乌头碱、人参皂苷Rg1及延胡索乙素经皮渗透及协同促渗探究.docVIP

乌头碱、人参皂苷Rg1及延胡索乙素经皮渗透及协同促渗探究 　 作者：张晴,孙玉明,汪 晴,郝佳佳,李子敬,李明慧 【摘要】 目的 研究乌头碱、人参皂苷Rg1与延胡索乙素的透皮吸收及其相互间经皮渗透的影响。方法 采用Permcell KH-5P型横式扩散池分别进行全皮和去角质层皮肤的体外透皮实验,用高效液相色谱法测定乌头碱、人参皂苷Rg1与延胡索乙素的累积透过量,并计算出它们的经皮渗透动力学参数。测定有效成分的油水分配系数(LogP),考察2种及3种有效成分组合的透皮行为及相互影响。结果 乌头碱、人参皂苷Rg1与延胡索乙素在全皮中的扩散系数分别为123.95、50.32、96.25(×10-10 cm2/s),在活性表皮中的扩散系数分别为539.00、93.60、354.70(×10-10 cm2/s),LogP依次分别为1.66、0.66、0.57。在3种有效成分共存的体系中,三者的累积透过量出现64%～293%不同程度的提高。结论 3种有效成分合用对经皮吸收会产生协同促进作用,其中乌头碱与人参皂苷Rg1间的经皮协同促渗作用最明显。 【关键词】 乌头碱；人参皂苷Rg1；延胡索乙素；油水分配系数；经皮渗透 Abstract：Objective To study percutaneous absorption kinetics and synergistic penetration enhancement of tetrahydropalmatine, aconitine and ginsenoside Rg1. Methods The in vitro intact and stripped skin permeation experiments were carried out by using Permcell KH-5P horizontal proliferation system. The percutaneous kinetic parameters of tetrahydropalmatine, aconitine and ginsenoside Rg1 were determined by HPLC, and the transdermal behaviors of the three active ingredients and interactions of combination were investigated. Result The cumulative amounts in 24 h of intact skin of tetrahydropalmatine, aconitine and ginsenoside Rg1 were 123.95, 50.32, 96.25 (×10-10 cm2/s). The cumulative amounts in 24 h of stripped skin of them were 539.00, 93.60, 354.70 (×10-10 cm2/s). The LogP were 1.66, 0.66 and 0.57 respectively. Each component had cumulated amount permeated of improvement by 64%～293% in coexistence system of three active ingredients. Conclusion The combination of three active ingredients results in a synergistic enhancement effect on percutaneous absorption of every active ingredient, and it is shown that the maximal enhancement effect appears between aconitine and ginsenoside Rg1. Key words：aconitine；ginsenoside Rg1；tetrahydropalmatine；LogP；transdermal permeation 川乌祛寒湿风痹、血痹,三七和营止血、通脉行瘀,行瘀血而敛新血,是活血止痛外用方剂中常用的两种药材,它们经常配伍使用,以达活血散瘀、理气止痛之协同功效,如云南白药中含有川乌和三七等药材,其活血止血、消肿止痛的功效显著[1]。延胡索活血、利气、止痛,也是止痛方剂中常用的中药材,如冰辛巴布剂由延胡索、三七等多种药材组成,对热刺激引起的疼痛抑制作用明显[2]。 与口服给药不同,