正交试验法优化祖师麻凝胶膏组方及其体外透皮特性研究  

Optimization of Zushima Gel Paste by orthogonal test and its trans-dermal characteristics in vitro

作　　者：韩锋 李孟琼 徐明 刘楚红 赖文燕 HAN Feng;LI Meng-qiong;XU Ming;LIU Chu-hong;LAI Wen-yan(Guangzhou Lixin Pharmaceutical Co.,Ltd,,Guangzhou 510535,China)

机构地区：[1]广州市力鑫药业有限公司,广东广州510535

出　　处：《现代药物与临床》2021年第3期447-452,共6页Drugs & Clinic

基　　金：广州市科技计划项目(201902010012)。

摘　　要：目的采用正交试验优化祖师麻凝胶膏的组方,并研究其体外透皮吸收行为。方法以初黏度、膏体强度和释放度为考察指标,综合评分,采用L18(37)正交试验对空白基质辅料的用量进行优化,确定最佳处方组合并进行验证试验。采用改良的Franz扩散池,通过体外透皮试验,采用HPLC法同时测定最佳处方中瑞香苷、瑞香素-8-O-β-D-葡萄糖苷、祖师麻甲素的体外透皮渗透量。结果优选出祖师麻凝胶膏黏合剂最佳组方为卡波姆980、聚维酮K30、二氧化硅、阿拉伯胶、聚维酮K90、明胶、聚乙二醇400比例为8∶3∶4∶12∶8∶10∶8,体外透皮行为符合零级动力学过程。结论采用优选的黏合剂组方制备的凝胶膏剂的黏附性、膏体强度、释药性能等均良好,具有较好的使用舒适度,可作为祖师麻凝胶膏的基础制剂组方使用,并可以为新型凝胶膏剂的开发提供技术参考。Objective To optimize the formulation of Zushima Gel Paste by orthogonal test and study its trans-dermal absorption behavior in vitro. Methods The initial viscosity, paste strength, and release degree were used as indexes, and the dosage of blank matrix excipients was optimized by L18(37) orthogonal test to determine the optimal formulation combination and carry out validation test. The in vitro trans-dermal permeation of daphnetin, daphnetin-8-O-β-D-glucoside, and daphnetin in the optimal formulation was simultaneously determined by HPLC method using a modified Franz diffusion cell. Results The optimum formulation of Zushima Gel Paste was carbomer 980, polyvinyl K30, micronized silica gel, acacacia, polyvinyl K90, gelatin, and polyethylene glycol 400 with proportion of 8∶3∶4∶12∶8∶10∶8. The in vitro transdermal behavior conformed to the Zero-order kinetic process. Conclusion The gel paste prepared with the optimized adhesive formula has good adhesion, ointment strength, and drug release performance, and has good use comfort. It can be used as the basic preparation formula of Zushima Gel Paste, and can provide technical reference for the development of new gel ointment.

关 键 词：祖师麻凝胶膏 组方 正交试验 释放度 瑞香苷 瑞香素-8-O-β-D-葡萄糖苷 祖师麻甲素 体外透皮吸收 

分 类 号：R944.2[医药卫生—药剂学]