Jain A K, Panchagnula R
Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), Mohali, India.
Methods Find Exp Clin Pharmacol. 2003 Jul-Aug;25(6):413-21. doi: 10.1358/mf.2003.25.6.769645.
The aim of the present study was to investigate the effects of fatty acids on the permeation of tricyclic antidepressants, e.g., imipramine hydrochloride (IMH) and amitriptyline hydrochloride (AMH). Five percent w/v of saturated (lauric acid) and unsaturated (oleic acid, linoleic acid, linolenic acid, trans-elaidic acid and trans-vaccenic acid) fatty acids in an ethanol (EtOH):water (2:1) system were used in this study. Flux and lag-time of tricyclic antidepressants were significantly increased and reduced, respectively, compared with control (p < 0.05). There were no significant differences between the effects of lauric and unsaturated fatty acids, both cis and trans, on the permeation of IMH and AMH (except vaccenic acid in case of IMH). The formation of 'grain boundaries' by straight chain fatty acids (saturated and trans-unsaturated fatty acids) could not be observed by Fourier-transform infrared spectroscopy (FT-IR). However, perturbation or increased bilayer fluidity of Stratum corneum (SC) induced by cis-unsaturated fatty acid was observed by FT-IR.
本研究的目的是探究脂肪酸对三环类抗抑郁药（如盐酸丙咪嗪（IMH）和盐酸阿米替林（AMH））渗透的影响。本研究使用了在乙醇（EtOH）：水（2：1）体系中5%w/v的饱和脂肪酸（月桂酸）和不饱和脂肪酸（油酸、亚油酸、亚麻酸、反式反油酸和反式vaccenic酸）。与对照组相比，三环类抗抑郁药的通量显著增加，滞后时间显著缩短（p<0.05）。月桂酸和不饱和脂肪酸（包括顺式和反式）对IMH和AMH渗透的影响之间没有显著差异（IMH的情况除外，vaccenic酸有差异）。通过傅里叶变换红外光谱（FT-IR）未观察到直链脂肪酸（饱和脂肪酸和反式不饱和脂肪酸）形成“晶界”。然而，通过FT-IR观察到顺式不饱和脂肪酸诱导角质层（SC）的扰动或双层流动性增加。
