土家族常用基质调敷接骨膏粉末体外经皮吸收药动学研究

Percutaneous Absorption in Vitro of Jiegugao Blended and Pasted by Commonly Used Ointment Matrices in Tujia Minority

目的建立紫丁香苷、异嗪皮啶HPLC同步检测方法,考察接骨膏粉末用白醋、蜂蜜和凡士林为基质调敷时的体外透皮吸收特性,探讨土家族常用药膏基质的作用。方法以离体大鼠腹部皮肤为透皮屏障,采用改良Franz扩散池模拟体外透皮吸收实验,用HPLC测定接收液中紫丁香苷、异嗪皮啶的含量,建立经皮吸收方程,计算累积渗透量、渗透速率等相关参数。结果采用Syncronis C18色谱柱(250 mm×4.6 mm,5μm),流动相为乙腈-0.1%磷酸(20∶80),流速1.0 m L/min,检测波长265 nm,紫丁香苷回归方程A=10 686.454 6C+1565.778 8(r=1.000 0),异嗪皮啶回归方程A=12 297.305 4C-5913.729 9(r=0.999 9)。以白醋、蜂蜜和凡士林为基质调敷接骨膏粉末及不添加基质时,紫丁香苷的稳态透皮速率分别为7.549 2、4.580 3、3.890 8、5.378 4μg·cm^(-2)·h^(-1),累积透过百分率分别为25.66%、16.11%、13.73%、18.78%;异嗪皮啶的稳态透皮速率分别为2.536 9、1.941 8、1.178 2、2.293 6μg·cm^(-2)·h^(-1),累积透过百分率分别为47.04%、35.06%、22.11%、41.11%。结论以白醋为基质,有利于促进接骨膏粉末中药效成分的经皮吸收;以蜂蜜和凡士林为基质,会阻滞接骨膏粉末中药效成分的经皮吸收,但可作为缓释基质使用。

Objective To establish a method to simultaneously determine syringing and isofraxidin by HPLC; To investigate the features of percutaneous absorption in vitro of Jiegugao blended and pasted by white vinegar, honey and vaseline; To discuss the mechanism of commonly used ointment matrices in Tujia Minority. Methods Rat abdomen skin in vitro was as transdermal barrier; the modified Franz diffusion pool was used to simulate human skin medication; the content of syringin and isoprofen was determined by HPLC; the percutaneous absorption equation was established and the related parameters, such as cumulative permeation rate and permeation rate, were calculated. Results When using Syncronis C18（250 mm × 4.6 mm, 5 μm） as chromatographic column, acetonitrile-0.1% phosphoric acid as mobile phase, 1.0 m L/min as perfusion speed and 265 nm as determine wavelength, regression equation of syringingwas A=10 686.454 6C＋1565.778 8（r=1.000 0）, regression equation of isofraxidin was A=12 297.305 4C-5913.729 9（r=0.999 9）. Cumulative permeation quantity of syringing in Jiegugao blended and pasted by white vinegar, honey, vaseline and blank were 7.549 2, 4.580 3, 3.890 8 and 5.378 4 μg·cm-2·h-1 respectively and permeation rate were 25.66%, 16.11%, 13.73% and 18.78%. Meanwhile, cumulative permeation quantity of isofraxidin were 2.536 9, 1.941 8, 1.178 2 and 2.293 6 μg·cm-2·h-1 respectively and permeation rate were 47.04%, 35.06%, 22.11% and 41.11%. Conclusion Using white vinegar as the ointment matrix can promote the percutaneous absorption of effective composition in Jiegugao blended. However, it will retard the percutaneous absorption of effective composition in Jiegugao when using honey and vaseline as the ointment matrices, but honey and vaseline can be used as a slow-release matrix.