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。
Abstract
OBJECTIVE To study the in vitro percutaneous permeation properties of rhodojaponin Ⅲ(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-Ⅲ such 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-Ⅲ was(0.98±0.02). The RSD of RJ-Ⅲ concentration was 3.98%,when RJ-Ⅲ was incubated in the skin homogenates for 24 h.Then the in vitro percutaneous penetration parameters of RJ-Ⅲ were investigated in mice skin, rat active epidermis and rat skin. The experiments showed that the steady penetration rate of RJ-Ⅲ was (5.05±0.28), (3.62±0.30), (1.04±0.10) μg·cm-2·h-1, the permeability coefficient of RJ-Ⅲ was 7.3×10-3, 5.2×10-3, 1.4×10-3 cm·h-1, respectively. In terms of skin storage, RJ-Ⅲ was more retention in the receiving compartment than in the stratum corneum and active epidermis. CONCLUSION RJ-Ⅲ possesses 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
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Key words
rhodojaponin Ⅲ /
oil-water partition coefficient /
percutaneous permeation /
stability /
skin retention
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中图分类号：
R917
R944
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参考文献
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脚注
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基金
上海市科委支撑项目资助(14401901400)
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