奥昔布宁透皮贴剂的制备及其体外透皮性研究

目的：制备奥昔布宁透皮贴剂，并对其体外透皮性进行研究。方法：以奥昔布宁为主药，聚丙烯酸树脂E100为辅料，制备奥昔布宁透皮贴剂。采用高效液相色谱法，比较不同渗透促进剂（3％、5％氮酮，5％、10％、15％三醋酸甘油酯，5％、10％肉豆蔻酸异丙酯）对奥昔布宁透皮贴剂的稳态透皮速率（z）的影响，选出最佳渗透促进剂；采用正交试验法，以上和初黏力、持黏力为指标．考察增塑剂癸二酸二丁酯、交联剂丁二酸用量和载药量对贴剂透皮性的影响，优化最佳处方。结果：最佳渗透促进剂为15％三醋酸甘油酯；最优处方为增塑剂25％、交联剂6％、载药量25％；制备的奥昔布宁透皮贴剂的体外为6．24gg／（cm2·h），初黏力为22号钢珠，持黏力为81min。结论：制备的奥昔布宁透皮贴剂具有良好的透皮性。

Preparation of Oxybutynin Transdermal Patch and Its Percutaneous Permeability in vitro

OBJECTIVE： To prepare Oxybutynin transdermal patch, and to study percutaneous permeability in vitro of it. METHODS： Oxybutynin transdermal patch was prepared using oxybutynin as main components and Eudragit El00 as excipients. The effects of different penetration enhancer （3% and 5% azone, 5% , 10% and 15% triacetin, 5% and 10% isopropyl my- ristate） on steady permeation rate （Js） of Oxybutynin transdermal patch were compared by HPLC, and finally the optimal penetra- tion enhancers were selected. The effects of plasticizer dibutyl sebacate content, crosslinking agent succinic acid content and drug-loading amount on percutaneous permeability of the patch were investigated by orthogonal test using percutaneous permeation rate, initial adhesive ability and persistent adhesive ability as index to optimize the formulation. RESULTS： The optimal permeation enhancer was 15% triacetin. Optimal formulation was as follows： plasticizer of 25%, crosslinking agent of 6% and drug-loading amount of 25%. The ~ of the patch was 6.24 p.g/（cm~.h）, initial and persistent adhesive ability were equal to No. 22 steel ball and 81 min. CONCLUSIONS： Prepared Oxybutynin transdermal patch shows good percutaneous permeability.