Yuan Yue, Li San-ming, Mo Feng-kui, Zhong Da-fang
Laboratory of Drug Metabolism and Pharmacokinetics, Shenyang Pharmaceutical University, Wenhua Road 103, Shenyang 110016, People's Republic of China.
Int J Pharm. 2006 Sep 14;321(1-2):117-23. doi: 10.1016/j.ijpharm.2006.06.021. Epub 2006 Jun 20.
A new oil-in-water microemulsion containing 0.375% meloxicam was developed in order to improve the skin permeability of meloxicam. Among various surfactants and cosurfactants investigated in the microemulsion system, polyoxyethylene sorbitan trioleate (Tween 85) showed excellent solubility and ethanol expressed skin permeation enhancing effect for meloxicam. The microemulsion existence ranges were defined through the construction of the pseudo-ternary phase diagram. The effect of the content of isopropyl myristate (IPM) and the effect of the mass ratio of the surfactant/cosurfactant (Km) on skin permeation of meloxicam were evaluated with excised rat skins. The optimum formulation with the highest skin permeation rate (5.40 microg/cm2/h) consisted of 0.375% meloxicam, 5% IPM, 50% Tween 85/ethanol (1:1) and water.
为提高美洛昔康的皮肤渗透性，研发了一种含0.375%美洛昔康的新型水包油微乳剂。在微乳剂体系中研究的各种表面活性剂和助表面活性剂中，聚氧乙烯山梨醇酐三油酸酯（吐温85）表现出优异的溶解性，乙醇对美洛昔康具有皮肤渗透增强作用。通过构建拟三元相图确定了微乳剂的存在范围。用离体大鼠皮肤评价了肉豆蔻酸异丙酯（IPM）含量和美洛昔康皮肤渗透的表面活性剂/助表面活性剂质量比（Km）的影响。皮肤渗透速率最高（5.40μg/cm²/h）的最佳配方由0.375%美洛昔康、5% IPM、50%吐温85/乙醇（1:1）和水组成。
