkgo biloba, and garlic extracts. Other amino acids such as L-cysteine or L-citrulline may be added. Combination with an acetylcholine precursor such as choline chloride or phosphatidylcholine may be desirable, for example, to enhance vasodilation. It is to be understood that such combination therapy constitutes a further aspect of the compositions and methods of treatment provided herein.
RIA-1743
RIA-1744
1. A method for increasing accumulation of beta-alanylhistidine peptide in muscle tissue to delay onset of muscle fatigue in a subject while decreasing the effects of paraesthesia, the method comprising the step of:
administering free beta-alanine, an ester or a salt thereof, to the subject over time in an amount effective to cause accumulation of beta-alanylhistidine peptide in the muscle tissue of the subject,
wherein the free beta-alanine, the ester or the salt thereof, is in a sustained release formulation that decreases the effects of paraesthesia in the subject,
wherein the free beta-alanine, ester or salt thereof, in the sustained release formulation is provided in an amount ranging from about 0.1 to about 10.0 grams, and
wherein the sustained release formulation is provided in a daily dose effective to increase levels of beta-alanine in the subject's blood or blood plasma.
2. The method of claim 1, wherein the free beta-alanine, ester or salt thereof, in the sustained release formulation is provided in an amount ranging from about 1.0 to about 10.0 grams.
3. The method of claim 1, wherein the free beta-alanine, ester or salt thereof, in the sustained release formulation is provided in an amount ranging from about 1.0 to about 9.0 grams.
4. The method of claim 1, wherein the free beta-alanine, ester or salt thereof, in the sustained release formulation is provided in an amount ranging from about 2.0 to about 8.0 grams.
5. The method of claim 1, wherein the free beta-alanine, ester or salt thereof, in the sustained release formulation is provided in an amount ranging from about 3.0 to about 7.0 grams.
6. The method of claim 1, wherein the free beta-alanine, ester or salt thereof, in the sustained release formulation is provided in an amount ranging from about 4.0 to about 6.0 grams.
7. The method of claim 1, wherein the sustained release formulation is in a solid, liquid or semi-liquid.
8. The method of claim 1, wherein the sustained release formulation is part of a drink, energy bar, edible suspension or food stuff.
9. The method of claim 7, wherein components in the sustained release formulation retard absorption of beta-alanine into the body.
10. The method of claim 7, wherein part of the free beta-alanine is found in an emulsion.