白脉软膏主要成分体外经皮透过性的研究

In vitro transdermal permeation of main compositions in Baimai Ointment

建立白脉软膏透皮接收液中甘草酸铵、甘松新酮、姜黄素的含量测定方法,并对白脉软膏的经皮渗透性和2种促透剂对3种成分透皮吸收的影响进行考察。采用HPLC测定透皮接收液中甘草酸铵、甘松新酮、姜黄素的含量,以立式改良的Franz透皮扩散池,小鼠腹部皮肤(处理与不处理)进行体外透皮实验,优选透皮接收液,考察白脉软膏透皮吸收规律及促透剂的影响。结果表明,3种接收液PG-ET-NS(3∶3∶4),PEG-ET-NS(3∶3∶4),ET-NS(3∶7),以PEG-ET-NS(3∶3∶4)综合溶解能力较好,以其为接收液进行体外透皮实验,24 h甘草酸铵、甘松新酮和姜黄素累计透过量分别为5. 73,18. 99,0. 38μg·cm-2。以QEF和ER为促透性能综合考察指标,甘草酸铵的综合促透性能为3%聚乙二醇≈1. 19倍(3%氮酮)=1. 94倍(空白),甘松新酮的综合促透性能为3%聚乙二醇≈1. 28倍(3%氮酮)=1. 37倍(空白),姜黄素的综合促透性能为3%聚乙二醇≈1. 77倍(3%氮酮)≈3. 42倍(空白),2种促透剂对3种成分的综合促透性能为3%聚乙二醇>3%氮酮>空白。白脉软膏中甘草酸铵、甘松新酮、姜黄素的透皮吸收曲线符合零级方程,表明3种成分的透皮过程与软膏中各成分的浓度无关,且为扩散过程,该实验为软膏类经皮制剂体外透过性的研究提供参考。

To establish a determination method for the contents of ammonium glycyrrhetate,nardosinone,and curcumin in transdermal receptor liquid of Baimai Ointment,and investigate the percutaneous permeability of Baimai Ointment and the effects of two kinds of penetration enhancers on percutaneous absorption of three components.The contents of ammonium glycyrrhetate,nardosinone,and curcumin in transdermal receptor liquid were determined by high pressure liquid chromatography(HPLC).The vertical modified Franz diffusion cell was used to perform a transdermal experiment in vitro with the abdominal skin of mice(treated and untreated).The transdermal receptor liquid was preferably used to investigate the transdermal absorption rule of the Baimai Ointment and the effect of the penetration enhancer.The results showed that the comprehensive solubility of PEG-ET-NS(3∶3∶4)was best among three types of receptor liquid PG-ET-NS(3∶3∶4),PEG-ET-NS(3∶3∶4),ET-NS(3∶7).PEG-ET-NS was used as the receptor liquid for in vitro transdermal experiments.The cumulative permeation area of ammonium glycyrrhetate,nardosinone and curcumin within 24 h was 5.73,18.99,0.38μg·cm-2respectively.Taking QEFand ER as comprehensive evaluation indicators of permeation performance,the comprehensive penetration-promoting performance of ammonium glycyrrhizinate:3%PEG 400-ethanol-normal saline≈1.19 times(3%azone)=1.94 times(blank);comprehensive penetration-promoting performance of nardosinone:3%PEG 400-ethanol-normal saline≈1.28 times(3%azone)=1.37 times(blank);the comprehensive penetration performance of curcumin:3%PEG 400-ethanol-normal saline≈1.77 times(3%azone)≈3.42 times(blank).The comprehensive penetration enhancement properties of the two penetration enhancers were as follows:3%PEG 400-ethanol-normal saline>3%azone>blank.The transdermal absorption curve of ammonium glycyrrhetate,nardosinone and curcumin in Baimai Ointment were consistent with the zero-order equation,indicating that the transdermal absorption process was irrelevant to the concentration of three components,and its was a diffusion process.This experiment provides reference for the study of ointment transdermal preparations.