不同透皮促渗剂对苦豆子凝胶剂中生物碱体外透皮吸收的影响  

Effects of Different Transdermal Enhancers on Percutaneous Absorption of Alkaloids from Sophora alopecuroides Gels

作　　者：李军[1,2] 陈海燕 郝彩琴[1] 冷晓红[1] LI Jun;CHEN Hai-yan;HAO Cai-qin;LENG Xiao-hong(Ningxia Research Center for Development and Utilization of Chinese Medicinal Materials,Ningxia Polytechnic,Yinchuan 750021,China;School of Life Sciences,Ningxia University,Yinchuan 750021,China)

机构地区：[1]宁夏职业技术学院宁夏中药材开发与利用工程技术研究中心,宁夏银川750021 [2]宁夏大学生命科学学院,宁夏银川750021

出　　处：《中国现代中药》2023年第5期1071-1078,共8页Modern Chinese Medicine

基　　金：宁夏回族自治区重点研发计划项目(2020BFG03002)。

摘　　要：目的:研究透皮促渗剂对苦豆子凝胶中槐定碱和苦参碱透皮吸收的影响,筛选最佳透皮促渗剂。方法:以SD大鼠皮肤为渗透屏障,采用Franz扩散池进行体外透皮吸收实验,高效液相色谱法(HPLC)测定槐定碱和苦参碱的含量,计算渗透动力学参数,评价不同促渗剂及联合使用对苦豆子凝胶剂透皮吸收的作用。结果:3种促渗剂单用时,对苦豆子凝胶剂中槐定碱和苦参碱透皮性能较好的为3%氮酮、4%冰片和4%薄荷醇。联合使用时,优选出的较佳复合促渗剂为1%冰片+1%薄荷脑,两者联合使用优于氮酮、冰片、薄荷脑单独使用及其他组合,其槐定碱和苦参碱24 h单位面积累积透过量(Q_(24))可达6.858、7.018 mg·cm^(-2),促渗倍数(ER)可达4.402、3.658,协同作用明显。结论:优选出的复合促渗剂对苦豆子凝胶剂中的槐定碱和苦参碱促渗效果较好,为苦豆子凝胶剂制备工艺及功效研究提供参考。Objective:To investigate the effects of transdermal enhancers on the percutaneous absorption of sophoridine and matrine in Sophora alopecuroides gels and screen out the optimal transdermal enhancer.Methods:With the skin of SD rats as the permeation barrier,the Franz diffusion cell was used for the in vitro percutaneous absorption experiment.The content of sophoridine and matrine was determined by high performance liquid chromatography(HPLC).The permeation kinetic parameters were calculated to evaluate the effects of different transdermal enhancers on the percutaneous absorption of sophoridine and matrine in S.alopecuroides gels.Results:When used alone,4%menthol,4%borneol,and 3%azone showed good performance.The best transdermal enhancer combination was 1%borneol+1%menthol,which outperformed single transdermal enhancers and other combinations.Specifically,this combination showcased the cumulative amounts(Q_(24))of sophoridine and matrine permeated for 24 h being 6.858 and 7.018 mg·cm^(-2) and the enhancement ratios of 4.402 and 3.658,respectively,demonstrating significant synergistic effect.Conclusion:The optimized transdermal enhancer combination has good effects on the penetration of sophoridine and matrine in S.alopecuroides gels.The findings provide a foundation for the following preparation and efficacy study of S.alopecuroides gels.

关 键 词：苦豆子凝胶剂 透皮吸收 槐定碱 苦参碱 促渗剂 高效液相色谱法 

分 类 号：R285[医药卫生—中药学] R286[医药卫生—中医学]