Highly soluble purine bioactive compounds and compositions thereof
View Patent ↗The invention provides nutritional supplements, in powder, tablet or capsule dosage forms and aqueous formulations, containing one or more of the purine bioactive compounds described including theacrine and theacrine species.
1. Stable aqueous compositions for oral administration of at least one biologically-active form of a purine alkaloid compound structurally related to caffeine to a mammalian subject, which compositions comprise:
a) 1,3,7,9-tetramethyluric acid (theacrine), (O(2), 2-Methoxy-1,9-dimethyl-7H-purine-6,8-dione (liberine) and (O(2), 1,7,9-trimethyluric acid (methylliberine), said liberine and methylliberine collectively referred to as theacrine species, wherein a basic uric acid structure has been partially or fully methylated in 2, 3 or 4 positions; and
b) at least one aqueous buffered solution having a pH range of about 1.5-9.0.
2. A composition according to claim 1 wherein said theacrine, or theacrine species are present in said aqueous composition in any amount between about 0.01% and about 10% by weight based on the total weight of said composition, including all percentages and ranges of percentages therebetween.
3. A composition according to claim 1 , further comprising one or more nutritional adjuvant materials selected from the group consisting of: flavoring agents, colorants, viscosity modifiers, preservatives, fragrances, amino acids and their salts, vitamins, minerals, essential fatty acids, enzymes, co-enzymes, mono-glycerides, di-glycerides, tri-glyceride ester oils emulsifiers, hydrolyzed proteins, whey protein, stabilizers, flow modifiers, viscosity improvers, chelating agents, anti-oxidants, anti-microbials, benzoates, alcohols, esters of para-hydroxybenzoic acid, propionates, preservatives, surfactants, including anionic, cationic or nonionic surfactants, or combinations thereof.
4. A composition according to claim 3 wherein the total amount of said one or more nutritional adjuvant materials present is present in any amount between about 0.01% and about 10% by weight based on the total weight of said composition.
5. A composition according to claim 1 further comprising one or more natural beverages, including, milk products, soy products, ice cream, yoghurt, citrus fruit juices, non-citrus fruit juices, vegetable juices, components of any of the foregoing, or combinations thereof.
6. A composition according to claim 5 wherein said one or more natural beverages is present in any amount between about 0.1% and about 99% by weight based on the total weight of said composition.
7. A composition according to claim 1 , comprising an anti-microbial preservative present in an effective amount to inhibit microbial growth.
8. A composition according to claim 7 wherein said preservative comprises a preservative selected from the group consisting of: one or more esters of para-hydroxy benzoic acid, propionates, and one or more sorbate salts.
9. A method for administering a bioactive form of theacrine to a mammalian subject said method comprising the steps of: preparing a composition according to claim 1 ; and orally administering said composition.
10. The method of claim 9 wherein said method further comprises increasing locomotor activity in the mammalian subject.
11. The method of claim 10 , wherein said increasing locomotor activity is maintained for extended time by chronic oral administration of said composition to the mammalian subject.
12. The method of claim 9 further comprising providing enhanced activity levels in a dose-dependent manner in the mammalian subject.
13. The method of claim 9 further comprising reducing inflammation in the mammalian subject.
14. The method of claim 9 further comprising reducing pain of the mammalian subject.
15. The method of claim 9 further comprising increasing endurance in the mammalian subject.
16. The method of claim 9 further comprising reducing depression in the mammalian subject.
17. The method of claim 9 further comprising alleviating the deleterious effects of hypergycemia in the mammalian subject.
18. The method of claim 9 further comprising alleviating the deleterious effects of sleep deprivation in the mammalian subject.
19. The method of claim 9 further comprising administering one or more of purine alkaloids in combination with at least one psychostimulant.
20. The method of claim 9 , wherein said step of orally administering comprises chronic or acute administration of a composition to the mammalian subject.