银杏内酯固体分散体的辅料优选
The Choice of Preferred Materials of Ginkgolide Solid Dispersions
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摘要: 目的 通过优选最佳辅料及配比来制备银杏内酯固体分散体，以提高银杏内酯体外溶出度。方法 选取聚丙烯酸树脂EPO(Eudragit EPO)、聚维酮K30(PVP K30)分别与银杏内酯以不同配比运用溶剂法制备固体分散体，测定银杏内酯B(ginkgolide B，GB)溶出度，并用差示扫描量热（DSC）、X-射线衍射（X-RD）、扫描电镜（SEM）进行物相表征。结果 以银杏内酯/EPO配比为1∶2、1∶4、1∶6、1∶8制备的固体分散体5 min内GB溶出度分别为65%、68%、70%、71%；银杏内酯/PVP K30在相应配比下制备的固体分散体5 min内GB溶出度分别为40%、50%、66%、70%，而5 min内原料药溶出度为10%。物相鉴别结果表明银杏内酯在2种载体制备的固体分散体中均以无定型状态均匀分散。结论 以银杏内酯/EPO配比为1∶2制备的固体分散体载药量高、溶出效果佳，是制备银杏内酯固体分散体的最佳选择，具有较好的应用前景。Abstract: OBJECTIVE Choosing the optimizing assistance materials and the best proportional to make the solid dispersion of Ginkgolides， which so that can tremendously improve the dissolution rate of Ginkgolides. METHODS We determine the dissolution rate of the solid dispersion respectively， which are made by Eudragit EPO and PVP K30 in different drug-material ratio. In addition， quantitative phase determination of them are measured by DSC， X-RD and SEM. RESULTS The dissolution rate of the solid dispersion with the Ginkgolides -EPO ratio in 1∶2， 1∶4， 1∶6， 1∶8 were 65%， 68%， 70% and 71% respectively in five minutes. In the corresponding proportion， The dissolution rate of the solid dispersion made by PVP K30 were 40%， 50%， 66%， 70% respectively. In the same time， the dissolution rate of the drug substance were 10%. Phase identification results showed that Ginkgolides can evenly dispers in amorphous state in the solid dispersion. CONCLUSION The solid dispersion with the Ginkgolides -EPO ratio of 1∶2 is the best choice to preparation， which has the tremendous drug-loading and dissolution efficiency， thereby having a excellent prospect of application.
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