CRYSTALLINE SOLVATE FORMS OF A PHARMACEUTICAL
Described herein are solid state 17α-ethynylandrost-5-ene-3β,7β,17β-triol including amorphous and crystalline forms and specific polymorphic forms thereof, and use of solid state 17α-ethynylandrost-5-ene-3β,7β,17β-triol in treating numerous diseases and disorders, including hyperglycemic conditions, such as type 2 diabetes and metabolic syndrome, autoimmune conditions, such as rheumatoid arthritis, ulcerative colitis and type 1 diabetes, among other inflammation related conditions, and neurodegenerative conditions in subjects or human patients.
1 . A method to treat a neurodegenerative condition comprising administering to a human or mammal in need thereof an effective amount of a pharmaceutical composition comprising a solid state form of 17α-ethynylandrost-5-ene-3β,7β,17β-triol and at least one pharmaceutically acceptable excipient.
2 . The method of claim 1 , wherein the neurodegenerative condition is Alzheimer's disease, Parkinson's disease or Amyotrophic Lateral Sclerosis.
3 . The method of claim 1 , wherein the solid state form of 17α-ethynylandrost-5-ene-3β,7β,17β-triol is crystalline solvate 17α-ethynylandrost-5-ene-3β,7β,17β-triol.
4 . The method of claim 3 , wherein the crystalline solvate is crystalline methanolate 17α-ethynylandrost-5-ene-3β,7β,17β-triol.
5 . The method of claim 3 , wherein the crystalline solvate is crystalline ethanolate 17α-ethynylandrost-5-ene-3β,7β,17β-triol.
6 . The method of claim 3 , wherein the crystalline solvate is crystalline hydrate 17α-ethynylandrost-5-ene-3β,7β,17β-triol.
7 . The method of claim 3 , wherein the crystalline solvate is Form III 17α-ethynylandrost-5-ene-3β,7β,17β-triol.
8 . The method of claim 3 , wherein the crystalline solvate is Form IV 17α-ethynylandrost-5-ene-3β,7β,17β-triol.
9 . The method of claim 3 , wherein the crystalline solvate is Form V 17α-ethynylandrost-5-ene-3β,7β,17β-triol.
10 . The method of claim 1 , wherein the solid state form of 17α-ethynylandrost-5-ene-3β,7β,17β-triol is amorphous 17α-ethynylandrost-5-ene-3β,7β,17β-triol.
11 . The method of claim 10 , wherein the pharmaceutical composition contains less than about 3% by weight of impurities.
12 . A method to treat an inflammation condition comprising administering to a human or mammal in need thereof an effective amount of a formulation comprising a solid state form of 17α-ethynylandrost-5-ene-3β,7β,17β-triol and at least one pharmaceutically acceptable excipient.
13 . The method of claim 12 , wherein the inflammation condition is an inflammatory bowel condition.
14 . The method of claim 12 , wherein the inflammation condition is an inflammatory lung condition.
15 . The method of claim 14 , wherein the inflammatory lung condition is cystic fibrosis, asthma, bronchitis or chronic obstructive pulmonary disease.
16 . The method of claim 12 , wherein the solid state form of 17α-ethynylandrost-5-ene-3β,7β,17β-triol is crystalline solvate 17α-ethynylandrost-5-ene-3β,7β,17β-triol.
17 . The method of claim 16 , wherein the crystalline solvate is crystalline methanolate 17α-ethynylandrost-5-ene-3β,7β,17β-triol.
18 . The method of claim 16 , wherein the crystalline solvate is crystalline ethanolate 17α-ethynylandrost-5-ene-3β,7β,17β-triol.
19 . The method of claim 16 , wherein the crystalline solvate is crystalline hydrate 17α-ethynylandrost-5-ene-3β,7β,17β-triol.
20 . The method of claim 16 , wherein the crystalline solvate is Form III 17α-ethynylandrost-5-ene-3β,7β,17β-triol.
21 . The method of claim 16 , wherein the crystalline solvate is Form IV 17α-ethynylandrost-5-ene-3β,7β,17β-triol.
22 . The method of claim 16 , wherein the crystalline solvate is Form V 17α-ethynylandrost-5-ene-3β,7β,17β-triol.
23 . The method of claim 12 , wherein the solid state form of 17α-ethynylandrost-5-ene-3β,7β,17β-triol is amorphous 17α-ethynylandrost-5-ene-3β,7β,17β-triol.
24 . The method of claim 23 , wherein the pharmaceutical composition contains less than about 3% by weight of impurities.
25 . A method to treat a metabolic syndrome, impaired glucose tolerance or a hyperglycemia condition comprising administering to a human or mammal in need thereof an effective amount of a formulation comprising a solid state form of 17α-ethynylandrost-5-ene-3β,7β,17β-triol and at least one pharmaceutically acceptable excipient.
26 . The method of claim 25 , wherein the hyperglycemia condition is type 1 diabetes or type 2 diabetes.
27 . The method of claim 25 , wherein the solid state form of 17α-ethynylandrost-5-ene-3β,7β,17β-triol is crystalline solvate 17α-ethynylandrost-5-ene-3β,7β,17β-triol.
28 . The method of claim 27 , wherein the crystalline solvate is crystalline methanolate 17α-ethynylandrost-5-ene-3β,7β,17β-triol.
29 . The method of claim 27 , wherein the crystalline solvate is crystalline ethanolate 17α-ethynylandrost-5-ene-3β,7β,17β-triol.
30 . The method of claim 27 , wherein the crystalline solvate is crystalline hydrate 17α-ethynylandrost-5-ene-3β,7β,17β-triol.
31 . The method of claim 27 , wherein the crystalline solvate is Form III 17α-ethynylandrost-5-ene-3β,7β,17β-triol.
32 . The method of claim 27 , wherein the crystalline solvate is Form IV 17α-ethynylandrost-5-ene-3β,7β,17β-triol.
33 . The method of claim 27 , wherein the crystalline solvate is Form V 17α-ethynylandrost-5-ene-3β,7β,17β-triol.
34 . The method of claim 25 , wherein the solid state form of 17α-ethynylandrost-5-ene-3β,7β,17β-triol is amorphous 17α-ethynylandrost-5-ene-3β,7β,17β-triol.
35 . The method of claim 34 , wherein the pharmaceutical composition contains less than about 3% by weight of impurities.