Department of Analytical Chemistry, University of Barcelona, Martí i Franquès 1-11, 08028 Barcelona, Spain.
J Pharm Sci. 2011 Mar;100(3):992-1000. doi: 10.1002/jps.22346. Epub 2010 Sep 16.
This paper describes the preparation and characterization of transdermal patches impregnated with naproxen. A mixture of ethylene vinyl acetate and Eudragit E100 (80:20, w/w) is used as a polymeric matrix to obtain a thin membrane to be impregnated. Drug impregnation is carried out under pressurized CO(2) as a processing medium according to a two-step procedure. The patch is first soaked at 1000 psi and 22 °C for 2 h, and then foamed as a result of the rapid release of CO(2) pressure in order to increase the porosity of the surface. Subsequently, the naproxen solution is placed in contact with the membrane and then soaked in CO(2) at 450 psi and 37 °C for 2.5 h to enhance the mass transfer of drug into the polymer matrix. The characterization of the resulting samples by liquid chromatography, microscopy, and calorimetry provides information on naproxen content and distribution. Patches synthesized in this way are loaded with about 1% naproxen. The drug release and diffusion process through a membrane have been studied chromatographically using a Franz diffusion cell. Results have shown that a sustained delivery for more than 24 h is obtained.
本文描述了载有萘普生的经皮贴剂的制备和特性。乙烯-醋酸乙烯酯和 Eudragit E100（80:20，w/w）的混合物用作聚合物基质，以获得要浸渍的薄膜。根据两步程序，在加压 CO(2) 作为加工介质中进行药物浸渍。首先将贴剂在 1000 psi 和 22°C 下浸泡 2 小时，然后由于 CO(2) 压力的快速释放而发泡，以增加表面的多孔性。随后，将萘普生溶液与膜接触，然后在 450 psi 和 37°C 下在 CO(2) 中浸泡 2.5 小时，以增强药物向聚合物基质中的传质。通过液相色谱、显微镜和量热法对所得样品进行的特性分析提供了有关萘普生含量和分布的信息。以这种方式合成的贴剂载有约 1%的萘普生。使用 Franz 扩散池通过色谱法研究了药物通过膜的释放和扩散过程。结果表明，获得了超过 24 小时的持续释放。
