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KMID : 0369820100400010033
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Jorunal of Korean Pharmaceutical Sciences
2010 Volume.40 No. 1 p.33 ~ p.38
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Formulation and Evaluation of Transdermal Patch Containing Sibutramine
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Robhash Kusam Subedi
Choi Hu Kyun
Park Young-Joon
Jang Joon-Ho
Kim Jae-Il
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Abstract
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Sibutramine is a serotonin-norepinephrine reuptake inhibitor indicated for the management of obesity in conjunction with a reduced calorie diet. The oral administration of sibutramine is followed by its dose-related side effects. In this study, sibutramine was formulated into drug in adhesive (DIA) patches in an attempt to overcome these problems. The effects of different formulation variables including pressure-sensitive adhesive (PSA), loading amount of drug, thickness of matrix and enhancer on the skin permeation of the drug were evaluated using excised hairless mouse skin. In the acrylic adhesive with carboxyl functional group, low release of sibutramine was observed due to the strong interaction between carboxyl group of adhesive and amine group of sibutramine. The acrylic adhesive without functional group provided good adhesion force and allowed high drug loading. Changing drug load as well as thickness of the matrix was found to alter permeation rate. PK40 and A40, were found to be effective enhancers for sibutramine. The optimized patch contained 20% sibutramine, and 5% A40 as permeation enhancer, in thick Duro- 87-9301 matrix.
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KEYWORD
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Sibutramine, transdermal drug delivery, pressure-sensitive adhesive penetration enhancement, antiobesity drug
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