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双氯芬酸二乙胺每日一次透皮凝胶的制剂与评价

Formulation and evaluation of once-a-day transdermal gels of diclofenac diethylamine.

作者信息

Baboota S, Shakeel F, Kohli K

机构信息

Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard, Hamdard University, New Delhi, India.

出版信息

Methods Find Exp Clin Pharmacol. 2006 Mar;28(2):109-14. doi: 10.1358/mf.2006.28.2.977842.

DOI:10.1358/mf.2006.28.2.977842
PMID:16636721
Abstract

The present study was undertaken to prepare and evaluate transdermal gels of diclofenac diethylamine (DDEA) containing penetration enhancers such as olesan oil and dimethyl sulfoxide (DMSO). Transdermal gels were prepared using different polymers such as carbopol-940, polyvinyl alcohol (PVA), hydroxy propyl methyl cellulose-K(4) M, hydroxy propyl cellulose-M, and sodium carboxy methyl cellulose. The formulated gels were subjected to physicochemical studies, in vitro release studies and in vitro skin permeations studies and were evaluated for drug content, viscosity, extrudability, spreadability, and pH. The in vitro release studies of prepared gels were performed using specially designed Fites cell and in vitro skin permeation studies were performed using keshary-chien diffusion cell through rat skin. Selected formulations were evaluated for their antiinflammatory activity using the carrageenan-induced paw edema in rats. The carbopol-940 and PVA gels containing 10% DMSO showed best in vitro skin permeation of DDEA. In vivo study for the selected formulation showed a sustained reduction in inflammation in the carrageenan induced paw edema in rats. The efficacies of carbopol-940 and PVA gels were also compared with that of the marketed Voveran gel,(R) and it was found that carbopol and PVA gels produced better results than the Voveran gel. (c) 2006 Prous Science. All rights reserved.

摘要

本研究旨在制备并评估含有油酸和二甲基亚砜(DMSO)等渗透促进剂的双氯芬酸二乙胺(DDEA)透皮凝胶。使用不同的聚合物如卡波姆-940、聚乙烯醇(PVA)、羟丙基甲基纤维素-K(4)M、羟丙基纤维素-M和羧甲基纤维素钠制备透皮凝胶。对所制备的凝胶进行物理化学研究、体外释放研究和体外皮肤渗透研究,并对其药物含量、粘度、挤出性、铺展性和pH值进行评估。使用专门设计的Fites细胞进行所制备凝胶的体外释放研究,并使用Keshary-Chien扩散池通过大鼠皮肤进行体外皮肤渗透研究。使用角叉菜胶诱导的大鼠足爪肿胀模型评估所选制剂的抗炎活性。含有10% DMSO的卡波姆-940和PVA凝胶显示出最佳的DDEA体外皮肤渗透性。所选制剂的体内研究表明,角叉菜胶诱导的大鼠足爪肿胀炎症持续减轻。还将卡波姆-940和PVA凝胶的疗效与市售的沃韦朗凝胶(Voveran gel)进行比较,发现卡波姆和PVA凝胶的效果优于沃韦朗凝胶。(c)2006年普劳斯科学出版社。保留所有权利。

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