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Last Updated: March 28, 2024

Claims for Patent: 10,052,337


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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.

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