US 12,311,057 B2
Pharmaceutical compositions
Eva Kristina Riesel, Mölndal (SE); Lena Margareta Pereswetoff-Morath, Spånga (SE); Kari Sandvold, Uppsala (SE); and Christian Olle Andreas Pedersen, Uppsala (SE)
Assigned to CALLIDITAS THERAPEUTICS AB, Stockholm (SE)
Filed by CALLIDITAS THERAPEUTICS AB, Stockholm (SE)
Filed on Nov. 1, 2024, as Appl. No. 18/934,978.
Application 18/934,978 is a continuation of application No. 18/392,602, filed on Dec. 21, 2023, granted, now 12,171,882.
Application 18/392,602 is a continuation of application No. 18/100,396, filed on Jan. 23, 2023, granted, now 11,896,719, issued on Feb. 13, 2024.
Claims priority of provisional application 63/302,216, filed on Jan. 24, 2022.
Claims priority of provisional application 63/302,226, filed on Jan. 24, 2022.
Claims priority of application No. 2217146 (GB), filed on Nov. 16, 2022; and application No. 2217150 (GB), filed on Nov. 16, 2022.
Prior Publication US 2025/0057775 A1, Feb. 20, 2025
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 9/48 (2006.01); A61K 9/28 (2006.01); A61K 9/50 (2006.01); A61K 31/58 (2006.01); A61P 13/12 (2006.01)
CPC A61K 9/4891 (2013.01) [A61K 9/2846 (2013.01); A61K 9/5047 (2013.01); A61K 31/58 (2013.01); A61P 13/12 (2018.01)] 30 Claims
OG exemplary drawing
 
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.