首页|黄芩不同炮制品黄酮类成分的整合药动学研究

黄芩不同炮制品黄酮类成分的整合药动学研究

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目的:比较黄芩炮制品中8种黄酮类成分在大鼠体内含量的差异,探明黄芩不同炮制品的药动学行为的差异,为其炮制原理的阐明提供科学依据.方法:选取20只SD大鼠随机分为空白组、生黄芩、酒黄芩和黄芩炭4组,每组5只,灌胃给药.以山柰素为内标,采用超高效液相色谱-三重四级杆串联质谱法(UPLC-QQQ-MS/MS)测定不同时间点大鼠血清中黄芩苷、5,7,2',5'-四羟基-8,6'-二甲氧基黄酮(HQ-6)、汉黄芩苷、黄芩素、汉黄芩素、白杨素、5,6-二羟基-7,8,2',6'-四甲氧基黄酮(HQ-2)、千层纸素-A等的浓度,利用各成分药-时曲线下面积(AUC0→∞)百分比作为自定义权重系数,计算在大鼠体内的综合血药浓度并建立整合药物代谢动力学(药动学)模型,比较黄芩炮制品中黄酮类成分的整合药动学参数的差异.结果:单成分的AUC0-∞差异较大;多成分整合药动力学结果显示,黄芩酒炙后,8种黄酮类成分的滞留时间(MRT0→∞)由17.22 h缩短为13.13 h.首次达峰时间(Tmax)由0.50 h缩短为0.25 h,2次(Tmax由4 h延长为8 h.黄芩炒炭后,黄芩炭的多成分整体的MRT0→∞为10.07 h,与酒黄芩比较,差异无统计学意义(P>0.05).黄芩炭存在0.25、1、2 h,3次达峰.结论:该方法专属性强、灵敏度高,可作为大鼠血清中8种黄酮类成分的同步检测及其药动学研究的方法,进一步诠释了黄芩"酒炙增效,炒炭存性"的科学内涵.
Integrated Pharmacokinetics of Flavonoids from Different Processed Products of Scutellariae Radix
Objective:To compare the content differences of eight flavonoid components in different processed products of Scutel-lariae Radix(SR)in rats and to explore the differences of pharmacokinetic behaviors of these products,providing scientific evidence for elucidating the processing principles.Methods:Twenty SD rats were randomly divided into control group,raw SR group,wine-processed SR group,and carbonized SR group,with five rats in each group.Drugs were administered by gavage.Using kaempferol as an internal standard,ultra-high-performance liquid chromatography-triple quadrupole mass spectrometry(UPLC-QQQ-MS/MS)was employed to measure the concentrations of baicalin,5,7,2',5'-tetrahydroxy-8,6'-dimethoxyflavone(HQ-6),wogonoside,baicalein,wogonin,chrysin,5,6-dihydroxy-7,8,2',6'-tetramethoxyflavone(HQ-2),and oroxylin A in rat serum at various time points.The ar-ea under the curve(AUC0→∞)percentage of each component was used as a custom weighting coefficient to calculate the overall ser-um concentration of the drugs in rats and establish an integrated pharmacokinetic model to compare the differences in pharmacoki-netic parameters of flavonoid components in processed products of SR.Results:The AUC0→∞ for single components varied signifi-cantly.The integrated pharmacokinetic results of multiple components showed that after wine processing of SR,the mean retention time(MRT0 →∞)of the eight flavonoid components was reduced from 17.22 h to 13.13 h.The time to reach peak concentration(Tmax)decreased from 0.50 h to 0.25 h,while the time to secondary peak increased from 4 h to 8 h.After carbonization of SR,the overall MRT for the carbonized product was 10.07 h,which was not significantly different from the wine-processed product(P>0.05).The carbonized SR showed three peaks at 0.25,1,and 2 h.Conclusion:This method is specific and highly sensitive,suit-able for simultaneous detection and pharmacokinetic studies of eight flavonoid components in rat serum,further elucidating the sci-entific meaning of"enhanced efficacy by wine processing and stability by carbonization'for SR.

Scutellariae RadixWine-processed Scutellariae RadixCarbonized Scutellariae RadixFlavonoidsIntegrated pharma-cokineticsProcessingUltra-high-performance liquid chromatography-triple quadrupole mass spectrometry(UPLC-QQQ-MS/MS)

宋亚南、王云、陈影、黄琪、张村

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中国中医科学院中药研究所,北京,100700

安徽中医药大学药学院,合肥,230012

黄芩 酒黄芩 黄芩炭 黄酮 整合药动学 炮制 超高效液相色谱-三重四级杆串联质谱法

2024

世界中医药
世界中医药学会联合会

世界中医药

CSTPCDCHSSCD北大核心
影响因子:1.266
ISSN:1673-7202
年,卷(期):2024.19(17)