中国临床药理学与治疗学2024，Vol.29Issue(1)：37-51,15.DOI:10.12092/j.issn.1009-2501.2024.01.004
达立通浸膏中延胡索乙素、川陈皮素和木香烃内酯在大鼠体内的药代动力学及组织分布研究
Pharmacokinetics and tissue distribution of tetrahydropalmatine,nobiletin,and costunolide in rats after oral administration of Dalitong extract
张渊茂 1张冉 1廖睿伟 1陶琳 2孟秀秀 1徐晨 1高芳芳 1阿基业 1王广基1
作者信息
- 1. 中国药科大学药物代谢动力学重点实验室,南京 210009,江苏
- 2. 南昌弘益药业有限公司,南昌 330006,江西
- 折叠
摘要
Abstract
AIM:To investigate the pharmacoki-netic properties of the main active components of Dalitong extract in SD rats after oral administration using UPLC-MS/MS.METHODS:An UPLC-MS/MS method was established to simultaneously detect tetrahydropalmatine,nobiletin and costunolide in the plasma and tissues of SD rats.The method was applied to investigate the pharmacokinetic charac-teristics and tissue distribution.RESULTS:After a single oral administration,the three active compo-nents were rapidly absorbed into the body,with a peak concentration(Cmax)of(13.73±7.50),(27.01± 17.69)and(6.73±29.94)ng/mL for tetrahydropal-matine,nobiletin,and costunolide,respectively.The time to reach the peak concentration(Tmax)was(1.40±0.93),(0.63±0.28)and(2.38±8.81)h,re-spectively.The area under the curve(AUC)was(80.43±40.03),(41.30±28.69)and(303.90±136.69)ng·h·mL-1,respectively,and the elimination half-life(t1/2)was(5.82±2.22),(1.08±0.01)and(4.95± 2.53)h,respectively.Multiple dosing significantly in-creased the exposure of the three components.There were significant differences in exposure be-tween male and female rats,with higher exposure observed in female rats(P＜0.05).The three active components were widely distributed in various tis-sues/organs,with the highest exposure observed in the gastrointestinal tract,followed by the liver and kidney.CONCLUSION:The UPLC-MS/MS method is accurate,sensitive,and reliable for the quantitative analysis of tetrahydropalmatine,nobiletin,and cos-tunolide.These three active components in Dali-tong extract can be absorbed,widely distributed in various tissues or organs,and rapidly metabolized/eliminated after oral administration.They are po-tential pharmacokinetic markers of Dalitong extract.关键词
达立通浸膏/延胡索乙素/川陈皮素/木香烃内酯/药物代谢动力学/组织分布Key words
Dalitong extract/tetrahydropalma-tine/nobiletin/costunolide/pharmacokinetics/tis-sue distribution分类
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张渊茂,张冉,廖睿伟,陶琳,孟秀秀,徐晨,高芳芳,阿基业,王广基..达立通浸膏中延胡索乙素、川陈皮素和木香烃内酯在大鼠体内的药代动力学及组织分布研究[J].中国临床药理学与治疗学,2024,29(1):37-51,15.
