	US 12,226,381 B2
	Composition of fused tricyclic gamma-amino acid derivatives and the preparation thereof
Xuanmiao Zhang, Sichuan (CN); Feng Peng, Sichuan (CN); Hua Mao, Sichuan (CN); Juanjuan Deng, Sichuan (CN); and Pangke Yan, Sichuan (CN)
Assigned to SICHUAN HAISCO PHARMACEUTICAL CO., LTD., Sichuan (CN)
Appl. No. 17/259,757
Filed by SICHUAN HAISCO PHARMACEUTICAL CO., LTD., Sichuan (CN)
PCT Filed Jul. 12, 2019, PCT No. PCT/CN2019/095856 § 371(c)(1), (2) Date Jan. 12, 2021, PCT Pub. No. WO2020/011257, PCT Pub. Date Jan. 16, 2020.
Claims priority of application No. 201810756863.X (CN), filed on Jul. 12, 2018.
Prior Publication US 2021/0186909 A1, Jun. 24, 2021
Int. Cl. A61K 31/195 (2006.01); A61K 9/00 (2006.01); A61K 9/16 (2006.01); A61K 9/20 (2006.01); A61K 9/48 (2006.01); A61P 29/00 (2006.01)

CPC A61K 31/195 (2013.01) [A61K 9/0053 (2013.01); A61K 9/1694 (2013.01); A61K 9/2009 (2013.01); A61K 9/2013 (2013.01); A61K 9/2018 (2013.01); A61K 9/2027 (2013.01); A61K 9/2054 (2013.01); A61K 9/2095 (2013.01); A61K 9/4833 (2013.01); A61K 9/485 (2013.01); A61K 9/4858 (2013.01); A61K 9/4866 (2013.01); A61P 29/00 (2018.01)]

11 Claims

1. A pharmaceutical composition in a form of capsule or tablet comprising:

(i) an active material having a structure as represented by formula (I) or a pharmaceutically acceptable salt in an amount of 5% to 45% by weight;

(ii) one or more filler; wherein the filler is a combination of mannitol with a content of 10% to 28% by weight, microcrystalline cellulose A with a content of 3% to 8% by weight and microcrystalline cellulose B with a content of 40% to 75% by weight; wherein, the microcrystalline cellulose A is microcrystalline cellulose 12; the microcrystalline cellulose B is microcrystalline celluloses of 102; and

(iii) one or more lubricating agents in an amount of 0.5% to 5.5% by weight; wherein the lubricating agent is magnesium stearate;

wherein the sum of weight percentages of all the components is 100%;

wherein the structure of formula (I) is as follows: