Transmucosal dephosphorylated psychoactive alkaloid composition and preparation thereof
A transmucosal psychoactive alkaloid composition including a psychoactive alkaloid extract or synthetic psychoactive alkaloid. The alkaloids in the extract are predominantly dephosphorylated rather than phosphorylated. The transmucosal psychoactive alkaloid composition also includes a mucoadhesive polymer, a carrier, and optional further excipients. The non-ingestive composition may be taken orally through the mucosa. A process for obtaining an oral transmucosal psychoactive alkaloid composition includes dephosphorylating the alkaloid during extraction, purifying the extracted alkaloid and standardizing to a specific concentration by adding measured quantities of excipients.
1. A transmucosal psychoactive alkaloid composition consisting of, by weight:
1-40% of a dephosphorylated psychoactive alkaloid extract comprising a psychoactive alkaloid that is psilocin, bufotenine, bufotenidine, norpsilocin, 4-hydroxytryptamine, N,N,N-trimethyl-4-hydroxytryptamine or any combination selected therefrom;
1-50% of mucoadhesive polymer;
10-65% of carrier; and
0-30.5% in total of one or more excipients other than the mucoadhesive polymer and the carrier.
2. The composition of claim 1 , wherein a content of the psychoactive alkaloid in the dephosphorylated psychoactive alkaloid extract is in a range from 0.1% to 99% by weight.
3. The composition of claim 2 , wherein the content of the psychoactive alkaloid in the dephosphorylated psychoactive alkaloid extract is defined as a percentage up to two decimal places.
4. The composition of claim 1 , wherein the dephosphorylated psychoactive alkaloid extract comprises naturally occurring substances from the group consisting of fats, sugars, carbohydrates, chitin, chitosan, minerals, waxes and proteins.
5. The composition of claim 4 , wherein the naturally occurring substances are present in the dephosphorylated psychoactive alkaloid extract in a concentration ranging from 1% to 99.9% by weight.
6. The composition of claim 1 , wherein the dephosphorylated psychoactive alkaloid extract has been through a purification process to remove one or more impurities selected from the group consisting of sugars, carbohydrates, chitin, chitosan, fats, minerals, waxes and proteins to result in a purified extract, and a content of the psychoactive alkaloid in the purified extract is in a range from 10% to 99% by weight.
7. The composition of claim 1 , comprising 15-35% by weight of the mucoadhesive polymer.
8. The composition of claim 1 , comprising 25-40% by weight of the carrier.
9. The composition of claim 1 , in a powder or a granular form.
10. The composition of claim 1 , in a tablet form.
11. The composition of claim 1 , comprising 10-50% by weight of the carrier.
12. The composition of claim 1 , wherein one of the one or more excipients is a binder and the composition comprises 5-20% by weight of the binder.
13. The composition of claim 12 , comprising 5-10% by weight of the binder.
14. The composition of claim 1 , wherein one of the one or more excipients is a preservative, and the composition comprises 1-5% by weight of the preservative.
15. The composition of claim 14 , comprising 3-5% by weight of the preservative.
16. The composition of claim 1 , wherein:
one of the one or more excipients is a bioavailability agent selected from the group consisting of beta cyclodextrin, alpha cyclodextrin, piperine, citric acid and beta-carbolines; and
the composition comprises up to 5% by weight of the bioavailability agent.
17. The composition of claim 16 , comprising 0.5-2% by weight of the bioavailability agent.
18. The composition of claim 1 , wherein one of the one or more excipients is a flavor agent, and the composition comprises up to 0.5% by weight of the flavor agent.
19. The composition of claim 18 , comprising 0.1% by weight of the flavor agent.
20. The composition of claim 1 , wherein one of the one or more excipients is a disintegrant and the composition comprises the disintegrant.
21. A process for obtaining a transmucosal psychoactive alkaloid composition, the process comprising:
mixing a dried powdered psychoactive alkaloid source with an acidified solvent to obtain a slurry, wherein:
the dried powdered psychoactive alkaloid source comprises psilocin, bufotenine, bufotenidine, norpsilocin, 4-hydroxytryptamine, N,N,N-trimethyl-4-hydroxytryptamine, psilocybin, baeocystin, norbaeocystin, aeruginascin or any combination selected therefrom; and
the acidified solvent has a pH of 3.5 or lower and is a mixture of an acid and a solvent that is a C1-C4 primary aliphatic alcohol, a C3-C4 ketone, water or any combination selected therefrom;
filtering the slurry to obtain a psychoactive alkaloid liquid;
adjusting the pH of the psychoactive alkaloid liquid to a pH ranging from 3.5-4.5;
evaporating the solvent from the psychoactive alkaloid liquid to obtain a dephosphorylated psychoactive alkaloid extract comprising a psychoactive alkaloid that is psilocin, bufotenine, bufotenidine, norpsilocin, 4-hydroxytryptamine, N,N,N-trimethyl-4-hydroxytryptamine or any combination selected therefrom; and
mixing the dephosphorylated psychoactive alkaloid extract with a mucoadhesive polymer and one or more other excipients including a carrier.
22. The process of claim 21 , wherein the transmucosal psychoactive alkaloid composition consists of, by weight:
1-40% of the dephosphorylated psychoactive alkaloid extract;
1-50% of the mucoadhesive polymer; and
10-95.5% of the one or more other excipients of which 10-65% is the carrier.
23. The process of claim 21 , wherein the acidified solvent has a pH ranging from 0.5-3.5.
24. The process of claim 21 , comprising:
interrupting the evaporating step when the solvent has been partially evaporated from the psychoactive alkaloid liquid, to result in a concentrated slurry;
measuring a psychoactive alkaloid content in the concentrated slurry;
measuring a dry mass content in the concentrated slurry;
using the psychoactive alkaloid content, the dry mass content, and a specified concentration of the psychoactive alkaloid in the transmucosal psychoactive alkaloid composition to determine a quantity of the mucoadhesive polymer and a quantity of the one or more other excipients to add to the concentrated slurry in order to obtain the specified concentration when the solvent is completely evaporated;
performing a second mixing step with the quantity of the mucoadhesive polymer and the quantity of the one or more other excipients, thereby standardizing the concentrated slurry; and
continuing the evaporating step to result in the transmucosal psychoactive alkaloid composition with a specified concentration of the psychoactive alkaloid.
25. The process of claim 21 , comprising adding a binder to the transmucosal psychoactive alkaloid composition.
26. The process of claim 21 , comprising adding a bioavailability agent to the transmucosal psychoactive alkaloid composition.
27. The process of claim 21 , comprising adding a flavor agent to the transmucosal psychoactive alkaloid composition.
28. The process of claim 21 , comprising adding a preservative to the transmucosal psychoactive alkaloid composition.
29. The process of claim 21 , comprising forming a tablet with the transmucosal psychoactive alkaloid composition.