Faculty of Pharmacy and Drug Applied Research Centre, Tabriz University of Medical Sciences, Tabriz, Iran.
Pharm Dev Technol. 2010 Dec;15(6):619-25. doi: 10.3109/10837450903397610. Epub 2009 Nov 20.
The enhancing effects of routinely used co-solvents, propylene glycol and 2-propanol, anionic and cationic surfactants and a co-surfactant with different concentrations were evaluated on the skin permeation of Finasteride. In vitro permeation experiments with rat skin revealed that the solvent mixture is a very important factor in the penetration of Finasteride through the skin. Unexpectedly, cationic and anionic surfactants in various concentrations did not show any enhancement effect on drug transdermal absorption but co-surfactant Transcutol P increased skin penetration of Finastride significantly. Transcutol P with 0.25% and 1% showed the best enhancement in the initial and final sampling time, respectively. Transcutol P in a concentration of 0.25% increased skin absorption of the drug nearly 3.6 times in the first 15 min. The highest enhancement ratio (ER) was gained in the presence of 1% Transcutol P (ER = 5.98). In this study, among the different topical Finastride formulations, Transcutol P 1% in combination with water, propylene glycol and 2-propanol (30, 10, and 60) showed the highest enhancement ratio.
评估了常规使用的共溶剂丙二醇和 2-丙醇、阴离子和阳离子表面活性剂以及不同浓度的共表面活性剂对非那雄胺皮肤渗透的增强作用。通过大鼠皮肤进行的体外渗透实验表明,溶剂混合物是非那雄胺通过皮肤渗透的一个非常重要的因素。出乎意料的是,不同浓度的阳离子和阴离子表面活性剂对药物经皮吸收没有任何增强作用,但共表面活性剂 Transcutol P 显著增加了非那雄胺的皮肤渗透。0.25%和 1%的 Transcutol P 在初始和最终采样时间分别显示出最佳的增强效果。在最初的 15 分钟内,浓度为 0.25%的 Transcutol P 使药物的皮肤吸收率增加了近 3.6 倍。在 1% Transcutol P 的存在下获得了最高的增强比(ER)(ER=5.98)。在这项研究中,在不同的局部非那雄胺制剂中,Transcutol P 1%与水、丙二醇和 2-丙醇(30、10 和 60)的组合显示出最高的增强比。