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盐酸丙咪嗪的经皮给药。I. 萜类化合物的作用。

Transdermal drug delivery of imipramine hydrochloride. I. Effect of terpenes.

作者信息

Jain Amit Kumar, Thomas Narisetty Sunil, Panchagnula Ramesh

机构信息

Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), Sector 67, Phase-X, Mohali-160062, Punjab, India.

出版信息

J Control Release. 2002 Feb 19;79(1-3):93-101. doi: 10.1016/s0168-3659(01)00524-7.

Abstract

The objective of this investigation was to study the effect of different terpenes on IMH permeation in EtOH:W (2:1) system. Permeation studies of IMH were carried out with unjacketed Franz diffusion cells through rat skin. The flux of IMH with terpenes was found to be significantly higher than that in control (EtOH:W, 2:1) (P<0.05). Amongst all studied terpenes, menthol, terpineol, cineole and menthone were found to be effective permeation enhancers for IMH. It was found that the contribution of diffusivity in enhanced permeation of IMH was much higher in comparison to partitioning of IMH in skin with terpene treatment. Results of this study were explained with the help of H-bond breaking potential and self-association of terpenes. In order to elucidate the effect of terpenes on stratum corneum barrier FT-IR was used.

摘要

本研究的目的是研究不同萜类化合物对乙醇

水(2:1)体系中吲哚美辛(IMH)渗透的影响。采用无夹套的Franz扩散池通过大鼠皮肤进行吲哚美辛的渗透研究。发现吲哚美辛与萜类化合物一起时的通量显著高于对照组(乙醇:水,2:1)(P<0.05)。在所有研究的萜类化合物中,薄荷醇、松油醇、桉叶油素和薄荷酮被发现是吲哚美辛有效的渗透促进剂。结果发现,与萜类化合物处理后吲哚美辛在皮肤中的分配相比,扩散系数对吲哚美辛渗透增强的贡献要高得多。借助氢键破坏潜力和萜类化合物的自缔合对本研究结果进行了解释。为了阐明萜类化合物对角质层屏障的影响,使用了傅里叶变换红外光谱(FT-IR)。

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