US 11,813,250 B2
Topical formulations containing mTOR inhibitors
Shoufeng Li, Basking Ridge, NJ (US); Yi Zhao, Monmouth Junction, NJ (US); and Qiaolin Ren, Jericho, NY (US)
Assigned to SHANGHAI AUCTA PHARMACEUTICALS CO., LTD., Shanghai (CN)
Filed by Shanghai Aucta Pharmaceuticals Co., Ltd., Shanghai (CN)
Filed on Sep. 2, 2022, as Appl. No. 17/929,569.
Application 17/929,569 is a continuation in part of application No. PCT/IB2020/055930, filed on Jun. 23, 2020.
Claims priority of provisional application 62/984,000, filed on Mar. 2, 2020.
Prior Publication US 2023/0100760 A1, Mar. 30, 2023
Int. Cl. A01N 37/00 (2006.01); A61K 31/215 (2006.01); A01N 37/12 (2006.01); A01N 37/44 (2006.01); A61K 31/24 (2006.01); A01N 25/00 (2006.01); A61K 31/436 (2006.01); A61P 17/00 (2006.01); A61K 9/00 (2006.01); A61K 9/06 (2006.01); A61K 47/06 (2006.01); A61K 47/12 (2006.01); A61K 47/14 (2017.01); A61K 47/20 (2006.01); A61K 47/22 (2006.01); A61K 47/44 (2017.01)
CPC A61K 31/436 (2013.01) [A61K 9/0014 (2013.01); A61K 9/06 (2013.01); A61K 47/06 (2013.01); A61K 47/12 (2013.01); A61K 47/14 (2013.01); A61K 47/20 (2013.01); A61K 47/22 (2013.01); A61K 47/44 (2013.01); A61P 17/00 (2018.01)] 20 Claims
 
1. A formulation for topical delivery of a therapeutic agent, comprising:
(a) a therapeutically effective amount of sirolimus, and
(b) a solvent comprising dimethyl sulfoxide (DMSO) and propylene carbonate;
(c) one or more pharmaceutically acceptable carriers, wherein the one or more pharmaceutically acceptable carriers comprise caprylocaproyl polyoxyl-8 glycerides ranging from about 1% to about 10% by weight in the formulation;
wherein the DMSO and the propylene carbonate are in a ratio selected from a range of from about 1:1 to about 1:10 and, at a temperature of 30° C. and a humidity of 65%, less than 5% of isomer C is detected in the formulation in about 2 weeks or less than 0.8% seco-rapamycin is detected in the formulation in about 2 weeks, wherein the isomer C is represented by the structure below

OG Complex Work Unit Chemistry