蟾酥酒制对蟾蜍甾烯含量变化及透皮吸收的影响  

Content variation and transdermal penetration of bufadienolides due to wine processing of toad venom

作　　者：李丹丹[1] 陈吴越 周昊言 吕翔[1] 周婧[1] 马宏跃[1] 王恒斌 狄留庆[1] 段金廒[1] LI Dan-dan;CHEN Wu-yue;ZHOU Hao-yan;Lü Xiang;ZHOU Jing;MA Hong-yue;WANG Heng-bin;DI Liu-qing;DUAN Jin-ao(School of Pharmacy,Nanjing University of Chinese Medicine,Jiangsu Key Laboratory of High Technology Research for TCM Formulae,Collaborative Innovation Center for Chinese Medicinal Resources Industrialization in Jiangsu Province,Nanjing 210023,China;Leiyunshang Pharmaceutical Group Co.,Ltd.,Suzhou 215009,China)

机构地区：[1]南京中医药大学,江苏省方剂高技术研究重点实验室/江苏省中药资源产业化过程协同创新中心,江苏南京210023 [2]雷允上药业集团有限公司,江苏苏州215009

出　　处：《中成药》2021年第2期424-428,共5页Chinese Traditional Patent Medicine

基　　金：国家自然科学基金(81673563,81274199);江苏省方剂高技术研究重点实验室/江苏省中药资源产业化过程协同创新中心资助项目(FJGJS⁃2015⁃15,ZDXM⁃14);六神丸质量标准化研究(BA2016104,ZYBZH⁃C⁃JS⁃30);江苏省六大人才高峰C类(YY⁃015);江苏省青蓝工程学术带头人项目(2019)。

摘　　要：目的研究酒制前后蟾酥中蟾蜍甾烯的含量变化及对外用透皮吸收的影响。方法样品溶液的分析采用Waters XBridge C18色谱柱(100 mm×4.6 mm,3.5μm);流动相乙腈⁃0.2%磷酸水,梯度洗脱;柱温35℃;体积流量0.7 mL/min;检测波长296 nm。通过体外Franz扩散池法测定酒制前后蟾酥透皮吸收率。结果24批样品中脂蟾毒配基、华蟾酥毒基、蟾毒灵、沙蟾毒精、蟾毒它灵、华蟾毒它灵在酒制前平均质量分数分别为3.20%、3.73%、1.69%、2.48%、1.44%、1.85%;酒制后平均质量分数分别为3.06%、3.63%、1.65%、2.30%、1.41%、1.82%。酒制前6种成分体外透皮吸收率分别为2.65%、2.44%、6.32%、6.01%、3.84%、5.44%;酒制后透皮吸收率分别为2.10%、2.36%、5.83%、4.44%、3.63%、4.73%。结论蟾蜍甾烯类成分经酒制后含量和其透皮吸收比率均有不同程度的降低,其中影响较大成分为沙蟾毒精和脂蟾毒配基。AIM To investigate the effects of wine processing on the content variation of bufadienolides and their transdermal absorption in vitro.METHODS The analysis of sample solution was performed on a 35℃thermostatic Waters XBridge C18 column(100 mm×4.6 mm,3.5μm),with the mobile phase comprising of acetonitrile⁃0.2%phosphoric acid flowing at 0.7 mL/min in a gradient elution manner,and the detection wavelength was set at 296 nm.The transdermal penetration of toad venom before and after wine processing was measured by the Franz diffusion cell method in vitro.RESULTS In twenty⁃four batches of samples,the average mass fractions of resibufogenin,cinobufagin,bufalin,arenobufagin,bufotalin,cinobufotalin before processing were 3.20%,3.73%,1.69%,2.48%,1.44%,1.85%,in contrast to the post processing values of 3.06%,3.63%,1.65%,2.30%,1.41%,1.82%.The transdermal absorption rates of six constituents before processing were 2.65%,2.44%,6.32%,6.01%,3.84%,5.44%,in contrast to the post processing values of 2.10%,2.36%,5.83%,4.44%,3.63%,4.73%.CONCLUSION Wine processing reduces differently the content and the transdermal absorption rate of various bufadienolides,leaving the greatest impact on arenobufagin and resibufogenin.

关 键 词：蟾酥 酒制 蟾蜍甾烯 透皮吸收 

分 类 号：R283.1[医药卫生—中药学]