Claims for Patent: 12,311,057

Summary for Patent: 12,311,057

Title:	Pharmaceutical compositions
Abstract:	The present invention provides for a method of treatment of IgA nephropathy, which method comprises:
Inventor(s):	Eva Kristina RIESEL, Lena Margareta PERESWETOFF-MORATH, Kari SANDVOLD, Christian Olle Andreas PEDERSEN
Assignee:	Calliditas Therapeutics AB
Application Number:	US18/934,978
Patent Claims:	1. A pharmaceutical composition comprising: a plurality of cores comprising budesonide encapsulated within a capsule comprising an enteric coating, wherein the plurality of cores are each coated with an extended release pharmaceutically-acceptable polymeric blend comprising a water-insoluble polymer having a solubility in water (at 25° C.) of less than about 0.1 mg/mL and a pore-forming polymer having a solubility in water (at 25° C.) of at least about 10 mg/mL, wherein the water-insoluble polymer is present in an amount of from about 47 wt. % to about 56 wt. % of the extended release pharmaceutically-acceptable polymeric blend and the pore-forming polymer is present in an amount of from about 32 wt. % to about 22 wt. % of the extended release pharmaceutically-acceptable polymeric blend; wherein the extended release pharmaceutically-acceptable polymeric blend is present in an amount of from 5 wt. % to about 18 wt. % of the total coated core weight; wherein the pharmaceutical composition meets the following release profile in a standard in vitro USP<711> dissolution test using a dissolution apparatus according to Apparatus 2 (Paddle Apparatus) at a paddle rotation speed of 100 rpm: a) no more than about 10% of the budesonide is released into an aqueous dissolution medium with a pH of about 1.2 within about 120 minutes; b) no more than about 10% of the budesonide is released into a pharmaceutically-relevant dissolution medium within about 30 minutes, wherein the pharmaceutically-relevant dissolution medium is a Level 1 Fasted State Simulated Intestinal Fluid at a pH of about 6.5, or a phosphate buffer medium at a pH of about 6.8; and c) at least about 70% of the budesonide is released into the pharmaceutically-relevant dissolution medium within about 120 minutes. 2. The pharmaceutical composition according to claim 1, wherein the water-insoluble polymer is an alkyl cellulose. 3. The pharmaceutical composition according to claim 2, wherein the alkyl cellulose is an ethyl cellulose. 4. The pharmaceutical composition according to claim 1, wherein the pore-forming polymer is selected from polyethylene glycol (PEG), hydroxypropylmethyl cellulose (HPMC), and hydroxypropyl cellulose (HPC). 5. The pharmaceutical composition according to claim 1, wherein the water-insoluble polymer is an alkyl cellulose and the pore-forming polymer is selected from polyethylene glycol (PEG), hydroxypropylmethyl cellulose (HPMC), and hydroxypropyl cellulose (HPC). 6. The pharmaceutical composition according to claim 1, wherein the extended release pharmaceutically-acceptable polymeric blend is present in an amount of from about 6 wt. % to about 13 wt. % of the total coated core weight. 7. The pharmaceutical composition according to claim 1, wherein the water-insoluble polymer and the pore-forming polymer are coalesced to form the extended release pharmaceutically-acceptable polymeric blend by curing the coated cores at a temperature of from about 55° C. to about 75° C. for about 1 hour to about 10 hours. 8. The pharmaceutical composition according to claim 1, wherein the pharmaceutically-relevant dissolution medium is a Level 1 Fasted State Simulated Intestinal Fluid at a pH of about 6.5. 9. The pharmaceutical composition according to claim 8, wherein the Level 1 Fasted State Simulated Intestinal Fluid comprises an added surfactant. 10. The pharmaceutical composition according to claim 9, wherein the added surfactant is present in an amount of about 0.5 mg/mL. 11. The pharmaceutical composition according to claim 1, wherein the pharmaceutically-relevant dissolution medium is a phosphate buffer medium at a pH of about 6.8. 12. The pharmaceutical composition according to claim 11, wherein the phosphate buffer medium comprises an added surfactant. 13. The pharmaceutical composition according to claim 12, wherein the surfactant is present in an amount of about 0.5 mg/mL. 14. The pharmaceutical composition according to claim 1, where the enteric coating is present in an amount of from about 34 mg to about 46 mg per capsule. 15. The pharmaceutical composition according to claim 1, where the enteric coating is present in an amount of from about 36 mg to about 40 mg per capsule. 16. The pharmaceutical composition according to claim 1, wherein the capsule is a size 1 capsule. 17. The pharmaceutical composition according to claim 1, wherein the capsule comprises about 4 mg of budesonide. 18. A method of treating IgA nephropathy in a subject in need thereof, comprising: orally administering to the subject the pharmaceutical composition of claim 1 at a daily dose of about 16 mg of budesonide. 19. The method according to claim 18, wherein the water-insoluble polymer is an alkyl cellulose. 20. The method according to claim 19, wherein the alkyl cellulose is an ethyl cellulose. 21. The method according to claim 18, wherein the pore-forming polymer is selected from polyethylene glycol (PEG), hydroxypropylmethyl cellulose (HPMC), and hydroxypropyl cellulose (HPC). 22. The method according to claim 18, wherein the water-insoluble polymer is an alkyl cellulose and the pore-forming polymer is selected from polyethylene glycol (PEG), hydroxypropylmethyl cellulose (HPMC), and hydroxypropyl cellulose (HPC). 23. The method according to claim 18, wherein the extended release pharmaceutically-acceptable polymeric blend is present in an amount of from about 6 wt. % to about 13 wt. % of the total coated core weight. 24. The method according to claim 18, wherein the water-insoluble polymer and the pore-forming polymer are coalesced to form the extended release pharmaceutically-acceptable polymeric blend by curing the coated cores at a temperature of from about 55° C. to about 75° C. for about 1 hour to about 10 hours. 25. The method according to claim 18, wherein the pharmaceutical composition is orally administered to the subject at least one hour before a meal. 26. The method according to claim 18, wherein the pharmaceutical composition is orally administered once daily. 27. The method according to claim 18, wherein the pharmaceutical composition is orally administered in the morning at least one hour before the first meal of the day. 28. The method according to claim 18, where the enteric coating is present in an amount of from about 34 mg to about 46 mg per capsule. 29. The method according to claim 18, where the enteric coating is present in an amount of from about 36 mg to about 40 mg per capsule. 30. The method according to claim 18, wherein the capsule is a size 1 capsule.