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目的:应用热熔挤出技术制备难溶性药物银杏总内酯固体分散体,以提高其体外溶出度。方法:选用聚丙烯酸树酯EPO(Eudragit EPO)、共聚维酮S-630(Plasdone S-630)、羟丙基纤维素(HPC)分别与银杏总内酯以一定比例混合,运用热熔挤出技术制备其固体分散体。采用差示扫描量热分析(DSC)、X-射线衍射分析(X-RD)、红外光谱(FT-IR)、体外溶出度来表征和评价所制备的固体分散体。结果:以Plasdone S-630为载体制备的银杏总内酯固体分散体药物溶出效果最佳,在0.1 mol/L的盐酸溶出介质中5 min的银杏内酯B累计溶出达到92%,明显高于物理混合物(1 h时仅有88%)。DSC及X-RD结果表明3种载体辅料所制得固体分散体中药物均以无定形状态存在。结论:热熔挤出技术制备银杏总内酯固体分散体是一种有效可行的提高其体外溶出度的方法。
OBJECTIVE: To prepare the solid dispersion of ginkgolide lactone, which is a poorly soluble drug, by hot melt extrusion in order to improve its in vitro dissolution. Methods: Eudragit EPO (Eudragit EPO), Plasdone S-630 (PPD) and hydroxypropylcellulose (HPC) were mixed with total ginkgolides in a certain proportion, respectively. The technical preparation of its solid dispersion. The prepared solid dispersions were characterized and evaluated using differential scanning calorimetry (DSC), X-ray diffraction (X-RD), infrared spectroscopy (FT-IR), and in vitro dissolution. Results: The drug dissolution of Ginkgo total lactone solid dispersion prepared with Plasdone S-630 was the best. The dissolution of Ginkgolide B reached 92% in 0.1 mol / L hydrochloric acid dissolution medium for 5 min, which was significantly higher than Physical mixture (only 88% at 1 h). The results of DSC and X-RD show that the solid dispersions prepared from the three kinds of carrier excipients all exist in an amorphous state. Conclusion: Hot-melt extrusion of Ginkgo biloba lactone solid dispersion is an effective and feasible method to improve its in vitro dissolution.