Revealing the roles of polymers in supersaturation stabilization from the perspective of crystallization behaviors: A case of nimodipine

Autor: Peixu, Zhao, Guowei, Hu, Haonan, Chen, Mo, Li, Yiting, Wang, Nan, Sun, Lulu, Wang, Yuan, Xu, Jialong, Xia, Baocheng, Tian, Yanhua, Liu, Zhonggui, He, Qiang, Fu
Rok vydání: 2022
Předmět:
Zdroj: International Journal of Pharmaceutics. 616:121538
ISSN: 0378-5173
DOI: 10.1016/j.ijpharm.2022.121538
Popis: Formulating drugs into amorphous solid dispersions (ASDs) represents an attractive means to enhance the aqueous solubility of drugs. Furthermore, water-soluble polymers have proven highly advantageous for stabilizing supersaturated solutions of ASDs. However, the performance and mechanism of various polymers in stabilizing supersaturated drug solutions have not been well-studied. The aim of this study was to investigate the effects of different commercial polymers on the dissolution behaviors and supersaturation stabilization of the ASDs and to further explore the mechanism of polymer mediated supersaturation maintenance by studying the crystallization behaviors of the ASDs. In this study, nimodipine (NMD) was used as a model drug because of its poor water-solubility and fast crystallization rate in aqueous solution, and three polymers polyvinylpyrrolidone (PVP), vinylpyrrolidone-vinyl acetate copolymer (PVP VA), and polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft co-polymer (Soluplus) was selected as the drug carriers to form the ASDs with NMD. Solid-state characterizations of the ASDs confirmed the amorphous state of the ASD systems. ASD
Databáze: OpenAIRE