Transdermal delivery of imipramine hydriochloride:: Development and evaluation (in vitro and in vivo) of reservoir gel formulation
Transdermal delivery of imipramine hydriochloride:: Development and evaluation (in vitro and in vivo) of reservoir gel formulation
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DOI：
10.1002/bdd.428
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发表时间：
2005-03-01
影响因子：
2.1
通讯作者：
Panchagnula, R
中科院分区：
文献类型：
--
作者：
Jain, AK;Panchagnula, R
本实验室早期报道的盐酸丙咪嗪（IMH）的体外渗透研究表明，（2.5% w/v）和油酸本研究的主要目的是评价该组合的体内性能;为此，将渗透促进剂与IMH一起掺入羟丙基甲基纤维素的水-醇凝胶中，并用作储库透皮贴剂中的药物基质。IMH凝胶的稳定性研究在40 ℃/75%RH下进行2个月。本研究的结果表明，在40 ℃/75%RH下储存的IMH凝胶在2个月内变成黄褐色，并且在40 ℃/75%RH下凝胶粘度的微小变化对IMH从凝胶中的释放速率没有显著影响（p > 0.05）。使用储库透皮贴剂在大鼠中测试凝胶的体内性能，该贴剂由背衬膜、药物基质和面积为12.5 cm（2）的保留膜组成。IMH的血浆浓度达到3 μ g/ml，并且在组织病理学研究中发现24小时闭塞是安全的。版权所有（c）2004年约翰威利父子有限公司。
The in vitro permeation studies of imipramine; hydrochloride (IMH) reported earlier from our laboratory showed that a combination of menthol (2.5% w/v) and oleic acid (2.5% w/v) worked well in terms of safety and efficacy The main objective of this study was to evaluate the in vivo performance of this combination; in order to do that, penetration enhancers were incorporated in a hydro-alcoholic gel of hydroxypropylmethyl cellulose along with IMH and used as the drug matrix in a reservoir transdermal patch. A stability study of IMH gel was performed at 40 degrees C/75% RH for 2 months. The results of this study indicate that gels of IMH stored at 40 degrees C/75% RH turned yellow brown in 2 months and the small change in viscosity of gel at 40 degrees C/75% RH had an insignificant effect on the release rate of lMH from the gel (p > 0.05). The in vivo performance of the gel was tested in rats using a reservoir transdermal patch, which consisted of a backing membrane, drug matrix and retaining membrane with an area of 12.5 cm(2). Plasma concentrations of 3 mu g/ml of IMH were achieved and in a histopathological study 24 h occlusion was found to be safe. Copyright (c) 2004 John Wiley & Sons, Ltd.