Theacrine-based supplement and method of use thereof in a synergistic combination with caffeine
A human dietary supplement comprises theacrine and optionally other compounds that modulate the effects of theacrine. Uses for the theacrine-containing supplement include improvement of at least one of mood, energy, focus, concentration or sexual desire or a reduction of at least one of anxiety or fatigue. A synergistic composition comprises co-administration of theacrine and caffeine, wherein the co-administered caffeine reduces theacrine oral clearance (CL/F) and oral volume of distribution (Vd/F). In addition, the co-administered caffeine increases area under the plasma concentration time curve (AUC) of theacrine, and increases theacrine maximum plasma concentration (C max ) in comparison with the corresponding pharmacokinetic parameters when theacrine is administered alone.
1. A method of formulating a dietary supplement comprising the step of:
combining a nutraceutically acceptable carrier with theacrine, caffeine, and methylliberine;
wherein the dietary supplement is formulated for oral administration;
wherein the theacrine is present in the dietary supplement in an amount that is to modulate activity of the caffeine; and
wherein the theacrine and caffeine are present in the dietary supplement in a ratio of about 0.5:1 to about 50:1 by weight caffeine:theacrine.
2. The method of claim 1 , wherein the theacrine has a purity of at least 95%.
3. The method of claim 1 , wherein the theacrine is present in the dietary supplement in an amount of from about 5 mg to about 850 mg.
4. The method of claim 1 , wherein the dietary supplement is formulated into a solid oral dosage form.
5. The method of claim 4 , wherein said solid oral dosage form is a powder, capsule, or tablet.
6. The method of claim 1 , wherein the dietary supplement is formulated to, upon oral administration, increase mood, energy, focus, concentration, and/or sexual desire.
7. The method of claim 1 , wherein the theacrine is produced synthetically or is isolated from a natural source and purified to at least 50% theacrine.
8. The method of claim 1 , wherein said caffeine is present in the dietary supplement in an amount of about 25 mg to about 650 mg.
9. The method of claim 1 , wherein the theacrine is present in the dietary supplement in an amount from about 65 mg to about 300 mg.
10. The method of claim 1 , wherein the ratio is about 1:1 to about 10:1.
11. The method of claim 1 , wherein the ratio is about 2:1 to about 4:1.
12. The method of claim 1 , wherein the ratio is about 1.2:1.
13. A method of modulating activity of a stimulant comprising the steps of:
providing a dietary supplement comprising a nutraceutically acceptable carrier in combination with theacrine, caffeine, and methylliberine, and
administering the dietary supplement to a subject to modulate activity of the stimulant;
wherein the dietary supplement is formulated for oral administration;
wherein the stimulant is caffeine, and theacrine is included in the supplement in an amount that modulates activity of the caffeine;
wherein the theacrine and caffeine are present in the dietary supplement in a ratio of about 0.5:1 to about 50:1 by weight caffeine:theacrine.
14. The method of claim 13 , wherein the theacrine has a purity of at least 95%.
15. The method of claim 13 , wherein the theacrine is present in the dietary supplement in an amount of from about 5 mg to about 850 mg.
16. The method of claim 13 , wherein the dietary supplement is formulated into a solid oral dosage form.
17. The method of claim 16 , wherein said solid oral dosage form is a powder, capsule, or tablet.
18. The method of claim 13 , wherein the dietary supplement is formulated to, upon oral administration, increase mood, energy, focus, concentration, and/or sexual desire.
19. The method of claim 13 , wherein the theacrine is produced synthetically or is isolated from a natural source and purified to at least 50% theacrine.
20. The method of claim 13 , wherein said caffeine is present in the dietary supplement in an amount of about 25 mg to about 650 mg.
21. The method of claim 13 , wherein the theacrine is present in the dietary supplement in an amount from about 65 mg to about 300 mg.
22. The method of claim 13 , wherein the ratio is about 1:1 to about 10:1.
23. The method of claim 13 , wherein the ratio is about 2:1 to about 4:1.
24. The method of claim 13 , wherein the ratio is about 1.2:1.