雷公藤配伍白芍对雷公藤提取物透皮吸收的影响

目的:考察雷公藤与白芍配伍后对雷公藤甲素和2种生物碱类成分(雷公藤吉碱、雷公藤次碱)透皮吸收的影响,从经皮转运的角度探讨雷公藤与白芍配伍减毒的机制。方法:采用改良Franz扩散池,以小鼠离体腹部皮肤为透皮屏障,以20%乙醇生理盐水为接收介质,通过HPLC测定接收液中雷公藤甲素(流动相乙腈-水梯度洗脱,检测波长220 nm)和雷公藤吉碱、雷公藤次碱[流动相乙腈-0.1%磷酸水溶液(57∶43),检测波长230 nm]的含量,计算其累积渗透量和稳态透皮速率等渗透动力学参数。结果:与雷公藤乳膏相比,雷公藤-白芍配伍乳膏均能降低雷公藤吉碱、雷公藤次碱的累积通过量,但对雷公藤甲素的累积透过量无影响;其中雷公藤-白芍以比例1∶2和1∶3配伍的乳膏中雷公藤吉碱和雷公藤次碱的24 h累积透过量呈明显的降低趋势。结论:雷公藤与白芍配伍经皮给药能降低毒性成分的透过量,同时不影响主要活性物质雷公藤甲素的透过量,从而达到了减毒增效的作用。

Effect of Tripterygii Radix et Rhizoma Combined with Paeoniae Radix Alba on Transdermal Absorption of Tripterygii Radix et Rhizoma Extract

Objective:To investigate the effect of compatibility of Tripterygii Radix et Rhizoma and Paeoniae Radix Alba on the percutaneous absorption of triptolide and two alkaloids(wilforgine and wilforine),to investigate the mechanism of reducing toxicity of Tripterygii Radix et Rhizoma combined with Paeoniae Radix Alba from the perspective of transdermal transport. Method:The modified Franz diffusion cell was employed,taking in vitro abdominal skin of mice as transdermal barrier,with 20% ethanol physiological saline as receiving medium,the contents of triptolide(mobile phase of acetonitrile-water for gradient elution,detection wavelength at 220 nm),wilforgine and wilforine[mobile phase of acetonitrile-0.1% phosphoric acid(57:43),detection wavelength at 230 nm]in the receiving liquid was determined by HPLC,then the cumulative permeation quantity,steady transdermal rate and other penetration kinetic parameters were calculated. Result:Compared with Tripterygii Radix et Rhizoma cream,compatibility of Paeoniae Radix Alba and Tripterygii Radix et Rhizoma cream group could reduce cumulative penetration amounts of wilforgine and wilforine;among them,cumulative penetration amounts at 24 h of wilforgine and wilforine in cream with compatibility of Tripterygii Radix et Rhizoma and Paeoniae Radix Alba in 1:2 and 1:3 showed a significant decreasing trend;but the cumulative penetration amount of triptolide without the influence of compatibility. Conclusion:The compatibility of Tripterygii Radix et Rhizoma and Paeoniae Radix Alba can decrease the permeation of toxic components,and do not affect the permeability of triptolide,which is the main active substance of Tripterygii Radix et Rhizoma,so as to achieve the effect of reducing toxicity and increasing efficiency.