盐酸西替利嗪巴布膏剂的药动学和生物利用度研究

摘要

Objective To study the pharmacokinetics and bioavailability of cetirizine (CET) cataplasm.Methods SD rats were divided into CET cataplasm group and CET oral group.The content of CET in the rat plasma and the content in the CET cataplasm were detected using HPLC.Results Pharmacokinetic parameters of CET cataplasm group were as follows:Tmax 2.35 h,Cmax 2.68 μg/mL,AUC 21.01 μg·h/mL,MRT 23.26 h;while the pharmacokinetic parameters of CET oral group were as follows:Tmax1.11 h,Cmax 11.65 μg/mL,AUC 35.62 μg·h/mL,MRT 12.13 h.The relative bioavailability was 30.81%.Conclusion Blood drug concentration of CET cataplasm was stable and lasting,and CET cataplasm has the characteristics of slow release.%目的 研究盐酸西替利嗪巴布膏剂在大鼠体内的药代动力学特征,并与口服给药的药动学进行比较,考察生物利用度.方法 选用SD大鼠,分为巴布膏剂组和口服给药组,采用高效液相色谱法测定血药浓度;并剥取剩余的西替利嗪巴布膏剂,测定剩余药量.结果 西替利嗪巴布膏剂组的Tmax为2.35 h,Cmax为2.68 μg/mL,AUC为21.01 μg·h/mL,MRT为23.26 h;西替利嗪口服组的Tmax为1.11 h,Cmax为11.65 μg/mL,AUC为35.62 μg·h/mL,MRT为12.13 h.扣除巴布膏剂中的剩余药量,按照实际进入皮肤的剂量计算得西替利嗪巴布膏剂相当于片剂的生物利用度为30.81%;不扣除巴布膏剂中的剩余药量,西替利嗪巴布膏剂相当于片剂的生物利用度为14.75%.结论 西替利嗪巴布膏剂的血药浓度平稳而持久,具有缓释的特征.