闹羊花素Ⅲ体外经皮渗透特性研究  

Percutaneous Permeation Characteristics Research of Rhodojaponin Ⅲ

作　　者：杨清云 刘敏臣 羊健 孙水根 张继全[1] 冯怡[1] YANG Qing-yun;LIU Min-chen;YANG Jian;SUN Shui-gen;ZHANG Ji-quan;FENG Yi(Engineering Research Center of Modern Preparation Technology of TCM of Ministry of Education,Shanghai University of Traditional Chinese Medicine,Shanghai 201203,China)

机构地区：[1]上海中医药大学中药现代化制剂技术教育部工程研究中心,上海201203

出　　处：《中国药学杂志》2022年第20期1750-1755,共6页Chinese Pharmaceutical Journal

基　　金：上海市科委支撑项目资助(14401901400)。

摘　　要：目的研究闹羊花素Ⅲ(rhodojaponin Ⅲ,RJ-Ⅲ)的体外经皮渗透特性。方法利用摇瓶法、皮肤孵育法、Franz扩散池法和胶带剥离法,分别考察RJ-Ⅲ的油水分配系数、RJ-Ⅲ在皮肤中的稳定性、体外经皮渗透参数和不同层次离体皮肤中的储留量。结果RJ-Ⅲ的油水分配系数为(0.98±0.02);RJ-Ⅲ在皮肤匀浆液中孵化24 h,RSD值为3.98%;离体透皮实验表明在小鼠皮肤、大鼠的活性表皮与皮肤上,RJ-Ⅲ的稳态透皮速率分别是(5.05±0.28)(3.62±0.30)(1.04±0.10)μg·cm^(-2)·h^(-1),经皮渗透系数分别为7.3×10^(-3)、5.2×10^(-3)、1.4×10^(-3) cm·h^(-1);皮肤储留实验表明,与角质层和活性表皮相比,RJ-Ⅲ更多的存在于接收室。结论RJ-Ⅲ具有良好的经皮稳定性和适宜的经皮渗透特性,为RJ-Ⅲ经皮给药制剂的开发提供理论基础和实验依据。OBJECTIVE To study the in vitro percutaneous permeation properties of rhodojaponinⅢ(RJ-Ⅲ).METHODS Bottle-shaking method,skin incubation method,in vitro diffusion cell method,and tape stripping method were used to determine the relevant parameters of RJ-Ⅲsuch as oil-water partition coefficient,stability in the skin,percutaneous penetration properties,and the retention amount in different layers of the skin.RESULTS The oil-water partition coefficient of RJ-Ⅲwas(0.98±0.02).The RSD of RJ-Ⅲconcentration was 3.98%,when RJ-Ⅲwas incubated in the skin homogenates for 24 h.Then the in vitro percutaneous penetration parameters of RJ-Ⅲwere investigated in mice skin,rat active epidermis and rat skin.The experiments showed that the steady penetration rate of RJ-Ⅲwas(5.05±0.28),(3.62±0.30),(1.04±0.10)μg·cm^(-2)·h^(-1),the permeability coefficient of RJ-Ⅲwas 7.3×10^(-3),5.2×10^(-3),1.4×10^(-3) cm·h^(-1),respectively.In terms of skin storage,RJ-Ⅲwas more retention in the receiving compartment than in the stratum corneum and active epidermis.CONCLUSION RJ-Ⅲpossesses appropriate good percutaneous stability and suitable percutaneous permeability properties,which provides a theoretical and experimental basis for the development of percutaneous drug administration preparations for RJ-Ⅲ.

关 键 词：闹羊花素Ⅲ 油水分配系数 经皮渗透特性 稳定性 皮肤储留 

分 类 号：R917[医药卫生—药物分析学] R944[医药卫生—药学]