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Transdermal delivery of imipramine hydrochloride: Development and evaluation ( in vitro and in vivo ) of reservoir gel formulation
Author(s) -
Jain Amit Kumar,
Panchagnula Ramesh
Publication year - 2005
Publication title -
biopharmaceutics and drug disposition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.419
H-Index - 58
eISSN - 1099-081X
pISSN - 0142-2782
DOI - 10.1002/bdd.428
Subject(s) - transdermal , chemistry , chromatography , in vivo , permeation , pharmacology , oleic acid , membrane , medicine , biochemistry , microbiology and biotechnology , biology
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°C/75% RH for 2 months. The results of this study indicate that gels of IMH stored at 40°C/75% RH turned yellow brown in 2 months and the small change in viscosity of gel at 40°C/75% RH had an insignificant effect on the release rate of IMH 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 µg/ml of IMH were achieved and in a histopathological study 24 h occlusion was found to be safe. Copyright © 2004 John Wiley & Sons, Ltd.