目的制备荆芥内酯聚乳酸乙醇酸纳米粒冻干粉末,并探讨其工艺与质量评价标准。方法以外观、色泽、再分散性为指标,优选支架剂的种类和浓度及冻干工艺;并对该冻干粉末的外观、再分散性、pH值、纳米粒的形态、粒径分布、多分散系数、质量分数、包封率及载药量等质量评价指标进行考察。结果10%甘露醇作为支架剂可以较好地防止纳米粒的聚集,优化的冻干工艺为-45℃预冻10 h,升温至-25℃维持5 h,再升温至-5℃维持2 h,再升温至10℃维持2 h,最后升温至30℃维持6 h。冻干粉末的外观和分散性良好,平均pH值为6.25,纳米粒平均粒径为80.2 nm,多分散系数为0.024 8,包封率为52.17%,载药量为28.73%。结论荆芥内酯纳米粒冻干粉末制备工艺简便、重复性好;所选用的质量评价方法适用于该冻干粉末,可有效反映其性质。

Objective To study the preparation technology and quality assay of schizonepetolide polylactic-co-glycolic acid nanoparticles(SCH-PLGA-NP) lyophilized powder.Methods The parameters of lyophilizing process were optimized.In addition,the types,concentration,and lyophilizing technology of supporting agent were tested by shape,color,and re-dispersion as indexes.And the quality assay of SCH-PLGA-NP lyophilized powder,such as shape,re-dispersion,pH value,morphology,diameter,re-dispersion,content,encapsulation efficiency,and drug loading of SCH-PLGA-NP lyophilized powder was investigated.Results The supporting agent of 10% manicol could prevent nanoparticles from aggregating very well.The optimal lyophilizing process was as follow: pre-cooled at-45 ℃ for 10 h,primary drying at-25 ℃ for 5 h,secondary drying at-5 ℃ for 2 h,the third drying at 10 ℃ for 2 h,and the finally drying at 30 ℃ for 6 h.The shape and re-dispersion of SCH-PLGA-NP lyophilized powder were good.The pH value was 6.25,mean diameter and re-dispersion of SCH-PLGA-NP were 80.2 nm and 0.024 8,respectively,the encapsulation efficiency and drug loading of SCH-PLGA-NP lyophilized powder were 52.17% and 28.73%,respectivelyConclusion This best preparation process is reasonable after repetition.The quality assay method above mentioned is simple and suitable to lyophilized powder with good repeatability,which could indicate its advantage.

江苏省高校自然科学研究计划项目(02KJA360001);江苏省研究生创新工程资助项目(xm04-76)