丙泊酚乳状注射液体外释放一致性评价

Consistency Evaluation on the Release in vitro of Propofol Injection Emulsion

目的:建立丙泊酚乳状注射液体外释放度的测定方法,并比较与丙泊酚乳状注射液参比制剂在释放介质中的体外释放行为。方法:采用反向透析技术,释放介质为pH 7.4并含30%无水乙醇的磷酸盐缓冲液,转速为100 r·min^-1,温度为37℃,以HPLC法测定丙泊酚的浓度,计算累积释放度,绘制释放曲线,以丙泊酚乳状注射液为受试制剂,以原研制剂(得普利麻)为参比制剂,采用差异因子(f1)和相似因子(f2)法评价释放曲线的相似度。结果:丙泊酚乳状注射液与原研制剂在pH 7.4并含30%无水乙醇的磷酸盐缓冲液中释放曲线的f1<5,f2>80,两种制剂体外释放行为相似。结论:本法可用于考察丙泊酚乳状注射液与原研制剂体外释放曲线的相似性,为其生产工艺提供参考。

Objective:To establish a method for determining the release of propofol injection emulsion in vitro and compare the release profile with that of the reference preparation.Methods:The retrodialysis technique was employed,the release medium was pH7.4 phosphate buffer solution containing 30%anhydrous ethanol,the rotation speed was 100 r·min^-1,and the temperature was 37℃.HPLC was used to determine the concentration of propofol,the cumulative release was calculated,and the release curve was drawn.Propofol injection emulsion was used as the test preparation,and the original preparation(diprivan)was applies as the reference preparation.The difference factor(f1)and similarity factor(f2)were used to evaluate the similarity of release curves.Results:The f1 values between propofol injection emulsion and the original preparation were less than 5,and the f2 values were more than 80 in the release medium,and the release behaviors of the two preparations in vitro were similar.Conclusion:The method can be used to study the similarity of the release curves of propofol injection emulsion and the original preparation in vitro,which provides reference for its preparation process.