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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。
OBJECTIVE To prepare solid dispersion of tanshinone ⅡA by spray freeze drying (SFD) and to improve its dissolution in water. Methods Tanshinone Ⅱ A dissolution as an index, screening of different excipients, and the prepared solid dispersion physical and chemical properties of the evaluation. Results Pharmacokinetics ratio (tanshinone ⅡA-poloxamer 188) was increased by 3 times than that of the original drug by spray freeze-drying under the condition of 1: 9. Most of tanshinone ⅡA was changed from crystal state In the amorphous state, the dissolution of tanshinone IIA is significantly increased, and 70% of the drug can be eluted from the solid dispersion within 10 min. Conclusion Compared with the original drug, the dissolution of tanshinone ⅡA solid dispersion prepared by spray freeze-drying has been greatly improved, which provides the necessary conditions for improving oral bioavailability.