Methods of improving tolerability, pharmacodynamics, and efficacy of beta-alanine and use therefor
The present invention relates in some aspects to compositions (e.g., pharmaceutical, nutritional compositions, etc.), formulations, and food or beverage products comprising, consisting essentially of, or consisting of (a) β-alanine or a derivative of β-alanine, and (b) at least one agent that inhibits the N-methyl D-aspartate (NMDA) pathway or a pathway which converges downstream with the NMDA pathway. The compositions, formulations, and food or beverage products are useful for enhancing physical performance, reducing β-alanine-induced paraesthesia, and improving tolerance and compliance to higher doses of β-alanine, thereby reducing the length of time it takes to achieve peak effect of β-alanine, and increasing the magnitude of peak effect on physical performance in a human or animal.
1 . A composition comprising (a) an effective amount of β-alanine or a derivative of β-alanine; and (b) an amount of at least one agent that modulates the N-methyl D-aspartate (NMDA) pathway,
wherein the amount of (b) is effective to reduce intolerable paraesthesia caused by (a) to a tolerable level,
wherein the at least one agent that modulates the NMDA pathway is selected from the group of agents consisting of L-glycine, botanical rhizome preparations or extracts selected from the group consisting of Acorus gramineus, Polygala tenuifolia, Celastrus paniculatus , and, Zizyphus jujuba var. spinosa , and combinations thereof, or wherein the at least one agent that modulates the NMDA pathway is an NMDA receptor antagonist selected from the group consisting of dextromethorphan, kynurenic acid, histogranin, memantine, meperidine, methadone, phencyclidine, and combinations thereof, and
wherein the composition is a solid and comprises 4 to 88% w/w of (a) and from 0.0005 to 45% w/w of (b) or is a liquid and comprises from 5 to 90% w/v of (a) and from 0.005 to 60% w/v of (b), and
wherein the derivative of beta alanine is selected from the group consisting of N-acetyl-β-alanine, fluorinated methyl β-alanine, 3-amino-3-fluoromethylpropionic acid, a β-alanine ester, a β-alanine amide, a β-alanine salt, and β-alanine nitrate.
2 . The composition of claim 1 , wherein the composition is a solid and comprises 4 to 88% w/w of (a) and from 0.0005 to 45% w/w of (b).
3 . The composition of claim 1 , wherein the composition is a liquid and comprises from 5 to 90% w/v of (a) and from 0.005 to 60% w/v of (b).
4 . The composition of claim 1 , further comprising a pharmaceutically acceptable carrier, diluent, or excipient.
5 . The composition of claim 1 , wherein the composition is a powder.
6 . The composition of claim 1 , wherein (a) comprises an effective amount of β-alanine.
7 . A composition comprising (a) an effective amount of β-alanine or a derivative of β-alanine; and (b) an amount of at least one agent that modulates the N-methyl D-aspartate (NMDA) pathway,
wherein the amount of (b) is effective to reduce intolerable paraesthesia caused by (a) to a tolerable level,
wherein the at least one agent that modulates the NMDA pathway comprises L-theanine and Zizyphus jujuba var. spinosa botanical rhizome extract or preparation,
wherein the composition is a solid and comprises 4 to 88% w/w of (a) and from 0.0005 to 45% w/w of (b) or is a liquid and comprises from 5 to 90% w/v of (a) and from 0.005 to 60% w/v of (b), and
wherein the derivative of beta alanine is selected from the group consisting of N-acetyl-β-alanine, fluorinated methyl β-alanine, 3-amino-3-fluoromethylpropionic acid, a β-alanine ester, a β-alanine amide, a β-alanine salt, and β-alanine nitrate.
8 . The composition of claim 7 , wherein (a) comprises an effective amount of β-alanine.
9 . A composition comprising (a) an effective amount of β-alanine or a derivative of β-alanine; and (b) an amount of at least one agent that modulates the N-methyl D-aspartate (NMDA) pathway,
wherein the amount of (b) is effective to reduce intolerable paraesthesia caused by (a) to a tolerable level,
wherein the at least one agent that modulates the NMDA pathway comprises L-theanine, Celastrus paniculatus botanical rhizome preparation or extract, and Zizyphus jujuba var. spinosa botanical rhizome preparation or extract, wherein the composition is a solid and comprises 4 to 88% w/w of (a) and from 0.0005 to 45% w/w of (b) or is a liquid and comprises from 5 to 90% w/v of (a) and from 0.005 to 60% w/v of (b), and
wherein the derivative of beta alanine is selected from the group consisting of N-acetyl-β-alanine, fluorinated methyl β-alanine, 3-amino-3-fluoromethylpropionic acid, a β-alanine ester, a β-alanine amide, a β-alanine salt, and β-alanine nitrate.
10 . The composition of claim 9 , wherein (a) and (b) are present at a weight ratio of between 1:1 to 1:80.
11 . The composition of claim 9 , wherein (a) comprises an effective amount of β-alanine.