文献类型：期刊文献

英文题名：Stabilizing Effect of Soluplus on Erlotinib Metastable Crystal Form in Microparticles and Amorphous Solid Dispersions

作者：Jia, Shuyu[1];Ning, Shangqi[1];Leng, Yuting[1];Jing, Qiufang[1];Xu, Zhongyu[1];Ren, Fuzheng[1]

机构：[1]East China Univ Sci & Technol, Shanghai Frontiers Sci Ctr Optogenet Tech Cell Me, Engn Res Ctr Pharmaceut Proc Chem, Sch Pharm,Minist Educ,Shanghai Key Lab New Drug D, Shanghai 200237, Peoples R China

年份：2022

卷号：14

期号：6

外文期刊名：POLYMERS

收录：;EI(收录号：20221311852685);WOS:【SCI-EXPANDED(收录号:WOS:000774327400001)】；

基金：Shanghai Key Laboratory of New Drug Design (Grant No. 17DZ2271000); Shanghai Frontiers Science Center of Optogenetic Techniques for Cell Metabolism (Shanghai Municipal Education Commission).

语种：英文

外文关键词：erlotinib; soluplus; microparticles; solid dispersions; stabilization

摘要：Microparticles (MPs) and amorphous solid dispersions (SDs) are effective methods to improve the dissolution of insoluble drugs. However, stability is a concern for these two high-energy systems, resulting from high surface area and amorphous polymorph, respectively. As an amphiphilic polymer, Soluplus (SOL) is usually used as a carrier in SDs. In this study, erlotinib microparticles (ERL MPs) and erlotinib solid dispersions (ERL SDs) were prepared with SOL by bottom-up technology and solvent evaporation. The solid-state properties of ERL MPs and ERL SDs were characterized by Differential Scanning Calorimetry (DSC), Powder X-Ray Diffraction (PXRD) and Scanning Electron Microscopy (SEM). The ERL MPs existed in a metastable crystal form A while the ERL SDs existed in an amorphous state. Fourier transform infrared spectroscopy (FT-IR) showed that there was a hydrogen bond interaction between the N-H group of ERL and the carbonyl group of SOL in ERL MPs and SDs. The dissolution profiles of ERL SDs and ERL MPs were improved significantly. ERL MPs showed better stability than ERL SDs in accelerated stability test. The discrepant stabilizing effects of polymer SOL in two systems may provide effective ideas for solubilization of insoluble drugs and the stability of drugs after recrystallization.