氮酮与薄荷醇联用对5-氟尿嘧啶的促透作用  

Azone combined with menthol has penetration-promoting effect on 5-fluorouracil

作　　者：梁庆 王晖 LIANG Qing;WANG Hui(Guangdong Anjian Pharmaceutical co.LTD,Guangzhou 510224,Guangdong,China;School of Traditional Chinese Medicine,Guangdong Pharmaceutical University,Guangzhou 510006,Guangdong,China)

机构地区：[1]广东安健医药有限公司,广东广州510224 [2]广东药科大学中药学院,广东广州510006

出　　处：《中国临床药理学与治疗学》2020年第7期734-739,共6页Chinese Journal of Clinical Pharmacology and Therapeutics

基　　金：国家自然科学基金资助项目(81072591)。

摘　　要：目的:以5-氟尿嘧啶(5-FU)为模型药物,对氮酮和薄荷醇的促透特性进行比较,并探讨两种促透剂合用时的促透效果。方法:在离体透皮实验装置上进行透皮试验,由浓度计算累积透过量,运用倍量法对氮酮与薄荷醇联用的效果进行评价。结果:浓度为0.25%、0.50%、1.00%、2.00%的氮酮对5-FU均有促透作用,与空白对照组相比,差异具有统计学意义(P<0.01);浓度为0.25%、0.50%、1.00%、2.00%的薄荷醇对5-FU也有明显的促透作用,与空白对照相比,差异具有统计学意义(P<0.01);用倍量法对两种药物联用的作用进行评价分析时,二者联用未显示有协同作用。结论:氮酮和薄荷醇对(5-FU)均有促透作用,但二者以相同浓度合用时,未有明显的协同作用。AIM:To compare the effect of azone and menthol by using the 5-fluorouracil(5-FU)as drug model,and explore the mix effect of the two transdermal enhancers.METHODS:The test acts on the self-made instrument.After the test,calculate the total amount of the drug which has permeate through the skin was calculated and the mixed effect of azone and menthol was estimated by multiple quantity method.RESULTS:Both azone and menthol of concentrations of 0.25%,0.50%,1.00%and 2.00%had significant penetration promoting effect on 5-fluorouracil,which were significantly different from the control group(P<0.01).No synergistic effect was detected when evaluating the combined effect of the two drugs by multiple dose method.CONCLUSION:Both azone and menthol have promotion effect on 5-fluorouracil,but the combined use of the two drugs of same concentration show no synergistic effect.

关 键 词：氮酮 薄荷醇 5-氟尿嘧啶 倍量法 联合应用 透皮吸收 

分 类 号：R965.2[医药卫生—药理学]