喷雾冷冻干燥法制备丹参酮ⅡA固体分散体及其理化性质评价

 目的 采用喷雾冷冻干燥法（spray freeze drying, SFD）制备丹参酮ⅡA的固体分散体，提高其在水中的溶出度。方法 以丹参酮ⅡA的溶出度为指标，筛选不同的辅料, 并且对所制备的固体分散体进行理化性质的评价。结果 药辅比（丹参酮ⅡA-泊洛沙姆188）在1∶9的条件下，喷雾冷冻干燥法得到固体分散体比原药的比表面积增大3倍，其中大部分丹参酮ⅡA由晶体状态转变为无定形状态，丹参酮ⅡA的溶出度显著提高，70%的药物可以在10 min内从固体分散体中溶出。结论 和原药相比，喷雾冷冻干燥法制备的丹参酮ⅡA固体分散体的溶出度有很大改善，为提高其口服生物利用度提供了必要的条件。

Preparation of TanshinoneⅡA Solid Dispersion by Spray Freeze Drying and Its Characterization

OBJECTIVE To prepare tanshinone ⅡA solid dispersion using spray freeze drying(SFD) method.METHODS Dissolution profiles of tanshinone ⅡA from different solid dispersions prepared with various excipients were plotted.Based on the dissolution rate,F68 was selected as the excipient.The optimized formula was characterized in terms of morphology,surface area and crystallinity.RESULTS Compared to raw material,the specific surface of tanshinone ⅡA solid dispersion prepared by SFD method with drug-F68 ratio of 1∶9(w/w) increased by 3 folds.The majority of the tanshinoneⅡA in the solid dispersion transformed from crystalline form to amorphous state.As a result,the dissolution rate of TanshinoneⅡA significantly enhanced,and 70% of tanshinoneⅡA in the solid dispersion were dissolved in 10 min.CONCLUSION SFD method has been successfully utilized to prepare solid dispersion of tanshinoneⅡA with enhanced dissolution rate than that of the raw material,which is a prerequisite for increasing its oral bioavailability in vivo.