目的 制备以甘草酸为稳定剂的黄芩苷固体纳米晶体（baicalin solid nanocrystal，BCN-SN），并考察其体外释放特性。方法 采用高速剪切-高压均质法制备黄芩苷纳米混悬剂，并进一步冷冻干燥得BCN-SN，以平均粒径及多分散指数（PDI）为指标采用单因素实验优化处方及工艺参数，对所得BCN-SN进行理化性质表征，并测定其体外溶出度。结果 以甘草酸为稳定剂，甘露醇-甘草酸为冻干保护剂制备的BCN-SN平均粒径为（478.0±6.5）nm，PDI为0.230±0.015。扫描电镜显示BCN-SN呈不规则球形，大小较均匀；差式扫描量热法表明黄芩苷制备成固体纳米晶体后，以无定形状态存在；体外释放结果表明BCN-SN的溶出速率和溶解度显著高于物理混合物。结论 以甘草酸作为天然稳定剂的固体纳米晶体制备方法简便，能显著改善难溶性药物的溶解性，具有广阔的应有前景。

Objective To prepare baicalin solid nanocrystal (BCN-SN) stabilized by glycyrrhizic acid (GA) and determine its in vitro release characteristics. Methods The high-speed shearing-high pressure homogenization technology was adopted in the preparation of BCN nanosuspension, and then BCN nanosuspension was solidified into BCN-SN by freeze-drying. The formula and process of BCN-SN were optimized by the single factor experiment with average particle size and polydispersity index (PDI) as indicator. BCN-SN were prepared under the optimal conditions and characterized for crystal-linity and particle size. In vitro release of BCN-SN was also determined. Results The particle size of BCN-SN stabilized by GA and protected by mannitol-GA was (478.0 ±6.5) nm, and the polydispersity index (PDI) was 0.230 ±0.015, respectively. The results of SEM showed that BCN-SN was irregular spherical and DSC showed that BCN-SN was amorphous after being prepared into solid nanocrystal. In the in vitro dissolution test, BCN-SN showed a significantly increased dissolution. Conclusion The method employed to prepare the BCN-SN stabilized by GA is simple and low-cost. BCN-SN can significantly improve the dissolution of BCN, which has a broad application.

R283.6

四川省中医药管理局科研项目（2018YY001）