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目的优化羟丙基-γ-环糊精(HP-γ-CD)包合黄芩素的工艺条件。方法采用冷冻干燥法,以包合物的得率、包封率和载药率为考察指标,通过L9(3)4正交设计优选黄芩素(Ba)与HP-γ-CD摩尔比、包合温度、包合时间、包合溶剂比(水∶无水乙醇),综合评价确定最佳制备工艺;采用X射线衍射分析和差示扫描量热分析验证包合物。结果最优包合条件:Ba与HP-γ-CD摩尔比为1∶3,温度45℃,包合时间4 h,包合溶剂比(水∶无水乙醇)2∶3;采用最优包合条件制备的Ba-HP-γ-CD包合物得率为93.97%,包封率为95.96%,载药率为5.20%,其粉末经鉴定已形成包合物;Ba-HP-γ-CD包合物能够显著提高Ba的溶解度。结论优选的包合工艺合理可行,为黄芩素制备成各种剂型奠定了良好基础。
Objective To optimize the process conditions of baicalein inclusion by HP-γ-CD. Methods The freeze-drying method was used to determine the entrapment yield, entrapment efficiency and drug loading rate. The orthogonal design of L9 (3) 4 was used to optimize the molar ratio of baicalein (Ba) to HP-γ-CD, The optimum preparation conditions were determined by comprehensive evaluation of the temperature, inclusion temperature, inclusion ratio (water: ethanol), and the inclusion complex was confirmed by X-ray diffraction and differential scanning calorimetry. Results The optimum inclusion conditions were as follows: the molar ratio of Ba to HP-γ-CD was 1: 3, the temperature was 45 ℃, the inclusion time was 4 h, the inclusion ratio of solvent to water was 2: 3, The yield of Ba-HP-γ-CD inclusion complex was 93.97%, the encapsulation efficiency was 95.96% and the drug loading rate was 5.20%. The Ba-HP-γ- CD inclusion can significantly improve the solubility of Ba. Conclusion The optimal inclusion process is reasonable and feasible, which has laid a good foundation for the preparation of various dosage forms of baicalein.