不同促渗剂对马钱子碱囊泡凝胶体外渗透性能的影响

Effects of Different Penetration Enhancers on in vitro Permeability of Brucine Vesicles Gels

目的:通过药效试验筛选马钱子抗炎镇痛的主要药效成分,优选马钱子碱囊泡凝胶的体外透皮促渗剂。方法:考察不同马钱子提取物对佐剂性关节炎大鼠关节肿胀度和屈关节疼痛的影响,确定抗炎镇痛的关键成分。采用p H梯度法制备马钱子碱囊泡凝胶,利用Franz扩散池进行体外透皮试验,扩散池透皮面积2.8 cm2,接受池体积6.5 m L,磁力搅拌速度500 r·min-1,水浴温度(37±1)℃,接受液为p H 7.4磷酸盐缓冲液,考察不同种类和不同用量促渗剂对该制剂体外渗透性能的影响。结果:马钱子碱是马钱子抗炎镇痛的主要药效成分。不同促渗剂均能促进马钱子碱囊泡凝胶的体外渗透性能,不同促渗剂对马钱子碱体外渗透的作用强弱顺序为氮酮>聚山梨酯-20>油酸聚乙二醇甘油酯>月桂酸聚乙二醇甘油酯>肉豆蔻酸异丙脂>聚甘油脂肪酸酯>乙醇>1-甲基-2-吡咯烷酮>水,不同用量氮酮对马钱子碱的促渗作用强弱为10%>7.5%>5%>3%>4%>2%>1%>0.5%。结论:马钱子碱具有抗炎镇痛作用,加入3%氮酮的马钱子囊泡凝胶体外透皮效果较好。

Objective： To screen main effective composition of anti-inflammatory and analgesic in Strychni Semen by Pharmacodynamics test, to optimize in vitro penetration enhancers of brucine vesicles gels. Method ： Key ingredients of anti-inflammatory and analgesic were determined by investigating effects of in different Strychni Semen extracts on articular swelling degree and flexion joint pain of adjuvants arthritis （AA） rats. Brucine vesicles gels was prepared by pH gradient method, transdermal experiment with Franz diffusion cell was employed to conmpare effects of different penetration enhancers on in vitro permeation of brucine vesicles gels. Result： Brucine was a major efficacy component of anti-inflammatory and analgesic in Strychni Semen. Different penetration enhancers all could promote in vitro permeation of brucine vesicles gels, which was in order of azone 〉 polysorbate-20 〉 oleoyl polyoxyl-6 glycerides 〉 gelucire 44-14 〉 isopropyl myristate 〉 polyglycerol fatty acid esters 〉 ethanol 〉 1-methyl-2-pyrrolidone 〉 water. Conclusion： Brucine has anti-inflammatory and analgesic effect, optimal penetration enhancer of brucine vesicles gels is 3% azone.