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三种双氯芬酸局部用制剂的皮肤渗透性比较:一项体外研究。

Comparison of skin permeability for three diclofenac topical formulations: an in vitro study.

作者信息

Folzer E, Gonzalez D, Singh R, Derendorf H

机构信息

Department of Pharmaceutics, College of Pharmacy, University of Florida, Gainesville, FL 32610-0495, USA.

出版信息

Pharmazie. 2014 Jan;69(1):27-31.

Abstract

Diclofenac is a hydrophilic non-steroidal anti-inflammatory drug (NSAID) widely used in humans and animals. There are limited published studies evaluating diclofenac's skin permeation following topical administration. The aim of our study was to evaluate and compare the in vitro permeation of three different diclofenac-containing formulations (patch, gel, solution) over 24 hours. These formulations were applied (n = 6 per formulation) to pig skin sandwiched between the two chambers in a static Franz diffusion cell and aliquots from the receptor medium were sampled at pre-defined time points. An HPLC method with UV detection was developed and validated with the aim of characterizing the transepidermal penetration in the in vitro system. Using this assay to determine the permeation parameters, results at 24 hours showed that the Flector patch released the highest drug amount (54.6%), whereas a lower drug amount was delivered with the Voltaren Emulgel (38.2%) and the solution (34.4%). The commercial gel showed the highest flux (39.9 +/- 0.9 microg/cm2/h) and the shortest lag-time (1.97 +/- 0.02 h). Based on these in vitro results using pig skin, the transdermal patch resulted in a long-lasting controlled release of diclofenac, while the gel had the shortest lag-time.

摘要

双氯芬酸是一种亲水性非甾体抗炎药(NSAID),广泛应用于人和动物。关于局部给药后双氯芬酸皮肤渗透的已发表研究有限。我们研究的目的是评估和比较三种不同含双氯芬酸制剂(贴剂、凝胶剂、溶液剂)在24小时内的体外渗透情况。将这些制剂(每种制剂n = 6)应用于夹在静态Franz扩散池两个腔室之间的猪皮上,并在预定义的时间点从接受介质中采集等分试样。开发并验证了一种带有紫外检测的高效液相色谱法,以表征体外系统中的经皮渗透情况。使用该测定法确定渗透参数,24小时时的结果表明,Flector贴剂释放的药物量最高(54.6%),而扶他林乳胶剂(38.2%)和溶液剂(34.4%)释放的药物量较低。市售凝胶剂显示出最高通量(39.9 +/- 0.9微克/平方厘米/小时)和最短滞后时间(1.97 +/- 0.02小时)。基于使用猪皮的这些体外结果,透皮贴剂导致双氯芬酸的长效控释,而凝胶剂的滞后时间最短。

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