Preparation and Uses of Obeticholic Acid
The present invention relates to obeticholic acid: or a pharmaceutically acceptable salt, solvate or amino acid conjugate thereof. Obeticholic acid is useful for the treatment or prevention of a FXR mediated disease or condition, cardiovascular disease or cholestatic liver disease, and for reducing HDL cholesterol, for lowering triglycerides in a mammal, or for inhibition of fibrosis. The present invention also relates to processes for the synthesis of obeticholic acid.
1 . A tablet comprising a non-crystalline obeticholic acid in the amount of about 1 mg to about 25 mg.
2 . The tablet of claim 1 , wherein the non-crystalline obeticolic acid is in the amount of about 25 mg.
3 . The tablet of claim 1 , wherein the non-crystalline obeticolic acid is in the amount of about 10 mg.
4 . The tablet of claim 1 , wherein the non-crystalline obeticolic acid is in the amount of about 5 mg.
5 . The tablet of claim 1 , wherein the non-crystalline obeticolic acid is in the amount of about 1 mg to about 5 mg.
6 . The tablet of claim 1 , wherein the non-crystalline obeticolic acid is in the amount of about 1.2 mg to about 1.8 mg.
7 . The tablet of claim 1 , wherein the non-crystalline obeticolic acid is in the amount of about 1.3 mg to about 1.7 mg.
8 . The tablet of claim 1 , wherein the non-crystalline obeticolic acid is in the amount of about 1.5 mg.
9 . The tablet of claim 1 , wherein the non-crystalline obeticolic acid is in the amount of about 1 mg.
10 . A method for treating NASH comprising administering to a subject in need thereof a tablet comprising a non-crystalline obeticholic acid in the amount of about 1-25 mg in single or divided dose daily.
11 . The method of claim 10 , wherein the non-crystalline obeticholic acid is in the amount of about 25 mg.
12 . The method of claim 10 , wherein the non-crystalline obeticholic acid is in the amount of about 10 mg.
13 . The method of claim 10 , wherein the dose is a single dose daily.
14 . A method of treating biliary atresia comprising administering to a subject in need thereof a table comprising non-crystalline obeticholic acid in the amount of about 1 mg to about 25 mg in single or divided dose daily.
15 . The method of claim 14 , wherein obeticholic acid is in the amount of about 1 mg to about 5 mg.
16 . The method of claim 14 , wherein obeticholic acid is in the amount of about 1.2 mg to about 1.8 mg.
17 . The method of claim 14 , wherein obeticholic acid is in the amount of about 1.3 mg to about 1.5 mg.
18 . The method of claim 14 , wherein obeticholic acid is in the amount of about 1.5 mg.
19 . The method of claim 14 , wherein the obeticholic acid in in the amount of about 1 mg.
20 . The method of claim 14 , wherein the subject is a child.