黄芩素注射用冻干粉针剂的制备  

Preparation of baicalein freeze-dried powder injection

作　　者：张晓博[1] 谷艳玲[1] 张丽男[1] 哈婧[1] 马楠[1] 齐献利 高子彬[1] 

机构地区：[1]河北科技大学化学与制药工程学院,石家庄050018

出　　处：《中国新药杂志》2015年第12期1354-1357,共4页Chinese Journal of New Drugs

基　　金：国家"重大新药创制"科技重大专项(2014ZX09507001)

摘　　要：目的:通过制备卵磷脂/非离子表面活性剂混合胶束,制成黄芩素冻干粉针剂,提高黄芩素在水中的分散程度。方法:建立黄芩素冻干粉针剂药物含量测定的方法,通过单因素实验考察表面活性剂的配比、温度、超声功率对黄芩素在水中分散量的影响以及对赋形剂的种类和用量进行筛选,并对冻干制品的p H值、性状、粒径、复溶情况等进行了考察。结果:优选出制备工艺为:有机相中卵磷脂S75∶聚乙二醇(PEG)十二羟基硬脂酸锂(solutol)=9∶4,1.86%卵磷脂S75为水相,240 W功率下超声1 min,5%甘露醇为冻干保护剂,冷冻干燥制得冻干粉。复溶后平均粒径为(113.3±5.3)nm,透射电镜(TEM)下胶束形态为圆形。结论:黄芩素混合胶束的制备工艺简便,能有效提高黄芩素的分散度,粒径分布理想,制成冻干粉后提高了药物的稳定性,便于保存。Objective：To prepare baicalein freeze-dried powder injection to improve baicalein dispersion in water via lecithin-nonionic surfactant mixed micelles. Methods：The method was established for determining the drug content of baicalein freeze-dried powder injection. An optimized preparation process was obtained by single- factor method which studied the effects of several factors on the dispersion of baicalein in water,including the ratio of surfactants,temperature and ultrasonic power, and screened the type and amount of excipients. The pH value, characteristics,particle size and reconstitution condition of baiealein freeze-dried products were determined. Re- suits：The optimized preparation process was as follows：the ratio of lecithin $75 and solutol in the organic phase was 9：4 ,in which baicalein was dissolved,and the solution was dripped to 1.86% lecithin $75 aqueous phase. The ba- icalein freeze-dried powder injection was obtained when the solution was treated by ultrasound at the power of 240 W for 1 min,and 5% mannitol was selected as lyoprotectant. After reconstitution,the particles showed a round shape with an average particle size of （113. 3 ± 5. 3） nm when observed by transmission electron microscope （TEM）. Conclusion ：The preparation process of baicalein freeze-dried powder injection is simple and convenient, which can significantly enhance the dispersion of baicalein in water with a uniform particle size distribution. The freeze-dried product has good stability which is easy for storage.

关 键 词：黄芩素 卵磷脂 表面活性剂 冻干粉 混合胶束 

分 类 号：R283.6[医药卫生—中药学]