热熔挤出技术制备固体分散体研究.pdfVIP

( 110016) [] X beagle HPMC Eudragit EPO S630 Eudragit EPO PVP/VA HPMC [] The Application of Hot-Melt Extrusion in Preparing Solid Dispersions ZHENG Xin, YANG Rui, TANG Xing*, ZHENG liang-yuan School of Pharmacy Shenyang Pharmaceutical University Shenyang 110016 China [Abstract]. The objective of the study was to characterize the physical and rheological properties of drug and selected polymers to assess their suitability for use in the hot-melt extrusion (HME) process as a means to improve solubility by manufacturing either solid dispersion or solid solution. The evaluation of the properties of the dispersions was performed using solubility parameters calculation, solubility measurements, dissolution studies, IR, DSC, SEM and XRPD. The results of experiments indicated that nimodipine were in the solid solution in the PVP/VA and Eudragit EPO systems, while amorphous state in the HPMC system. The solid dispersions of nimodipine with three formulations markedly enhanced drug dissolution compared to the pure drug and the physical mixturse. The enhancement of dissolution rate was influenced by the polymer drug ratio. The mean bioavailability of nimodipine was comparable after ® ® administration of the Eudragit EPO solid dispersion and Nimotop , but the HPMC and PVP/VA dispersions exhibited much lower bioavailability. However, the AUC0–12 h values of all three solid dispersions wer