青藤碱传递体经皮给药的药动学和药效学研究  

Studies on Transdermal Pharmacokinetic and Pharmacodynamics of Sinomenine Transfersomes

作　　者：惠先[1] 徐坤[1] 豆婧婧[1] 陈贵[1] 闫菁华[1] 郝保华[1] 

机构地区：[1]西北大学生命科学院中药系,西安710069

出　　处：《中国药学杂志》2011年第5期374-377,共4页Chinese Pharmaceutical Journal

基　　金：国家重大新药创制科技重大专项(2009ZX09502-019);西北大学研究生创新项目(09YJC36);陕西省教育厅产业培育项目(2010JC20)

摘　　要：目的研究传递体对青藤碱经皮给药的影响。方法通过薄膜分散法制备青藤碱传递体,并测定经皮给药和静脉注射给药2种给药方式下动物血药浓度和脑组织中药物的含量,以及不同给药方式下小鼠镇静镇痛和抗炎镇痛作用效果的变化,考察传递体对青藤碱在体内吸收、分布以及它对青藤碱止痛效果的影响。结果经皮给药传递体能提高青藤碱的透过量,显著升高血液和脑组织中药物的浓度,提高镇痛疗效。静脉注射青藤碱传递体能提高脑组织中的药物含量,增强中枢镇痛作用,但在一定程度上降低血药浓度,影响外周抗炎镇痛效果。结论传递体能改善青藤碱吸收、分布,影响药物的镇痛效果。OBJECTIVE To study the impacts of transfersomes in vivo administration of sinomenine.METHODS The sinomenine transfersomes were prepared by the mothod of membrane-dispersion.The impacts of transfersomes on absorption,distribution and central and peripheral analgesic effect of sinomenine were researched by determining concentrations of sinomenine in blood and brain tissue under intravenous injection and transdermal delivery.RESULTS Permeation dose of transfersomes via transdermal pathway was remarkably improved which significantly increases not only the concentrations of it in blood but also the mount of it in brain tissue,and analgesic effect was improved remarkably.The mount of transfersomes in brain tissue which significantly increases sedation-analgesic effect was increased but to some extent,the concentration of transfersomes in blood the was reduced which lowers peripheral anti-inflammatory and analgesic effect.CONCLUSION Transfersomes was able to notablely improve the absorption,distribution of sinomenine and had an effect on its pharmacodynamics.

关 键 词：青藤碱传递体 经皮给药吸收 分布 

分 类 号：R944[医药卫生—药剂学]