Treatment methods using pharmaceutical solid state forms
View Patent ↗The invention provides and describes solid state 17α-ethynyl-androst-5-ene-3β, 7β,17β-triol including amorphous and crystalline forms and specific polymorphic forms thereof. Anhydrates and solvates of 17α-ethynyl-androst-5-ene-3β, 7β,17β-triol include Form I anhydrate and Form IV and Form V solvates. The invention further relates to solid and suspension formulations containing 17α-ethynyl-androst-5-ene-3β,7β,17β-triol in a described solid state form and use of the formulations to treat hyperglycemic conditions, such as type 2 diabetes and metabolic syndrome, and autoimmune conditions, such as rheumatoid arthritis, ulcerative colitis and type 1 diabetes, among other inflammation related conditions in subjects or human patients. The invention also relates to methods to make liquid formulations from solid state forms of 17α-ethynyl-androst-5-ene-3β, 7β,17β-triol and uses of such formulations in treating the described conditions.
1. A method to treat an inflammation condition in a subject comprising administering to the subject an effective amount of crystalline Form I 17α-ethynylandrost-5-ene-3β,7β,17β-triol.
2. The method of claim 1 wherein the inflammation condition is a disease or condition associated with neuroinflammation.
3. The method of claim 2 wherein the disease or condition associated with neuroinflammation is Alzheimer's Disease, Parkinson's Disease, amyotropic lateral sclerosis or age-related macular degeneration.
4. The method of claim 1 wherein the inflammation condition is associated with ischemia, hemorrhage or a trauma.
5. The method of claim 4 wherein the inflammation condition associated with ischemia, hemorrhage or a trauma is a myocardial infarction or a stroke.
6. The method of claim 1 wherein the inflammation condition is an autoimmune disease, selected from the group consisting of type 1 diabetes, multiple sclerosis, and rheumatoid arthritis.
7. The method of claim 6 wherein the autoimmune disease is type 1 diabetes or multiple sclerosis.
8. The method of claim 1 wherein the inflammation condition is an inflammatory bowel disease.
9. The method of claim 8 wherein the inflammatory bowel disease is ulcerative colitis or Crohn's disease.
10. The method of claim 3 wherein the disease or condition associated with neuroinflammation is Parkinson's Disease.
11. The method of claim 1 wherein the crystalline Form I 17α-ethynylandrost-5-ene-3β,7β,17β-triol is a crystalline Form I 17α-ethynylandrost-5-ene-3β,7β,17β-triol anhydrate, wherein the inflammation condition is a disease or condition associated with neuroinflammation, selected from the group consisting of Alzheimer's Disease, Parkinson's Disease, amyotropic lateral sclerosis and age-related macular degeneration.
12. The method of claim 11 wherein the disease or condition associated with neuroinflammation is Parkinson's Disease.
13. A method to treat an inflammation condition in a subject comprising administering to the subject an effective amount of a crystalline Form III 17α-ethynylandrost-5-ene-3β,7β,17β-triol hydrate, wherein the inflammation condition is a disease or condition associated with neuroinflammation, selected from the group consisting of Alzheimer's Disease, Parkinson's Disease, amyotropic lateral sclerosis and age-related macular degeneration.
14. A method to treat an inflammation condition in a subject comprising administering to the subject an effective amount of a crystalline Form IV 17α-ethynylandrost-5-ene-3β,7β,17β-triol solvate, wherein the inflammation condition is a disease or condition associated with neuroinflammation, selected from the group consisting of Alzheimer's Disease, Parkinson's Disease, amyotropic lateral sclerosis and age-related macular degeneration.
15. A method to treat an inflammation condition in a subject comprising administering to the subject an effective amount of crystalline Form II 17α-ethynylandrost-5-ene-3β,7β,17β-triol, wherein the inflammation condition is a disease or condition associated with neuroinflammation selected from the group consisting of Alzheimer's Disease, Parkinson's Disease, amyotropic lateral sclerosis and age-related macular degeneration.
16. The method of claim 15 wherein the disease or condition associated with neuroinflammation is Parkinson's Disease.
17. The method of claim 13 , wherein the disease or condition associated with neuroinflammation is Parkinson's Disease.
18. The method of claim 14 , wherein the disease or condition associated with neuroinflammation is Parkinson's Disease.
19. The method of claim 13 , wherein the disease or condition associated with neuroinflammation is age-related macular degeneration.
20. The method of claim 14 , wherein the disease or condition associated with neuroinflammation is age-related macular degeneration.
21. The method of claim 15 , wherein the disease or condition associated with neuroinflammation is age-related macular degeneration.
22. The method of claim 6 wherein the autoimmune disease is rheumatoid arthritis.