尼索地平醇质体控释贴剂的体外经皮渗透特性及在大鼠体内药动学的研究  

Study on the transdermal penetration in vitro and pharmacokinetics in rats of Nisoldipine ethosomes controlled-release patches

作　　者：聂阳[1,2] 何盛江 许良葵[2] 黄海潮[2] 汪小根[2] 

机构地区：[1]广东省中药研究所,广东广州510520 [2]广东食品药品职业学院,广东广州510520

出　　处：《华西药学杂志》2015年第6期650-653,共4页West China Journal of Pharmaceutical Sciences

基　　金：广东省医学科研基金项目(编号:B2012063)

摘　　要：目的研究尼索地平醇质体控释贴剂的体外经皮渗透及在大鼠体内的药动学特征。方法采用Franz扩散池法进行体外透皮研究;采用HPLC法测定尼索地平的血药浓度,用3p87软件分析药动学参数。结果贴剂在体外经皮渗透的规律符合零级动力学模型;与口服给药相比,贴剂给药的血药浓度平稳,达峰时间延后,持效时间延长,相对生物利用度为242.32%。结论尼索地平控释贴剂具有显著控释特征,可较长时间维持稳定的血药浓度。OBJECTIVE To study the transdermal penetration in vitro and the pharmaeokineties in rats of Nisoldipine ethosomes controlled - release patches. METHODS Franz diffusion cell was used for the penetration mechanism in vitro. An HPLC method was developed to determine the Nisoldipine blood concentration, and the software 3p87 was used to analyze the pharmaceutical parameters. RESULTS The permeation characteristics of the patch through rats skin in vitro followed Zero - order kinetic characteristics. The pharmacokinetic results showed that the patch could provide steadily sustained blood concentration, prolong the peak time and extend the mean residence time compared with oral administration. The relative bioavailability of the patch was 242.32% versus oral adminis- tration. CONCLUSION The Nisoldipine controlled - release patches exhibit good controlled - release properties and maintain appro- priate blood concentration for a prolonging time.

关 键 词：尼索地平 醇质体 控释贴剂 经皮渗透 释药模式 药动学 生物利用度 高效液相色谱 

分 类 号：R94[医药卫生—药剂学] R917[医药卫生—药学]