Preparation of psilocybin, different polymorphic forms, intermediates, formulations and their use
This invention relates to the large-scale production of psilocybin for use in medicine. More particularly, it relates to a method of obtaining high purity crystalline psilocybin, particularly, in the form of Polymorph A. It further relates to a method for the manufacture of psilocybin and intermediates in the production thereof and formulations containing psilocybin.
1 . Crystalline psilocybin characterized by X-ray powder diffraction (XRPD) peaks at 17.5±0.1 and 19.7±0.1 °2θ, wherein the crystalline psilocybin is stable for at least 3 months at 25° C. and 60% relative humidity.
2 . The crystalline psilocybin of claim 1 , wherein the crystalline psilocybin is stable for at least 6 months at 25° C. and 60% relative humidity.
3 . The crystalline psilocybin of claim 1 , wherein the crystalline psilocybin is stable for at least 9 months at 25° C. and 60% relative humidity.
4 . The crystalline psilocybin of claim 1 , wherein the crystalline psilocybin is stable for at least 12 months at 25° C. and 60% relative humidity.
5 . The crystalline psilocybin of claim 1 , further characterized by at least one XRPD peak at 11.5±0.1, 12.0±0.1, or 14.5±0.1 °2θ.
6 . The crystalline psilocybin of claim 1 , further characterized by XRPD peaks at 11.5±0.1 and 12.0±0.1 °2θ.
7 . The crystalline psilocybin of claim 1 , further characterized by XRPD peaks at 11.5±0.1 and 14.5±0.1 °2θ.
8 . The crystalline psilocybin of claim 1 , further characterized by XRPD peaks at 12.0±0.1 and 14.5±0.1 °2θ.
9 . The crystalline psilocybin of claim 5 , further characterized by at least one XRPD peak at 20.4±0.1, 22.2±0.1, 24.3±0.1, or 25.7±0.1 °2θ.
10 . The crystalline psilocybin of claim 1 , having a chemical purity of greater than 97% as determined by high-performance liquid chromatography (HPLC) analysis.
11 . The crystalline psilocybin of claim 1 , having a chemical purity of greater than 98% as determined by HPLC.
12 . The crystalline psilocybin of claim 1 , having a chemical purity of greater than 99% as determined by HPLC.
13 . Crystalline psilocybin characterized by X-ray powder diffraction (XRPD) peaks at 17.5±0.1 and 19.7±0.1 °2θ, wherein the crystalline psilocybin is stable for at least 3 months at 40° C. and 75% relative humidity.
14 . The crystalline psilocybin of claim 13 , wherein the crystalline psilocybin is stable for at least 6 months at 40° C. and 75% relative humidity.
15 . The crystalline psilocybin of claim 13 , wherein the crystalline psilocybin is stable for at least 9 months at 40° C. and 75% relative humidity.
16 . The crystalline psilocybin of claim 13 , wherein the crystalline psilocybin is stable for at least 12 months at 40° C. and 75% relative humidity.
17 . The crystalline psilocybin of claim 13 , further characterized by at least one XRPD peak at 11.5±0.1, 12.0±0.1, or 14.5±0.1 °2θ.
18 . The crystalline psilocybin of claim 13 , further characterized by XRPD peaks at 11.5±0.1 and 12.0±0.1 °2θ.
19 . The crystalline psilocybin of claim 13 , further characterized by XRPD peaks at 11.5±0.1 and 14.5±0.1 °2θ.
20 . The crystalline psilocybin of claim 13 , further characterized by XRPD peaks at 12.0±0.1 and 14.5±0.1 °2θ.
21 . The crystalline psilocybin of claim 17 , further characterized by at least one XRPD peak at 20.4±0.1, 22.2±0.1, 24.3±0.1, or 25.7±0.1 °2θ.
22 . The crystalline psilocybin of claim 13 , having a chemical purity of greater than 97% as determined by high-performance liquid chromatography (HPLC) analysis.
23 . The crystalline psilocybin of claim 13 , having a chemical purity of greater than 98% as determined by HPLC.
24 . The crystalline psilocybin of claim 13 , having a chemical purity of greater than 99% as determined by HPLC.