采用溶出-渗透分析模型预测盐酸环丙沙星片的生物等效性

Prediction of Bioequivalence of Ciprofloxacin Hydrochloride Tablets by Applying Dissolubility-permeability Analysis Model

目的 建立体内外相关分析模型研究盐酸环丙沙星片体外溶出及渗透过程,对仿制制剂与参比制剂的生物等效性进行预测,并与临床体内生物等效性研究结果进行比较。方法 采用MacroFlux型药物生物等效性预测系统,以空腹肠模拟液为介质,分别比较参比制剂和仿制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和吸收过程,评估预测仿制制剂与参比制剂是否生物等效。结果 在空腹肠模拟液中,盐酸环丙沙星片仿制制剂与参比制剂的溶出行为和渗透速率基本一致,与临床体内生物等效性研究结果吻合,仿制制剂与参比制剂生物等效。结论 建立体内外相关分析模型快速而有效地预测了仿制制剂与参比制剂的生物等效性。

OBJECTIVE To study the dissolution and permeation process of ciprofloxacin hydrochloride tablets in vitro,establish a three-dimensional and internal correlation analysis model,aiming to predict the bioequivalence of generic products and reference preparations,and to compare the predicted results with the bioequivalence results in vivo.METHODS The Macro Flux drug bioequivalence prediction system was applied,with the simulated intestinal fluid(on an empty stomach) as the medium.The bioequivalence of original drug and generic products based on the dissolubility and permeability were compared respectively by investigating the key quality parameters from the process of drug release and absorption.RESULTS At the above medium,the dissolution behavior and penetration rate of generic product and reference of ciprofloxacin hydrochloride tablets were similar,and the predicted results matched well with the bioequivalence results in vivo.CONCLUSION A three-dimensional and internal correlation analysis model is established to predict the bioequivalence of generic products and reference preparations quickly and effectively.