公开(公告)号：US20230391788A1

公开(公告)日：2023-12-07

申请号：US18250853

申请日：2021-10-27

申请人： NAVIN SAXENA RESEARCH & TECHNOLOGY PVT. LTD.

发明人： Kunal SAXENA ,  Aarkarsh SAXENA

IPC分类号： C07D489/09 ,  A61K47/44 ,  A61K47/10 ,  A61K9/00 ,  A61K47/34 ,  A61K31/485

CPC分类号： C07D489/09 ,  A61K47/44 ,  A61K47/10 ,  A61K9/0019 ,  A61K47/34 ,  A61K31/485

摘要： Disclosed herein is an improved process for preparation of naltrexone decanoate under a monophasic medium using a single solvent by esterifying naltrexone with a decanoyl chloride in the presence of an organic base, wherein the solvent is preferably cyclo-pentyl-methyl-ether (CPME) which is non-toxic in nature. The invention further discloses the elimination of an impurity bis-decanoyl naltrexone obtained during the preparation of naltrexone decanoate by preparing acid addition salts of naltrexone decanoate and reconverting into naltrexone decanoate from its acid addition salts by neutralizing using a base in the presence of suitable solvent to obtain naltrexone decanoate with a purity of more than 99% The invention also discloses pharmaceutical composition of naltrexone decanoate with at least one pharmaceutically acceptable excipient and method of use of naltrexone decanoate for the treatment of opioid dependence, alcohol dependence for a period of 7 days to 90 days in a patient in need thereof.