三种双氯芬酸外用制剂的皮肤渗透性比较:一项体外研究。

E. Folzer, D. Gonzalez, R. Singh, H. Derendorf
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引用次数: 17

摘要

双氯芬酸是一种广泛应用于人类和动物的亲水性非甾体抗炎药。有有限的已发表的研究评估双氯芬酸外用后的皮肤渗透。我们的研究目的是评估和比较三种不同的双氯芬酸制剂(贴片、凝胶、溶液)在24小时内的体外渗透。在静态Franz扩散池中,将这些配方(每种配方n = 6)应用于夹在两个腔室之间的猪皮中,并在预定的时间点从受体培养基中抽取等分。建立并验证了紫外检测的高效液相色谱法,以表征其在体外体系中的透皮渗透。结果表明,24 h时,Flector贴片释放的药物量最高(54.6%),而volteraren乳凝胶和溶液释放的药物量较低(38.2%)。商品凝胶的释药通量最高(39.9 +/- 0.9 μ g/cm2/h),延迟时间最短(1.97 +/- 0.02 h)。基于猪皮体外实验结果,透皮贴剂具有较长的双氯芬酸控释时间,而凝胶具有最短的延迟时间。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Comparison of skin permeability for three diclofenac topical formulations: an in vitro study.
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.
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