Claims for Patent: 10,052,337

Summary for Patent: 10,052,337

Title:	Compositions of obeticholic acid and methods of use
Abstract:	The disclosure relates to obeticholic acid formulations with improved stability, dissolution, and/or solubility, methods of preparing the same for use and methods of treating various diseases and conditions.
Inventor(s):	Lancaster; Richard Gail (San Diego, CA), Olmstead; Kay K. (Escondido, CA), Kagihiro; Masashi (Suita, JP), Matono; Mitsuhiro (Sett-sushi, JP), Taoka; Ikuko (Toyonaka, JP), Pruzanski; Mark (New York, NY), Shapiro; David (Rancho Sante Fe, CA), Hooshmand-Rad; Roya (San Diego, CA), Pencek; Richard (San Diego, CA), Sciacca; Cathi (San Diego, CA), Eliot; Lise (San Diego, CA), Edwards; Jeffrey (San Diego, CA), MacConell; Leigh A. (Encinitas, CA), Marmon; Tonya K. (San Diego, CA)
Assignee:	Intercept Pharmaceuticals, Inc. (New York, NY)
Application Number:	15/139,138
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 10,052,337
Patent Claims:	1. A composition comprising obeticholic acid, or a pharmaceutically acceptable salt, ester, or amino acid conjugate thereof, wherein obeticholic acid or a pharmaceutically acceptable salt, ester, or amino acid conjugate thereof is in the form of particles, and wherein at least 50% of the particles have a diameter of 200 .mu.m or less. 2. The composition of claim 1, wherein at least 50% of the particles have a diameter of 100 .mu.m or less. 3. The composition of claim 2, wherein at least 50% of the particles have a diameter of 50 .mu.m or less. 4. The composition of claim 3, wherein at least 50% of the particles have a diameter of 10 .mu.m or less. 5. The composition of claim 4, wherein at least 50% of the particles have a diameter of 5 .mu.m or less. 6. The composition of claim 1, wherein at least 90% of the particles have a diameter of 200 .mu.m or less. 7. The composition of claim 6, wherein at least 90% of the particles have a diameter of 100 .mu.m or less. 8. The composition of claim 7, wherein at least 90% of the particles have a diameter of 25 .mu.m or less. 9. The composition of claim 1 further comprising at least one pharmaceutically acceptable excipient having an alcohol content of less than about 6% (wt/wt). 10. The composition of claim 9, wherein the at least one pharmaceutical acceptable excipient is sodium starch glycolate. 11. A tablet comprising an intra-granular portion and an extra-granular portion, the intra-granular portion comprising obeticholic acid, or a pharmaceutically acceptable salt, ester, or amino acid conjugate thereof, microcrystalline cellulose, and one or more additional pharmaceutical excipients, and the extra-granular portion comprising one or more pharmaceutical excipients. 12. The tablet of claim 11, wherein the extra-granular portion comprises microcrystalline cellulose. 13. A method for preparing a composition comprising obeticholic acid, or a pharmaceutically acceptable salt, ester, or amino acid conjugate thereof, in the form of particles, wherein at least 50% of the particles have a diameter of 200 .mu.m or less, comprising forming the particles through jet-milling. 14. The tablet of claim 11, wherein obeticholic acid or a pharmaceutically acceptable salt, ester, or amino acid conjugate thereof is jet-milled. 15. The tablet of claim 14, wherein obeticholic acid or a pharmaceutically acceptable salt, ester, or amino acid conjugate thereof is in the form of particles, and wherein at least 50% of the particles have a diameter of 200 .mu.m or less. 16. The composition of claim 1 is in a unit dosage form. 17. The composition of claim 16, wherein the unit dosage form is a tablet. 18. The composition of claim 17, wherein the tablet comprises an intra-granular portion and an extra-granular portion. 19. The composition of claim 18, wherein the intra-granular portion comprises microcrystalline cellulose and obeticholic acid, or a pharmaceutically acceptable salt, ester, or amino acid conjugate thereof in a ratio between about 20:1 to about 1:5.