基于UPLC-MS/MS研究去甲乌药碱体外透皮吸收规律

天然产物研究与开发 ›› 2022, Vol. 34 ›› Issue (增刊2): 81-86.

基于UPLC-MS/MS研究去甲乌药碱体外透皮吸收规律

郭承军1*，张宁2，张晓丽1，迟名锋1

1山东省运动康复研究中心，济南250101；2莱西市中医医院，青岛266699

出版日期:2022-12-07 发布日期:2022-12-07
基金资助:
山东省体育局科研攻关项目（鲁体科计字［2019］52号）

Study on the in vitro transdermal absorption of higenamine by UPLC-MS/MS

GUO Cheng-jun1*,ZHANG Ning2,ZHANG Xiao-li1,CHI Ming-feng1

1Shandong Sports Rehabilitation Research Center,Jinan 250101,China;2Laixi Hospital of Traditional Chinese Medicine,Qingdao 266699,China

Online:2022-12-07 Published:2022-12-07

摘要/Abstract

摘要：

通过研究去甲乌药碱经皮吸收的规律，一方面为去甲乌药碱外用强心制剂开发提供数据支持，另一方面为运动员的用药安全提供实验依据，杜绝因外用中药造成兴奋剂违规事件的发生。首先以HG的经皮透过率为考察指标，对溶剂含醇量、接收液pH、促透剂浓度进行了单因素实验，并通过正交试验获得供给液的最佳工艺参数，应用UPLC-MS/MS测得HG最大经皮透过量，从而得到最大经皮透过率。结果显示，HG经皮给药的供给液最佳工艺参数为溶剂10%乙醇水溶液，pH 7.0，促透剂氮酮浓度为0.8%，HG最大经皮透过率为(21.60±5.70)%。本文首次系统研究了HG透皮吸收规律，并测定了48 h最大透皮吸收率，考察了最佳工艺参数，为含HG的强心外用药物制剂开发提供初步的数据参考，为运动员安全使用外敷中药提供数据支持。

关键词: 去甲乌药碱, 超高效液相质谱联用, 反兴奋剂, 透皮吸收, 强心成分

Abstract:

To study the law of transdermal absorption of higenamine (HG),on the one hand,it provides data support for the development of the cardiotonic preparations for external use of HG,on the other hand,it provides an experimental basis for the drug safety of athletes,and eliminate the occurrence of doping violations caused by transdermal use of traditional Chinese medicine.Firstly,the transdermal penetration rate of HG was used as the index,and single-factor experiments were carried out on the alcohol concentration of the solution,pH of extract,and concentration of penetration enhancer.The best process parameters of the supply solution were obtained from the orthogonal test results.The maximum transdermal absorption rate of HG was determined by UPLC-MS/MS.The results showed that the optimum process parameters were solvent of 10% ethanol solution in water,pH 7.0 and 0.8% concentration of penetration enhancer azone.The maximum transdermal absorption rate of HG was (21.60±5.70)%.In this paper,the 48-hour maximum transdermal transmission rate of HG was systematically studied for the first time,and the optimal process parameters were determined,which provides a reference for the development of HG-containing cardiotonic drug preparations,provides data support for the safe use of externally applied traditional Chinese medicine by athletes.

Key words: higenamine, UPLC-MS/MS, anti-doping, transdermal absorption, cardiotonic component

中图分类号: R285.5

郭承军, 张宁, 张晓丽, 迟名锋. 基于UPLC-MS/MS研究去甲乌药碱体外透皮吸收规律[J]. 天然产物研究与开发, 2022, 34(增刊2): 81-86.

GUO Cheng-jun, ZHANG Ning, ZHANG Xiao-li, CHI Ming-feng. Study on the in vitro transdermal absorption of higenamine by UPLC-MS/MS[J]. NATURAL PRODUCT RESEARCH AND DEVELOPMENT, 2022, 34(增刊2): 81-86.