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目的:获取来曲唑的经皮扩散参数,以确定其能否研发成经皮给药新剂型。方法:用4个不同处方制备成的来曲唑霜剂进行离体动物皮肤的主药经皮扩散试验,用HPLC法检测并统计各样品的累计释放量,计算经皮扩散的动力学参数,并用滞留时间法验证、评价这些参数的可信度。结果:来曲唑的Tlag为1.23 h,Jss为4.73×10~(-5)mmol·cm~(-2)·h~(-1),D为1.658×10~6cm~2·h~(-1),Kp为1.35×10~(-6)cm·h~(-1)。结论:来曲唑的皮肤滞留时间较短(小于2h),稳态通量较大,适宜制备成经皮肤给药系统。
Objective: To obtain the letrozole percutaneous diffusion parameters to determine whether it can be developed into a new transdermal dosage form. Methods: Letrozole cream prepared by four different prescriptions was used to test the transdermal drug release of the exfoliated animal skin. The cumulative release of each sample was determined by HPLC. The kinetic parameters of percutaneous diffusion were calculated. And use the retention time method to verify and evaluate the credibility of these parameters. Results: The Tlag of letrozole was 1.23 h, the Jss was 4.73 × 10 -5 mmol · cm -2 · h -1, and the D was 1.658 × 10 ~ 6cm ~ 2 · h ~ (-1) -1), Kp was 1.35 × 10 ~ (-6) cm · h ~ (-1). Conclusion: Letrozole skin retention time is shorter (less than 2h), steady-state flux larger, suitable for the preparation of transdermal delivery system.