Cátedra de Farmacología, Facultad de Ciencias Veterinarias, Universidad Nacional de La Plata, Calle 60 y 118, cc 296 (1900), La Plata, CONICET, Argentina.
Vet J. 2010 Dec;186(3):312-5. doi: 10.1016/j.tvjl.2009.09.010. Epub 2009 Oct 7.
Diclofenac is a hydrophilic non-steroidal anti-inflammatory drug widely used in humans and animals. Previous reports have shown that this compound has low percutaneous absorption in horses. The effect of five penetration enhancers (10% urea, 15% and 20% oleic acid and 5% and 10% d-limonene) on the percutaneous absorption of diclofenac diethylamine through horse skin was evaluated in vitro using Franz-type diffusion cells. All tested penetration enhancers induced a significant increase in diclofenac diethylamine permeation, with limonene showing the highest enhancing effect at the lowest concentration (5%) applied. The presence of the permeation enhancers did not affect lag-time. This is the first in vitro study of the effects of penetration enhancers on transdermal permeation of diclofenac diethylamine across horse skin. The results suggested that urea, limonene and 5% oleic acid were useful for enhancing the transdermal absorption of diclofenac diethylamine and may assist in the development of a transdermal formulation of diclofenac diethylamine for use in horses.
双氯芬酸是一种亲水性非甾体抗炎药，广泛应用于人类和动物。先前的报告表明，该化合物在马中的经皮吸收较低。本研究采用 Franz 型扩散池体外评估了 5 种渗透增强剂（10%尿素、15%和 20%油酸以及 5%和 10%柠檬烯）对双氯芬酸钠二乙胺经马皮渗透的影响。所有测试的渗透增强剂均显著增加了双氯芬酸钠二乙胺的渗透，其中柠檬烯在应用的最低浓度（5%）下表现出最高的增强效果。渗透增强剂的存在并不影响滞后时间。这是首次研究渗透增强剂对双氯芬酸钠二乙胺经马皮透皮渗透的影响的体外研究。结果表明，尿素、柠檬烯和 5%油酸可有效增强双氯芬酸钠二乙胺的经皮吸收，可能有助于开发双氯芬酸钠二乙胺的透皮制剂，用于马。
