US 11,730,708 B2
Dosage form for use in treating or preventing of a disease
Priyanka Haksar, Thane (IN); Shraddha Joshi, Thane (IN); Umesh Kapale, Solapur (IN); Nilam Bharambe, Dombivali West (IN); Ashish Guha, Mumbai (IN); and Vinay Jain, Mumbai (IN)
Assigned to Evonik Operations GmbH, Essen (DE)
Appl. No. 17/757,043
Filed by Evonik Operations GmbH, Essen (DE)
PCT Filed Sep. 17, 2020, PCT No. PCT/EP2020/075962
§ 371(c)(1), (2) Date Jun. 8, 2022,
PCT Pub. No. WO2021/115650, PCT Pub. Date Jun. 17, 2021.
Claims priority of application No. 201941051259 (IN), filed on Dec. 11, 2019.
Prior Publication US 2023/0012981 A1, Jan. 19, 2023
Int. Cl. A61K 9/50 (2006.01); A61K 31/145 (2006.01); A61K 9/20 (2006.01); A61K 9/28 (2006.01); A61K 31/137 (2006.01); A61K 31/155 (2006.01); A61K 31/404 (2006.01); A61K 31/405 (2006.01); A61K 31/4402 (2006.01); A61K 31/4706 (2006.01); A61K 31/496 (2006.01); A61K 31/55 (2006.01); A61K 31/58 (2006.01); A61K 31/635 (2006.01); A61K 31/7048 (2006.01)
CPC A61K 31/145 (2013.01) [A61K 9/2054 (2013.01); A61K 9/2813 (2013.01); A61K 9/2826 (2013.01); A61K 9/2846 (2013.01); A61K 9/2866 (2013.01); A61K 31/137 (2013.01); A61K 31/155 (2013.01); A61K 31/404 (2013.01); A61K 31/405 (2013.01); A61K 31/4402 (2013.01); A61K 31/4706 (2013.01); A61K 31/496 (2013.01); A61K 31/55 (2013.01); A61K 31/58 (2013.01); A61K 31/635 (2013.01); A61K 31/7048 (2013.01)] 15 Claims
 
1. A dosage form, comprising:
a core, comprising a biologically active ingredient,
an intermediate coating layer (ICL) onto the core, comprising an alkaline agent, wherein the alkaline agent is selected from the group consisting of calcium oxide, calcium carbonate, magnesium carbonate, magnesium oxide, sodium carbonate, sodium bicarbonate, sodium hydroxide, and a combination thereof, and
an enteric coating layer (ECL) onto the intermediate coating layer, comprising an enteric polymer, the enteric layer forming an outer layer of the dosage form,
wherein a relation of the alkaline agent to the enteric polymer is 5 to 95% when calculated by the formula:

OG Complex Work Unit Math
wherein the biologically active ingredient is not a proton-pump inhibitor belonging to a class of substituted benzimidazole compounds,
wherein the biologically active ingredient is released in an amount of 10% or less at a pH of 1.2 for 120 min, and in an amount of 50% or more at a pH from 3 to 5.5 for 45 min in the small intestine, and
wherein the intermediate coating layer is present in an amount of 7.5 to 50% by weight, calculated based on the weight of the core,
wherein the dosage form is suitable for the treatment of a disease requiring release of 50% or more of the biologically active ingredient.