Mutalik Srinivas, Udupa Nayanabhirama, Kumar Sharath, Agarwal Sunil, Subramanian Ganesh, Ranjith Averineni K
Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal-576 104, Karnataka, India.
Life Sci. 2006 Sep 13;79(16):1568-77. doi: 10.1016/j.lfs.2006.05.002. Epub 2006 May 6.
The aim of the present investigation was to prepare glipizide matrix transdermal systems using the combinations of ethyl cellulose/polyvinylpyrrolidone and Eudragit RL-100/Eudragit RS-100. The systems were evaluated for various in vitro (drug content, drug permeation, scanning electron microscopy and drug-polymer interactions) and in vivo (acute and long-term hypoglycemic activity, biochemical and histopathological studies, skin irritation and pharmacokinetic studies in mice) parameters. Drug content of the patches was found to be more than 98%. Variations in drug permeation profiles were observed among various formulations. The scanning electron microscopy of the patches showed the formation of pores on the surface after in vitro permeation studies. The drug-polymer interaction results suggested no interaction between drug and polymers. The in vivo results revealed that the patches successfully prevented the severe hypoglycemia in the initial hours and they were also effective on chronic application. The transdermal route exhibited negligible skin irritation and produced better improvement with all the tested in vivo parameters compared to oral administration.
本研究的目的是使用乙基纤维素/聚乙烯吡咯烷酮以及丙烯酸树脂RL - 100/丙烯酸树脂RS - 100的组合制备格列吡嗪基质透皮给药系统。对这些系统进行了各种体外（药物含量、药物渗透、扫描电子显微镜和药物 - 聚合物相互作用）和体内（急性和长期降血糖活性、生化和组织病理学研究、皮肤刺激性以及小鼠体内药代动力学研究）参数的评估。发现贴剂的药物含量超过98%。在各种制剂中观察到药物渗透曲线的变化。贴剂的扫描电子显微镜显示在体外渗透研究后表面形成了孔隙。药物 - 聚合物相互作用结果表明药物与聚合物之间没有相互作用。体内结果表明，贴剂在最初几个小时成功预防了严重低血糖，并且在长期应用时也有效。与口服给药相比，透皮途径表现出可忽略不计的皮肤刺激性，并且在所有测试体内参数方面产生了更好的改善。
