目的 制备金丝桃苷固体纳米晶体(hyperoside solid nanocrystal, Hyp-SN), 并考察其体外释放特性。方法 采用高压均质法制备Hyp纳米混悬剂, 并进一步冷冻干燥得Hyp-SN。以平均粒径及多分散度指数(PI)为指标, 通过单因素试验优化处方及制备工艺;对最佳处方及制备工艺所得Hyp-SN进行理化性质表征, 并测定其体外释放特性。结果 以叔丁醇为冻干保护剂制备的Hyp-SN平均粒径为(405.2±14.6)nm, PI为0.25±0.08(n=3);扫描电镜显示Hyp-SN呈不规则棒状, 大小较均匀, X射线衍射图谱表明Hyp制备成纳米混悬剂后, 仍以结晶状态存在;体外释放结果表明Hyp-SN的溶出速率和溶解度显著高于Hyp物理混合物。结论 Hyp-SN制备方法简便, 能显著提高难溶性药物的溶解度和溶出速率, 具有广阔的应用前景。

Objective To prepare the hyperoside solid nanocrystal (Hyp-SN) and to determine the in vitro release. Methods The high pressure homogenization technology was applied to preparing Hyp nanosuspension, and then Hyp-NS was solidificated into Hyp-SN by freeze-drying. The fomulation and process of Hyp-SN were optimized by the single factor experiment. Dried powders were prepared under the optimal condition and characterized for crystallinity and particle size. In vitro dissolution of Hyp-SN was also determined. Results The particle size of Hyp-SN protected by tert-butyl alcohol was (405.2 ± 14.6) nm, as well as the polydispersity index (PI) was 0.25 ± 0.08. The results of SEM showed that Hyp-SN powder was irregular rod and XRD showed Hyp was crystalline in both coarse powder and nanosuspensions. In the in vitro dissolution test, Hyp-SN showed an increased dissolution markedly. Conclusion The method employed to prepare the Hyp-SN is simple and feasible. Hyp-SN could significantly improve the dissolution of Hyp. It has a broad application prospects.

国家新药创制重大专项(2012ZX09J12108-04C);国家教育部留学归国人员科研启动基金(20101561)