目的 比较丁桂活络膏与其改良剂型丁桂凝胶膏剂的体外释放及透皮特性。方法 分别采用微孔滤膜或Strat-M膜及改进的Franz扩散池进行体外释放及透皮试验, 用HPLC法定量分析制剂中君药羌活的有效成分羌活醇的量, 测定2种剂型的体外释放度、透皮量及透皮率。结果 丁桂凝胶膏剂的透皮方程为L_n=9.208 t－18.50, r=0.948, 体外累积释放度、透皮量、透皮率分别为85.34%、0.661 8 mg/g、65.67%;丁桂活络膏的透皮方程为L_n=4.285 t－6.704, r=0.977, 体外累积释放度、透皮量、透皮率分别为67.87%、0.181 6 mg/g、31.35%。结论 丁桂凝胶膏剂的体外释放度、透皮量及透皮率均优于丁桂活络膏, 透皮特性明显优于原剂型, 且凝胶膏剂不易过敏, 贴敷方便。

Objective To compare the release and transdermal behavior in vitro between Dinggui Huoluo Rubber Patch (DHRP) and Dinggui Gel Paste (DGP) which is the improved form. Methods Microporous filter membrane or Strat-M membrane and advanced Franz diffusion cell were chosen in the release and transdermal experiment in vitro. The content of notopterol, the active component of the key herb Notopterygium incisum in the preparation, was quantitatively determined by HPLC method to determine the release rate, penetration quantity, and penetration rate of the two forms. Results The penetration formula of DGP was L_n = 9.208 t－18.50, r = 0.948. The in vitro cumulative release rate, penetration quantity, and penetration rate were respectively 85.34%, 0.661 8 mg/g, and 65.67%. The penetration formula of DHRP was L_n = 4.285 t－6.704, r = 0.977. The in vitro cumulative release rate, penetration quantity, and penetration rate were respectively 67.87%, 0.181 6 mg/g, and 31.35%. Conclusion The transdermal behavior of DGP is obviously better than that of DHRP while its quantity and the rate of penetration and release are all better than those of rubber patch. Meanwhile the gel paste is less sensitized and more convenient to use.

国家科技部科研院所技术开发研究专项资金(2012EG145135);四川省科技支撑计划(2011SZ0306)