	US 12,343,430 B2
	Methods of improving pharmaceutical substance solubilization and products thereof
Zheng Tan, Beijing (CN); Jingang Wang, Beijing (CN); and Chen Yang, Beijing (CN)
Assigned to MUDANJIANG LINRUN PHARAMA EXCIPIENTS LLC., Mudanjiang (CN)
Appl. No. 17/598,797
Filed by MUDANJIANG LINRUN PHARAMA EXCIPIENTS LLC., Mudanjiang (CN)
PCT Filed Apr. 7, 2020, PCT No. PCT/US2020/027023 § 371(c)(1), (2) Date Sep. 27, 2021, PCT Pub. No. WO2020/210205, PCT Pub. Date Oct. 15, 2020.
Claims priority of provisional application 62/830,740, filed on Apr. 8, 2019.
Prior Publication US 2022/0175677 A1, Jun. 9, 2022
Int. Cl. A61K 9/14 (2006.01); A61K 47/32 (2006.01); A61K 47/34 (2017.01); A61K 47/38 (2006.01); B29B 7/00 (2006.01); B29B 9/12 (2006.01)

CPC A61K 9/146 (2013.01) [A61K 47/32 (2013.01); A61K 47/34 (2013.01); A61K 47/38 (2013.01); B29B 7/007 (2013.01); B29B 9/12 (2013.01)]

20 Claims

1. A method of increasing solubility of an active pharmaceutical ingredient (API), comprising co-attriting a dry or substantially dry mixture of the API and a solubility-enhancing excipient with a kneading or extrusion device without heating, and if needed, applying cooling to the device to maintain temperature below the melting point of the API to form a co-attrition mixture, and applying an attrition force sufficient to increase the API solubility by at least 20%, wherein the API content in the co-attrition mixture ranges from 10% to 90% by weight, and wherein the co-attrition mixture is a solid or semi-solid dispersion comprising the API in a crystalline or partially crystalline form.