目的研究孟鲁司特钠咀嚼片体外溶出及渗透过程,并建立体内外相关性模型对仿制制剂的生物等效性进行预测。方法采用Macro Flux型药物溶出度与渗透速率测试系统,以饱腹小肠模拟液(p H 5. 0)为介质,分别比较参比制剂和受试制剂的溶出及渗透行为,通过关键质量参数考察药物的释放与吸收过程,预测受试制剂的生物利用度,进而预测制剂间是否生物等效。结果在饱腹小肠模拟液中,孟鲁司特钠咀嚼片受试制剂与参比制剂的溶出行为和渗透速率基本一致,ρmax和AUC0-t无显著性差异,生物利用度约为参比制剂的97%。结论初步预测孟鲁司特钠咀嚼片受试制剂与参比制剂在体内生物等效。
Aim To develop and validate a RP-HPLC method for the analysis of paclitaxel in a solid dispersion. Methods Paclitaxel and the internal standard norethisterone were separated using a Phenomenex ODS 3 column and monitored at a wavelength at 227 nm. The isocratic mobile phase consisting of methanol-acetonitrile-water （40：30：30, V/V） was pumped at a flow-rate of 1.0 mL·min^-1. The dissolution studies were performed according to published studies. Results Under these chromatographic conditions, the calibration curve was linear in the range of 4-40 μg·mL ^-1 with the correlation coefficient of 0.9999. The mean recovery was 98.42 % （RSD = 1.19 %）. At the 60 min time point, the dissolution of paclitaxel from the solid dispersion was nearly 100 %, however, the original form of paclitaxel was about 30 %. Conclusion The method was proven to be specific, accurate and precise for determining the dissolution of paclitaxel from solid dispersion.
