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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 hyperoside solid nanocrystal (Hyp-SN) and investigate its in vitro release characteristics. Methods Hyp nanosuspensions were prepared by high pressure homogenization and further freeze-dried to obtain Hyp-SN. Based on the average particle size and polydispersity index (PI), the formulation and preparation process were optimized by single factor test. The optimum formulation and physicochemical properties of Hyp-SN obtained from the preparation were characterized and their in vitro release characteristics were determined. Results The mean diameter of Hyp-SN prepared with tert-butanol as lyoprotectant was (405.2 ± 14.6) nm and PI was 0.25 ± 0.08 (n = 3). Scanning electron microscopy showed Hyp-SN was irregularly rod- Homogeneous, X-ray diffraction pattern showed that Hyp was still in crystalline state after it was prepared as a nanosuspension. The in vitro release results showed that the dissolution rate and solubility of Hyp-SN were significantly higher than that of Hyp physical mixture. Conclusion The preparation method of Hyp-SN is simple, can significantly improve the solubility and dissolution rate of insoluble drugs, and has broad application prospects.