Effects of puerarin on the pharmacokinetics of triptolide in rats

Context: Puerarin and triptolide are sometimes used together for the treatment of disease in Chinese clinics; however, the drug–drug interaction between puerarin and triptolide is still unknown. Objective: This study investigates the effects of puerarin on the pharmacokinetics of triptolide in rats...

Descripción completa

Guardado en:

Detalles Bibliográficos
Autores principales:	Qingfa Wang, Yanping Wu, Fengting Xiang, Yan Feng, Zhenghao Li, Yufeng Ding
Formato:	article
Lenguaje:	EN
Publicado:	Taylor & Francis Group 2019
Materias:	caco-2 cells p-gp metabolism Therapeutics. Pharmacology RM1-950
Acceso en línea:	https://doaj.org/article/e5f3d490926b42039ec13101186d9bf0
Etiquetas:	Agregar Etiqueta Sin Etiquetas, Sea el primero en etiquetar este registro!

id	oai:doaj.org-article:e5f3d490926b42039ec13101186d9bf0
record_format	dspace
spelling	oai:doaj.org-article:e5f3d490926b42039ec13101186d9bf02021-11-17T14:21:56ZEffects of puerarin on the pharmacokinetics of triptolide in rats1388-02091744-511610.1080/13880209.2019.1626448https://doaj.org/article/e5f3d490926b42039ec13101186d9bf02019-01-01T00:00:00Zhttp://dx.doi.org/10.1080/13880209.2019.1626448https://doaj.org/toc/1388-0209https://doaj.org/toc/1744-5116Context: Puerarin and triptolide are sometimes used together for the treatment of disease in Chinese clinics; however, the drug–drug interaction between puerarin and triptolide is still unknown. Objective: This study investigates the effects of puerarin on the pharmacokinetics of triptolide in rats and clarifies its main mechanism. Materials and methods: The pharmacokinetic profiles of oral administration of triptolide (1 mg/kg) in Sprague-Dawley rats with (test group, n = 6) or without pretreatment (control group, n = 6) with puerarin (100 mg/kg/day for seven days) were investigated. The effects of puerarin on the transport and metabolic stability of triptolide were also investigated using Caco-2 cell transwell model and rat liver microsomes. Results: The results showed that puerarin could significantly increase the peak plasma concentration (from 187.25 ± 15.36 to 219.67 ± 21.52 ng/mL), and decrease its oral clearance (from 4.92 ± 0.35 to 62.46 ± 3.75 ± 0.19 L/h/kg). The Caco-2 cell transwell experiments indicated that puerarin could decrease the efflux ratio of triptolide from 2.70 to 1.33, and the intrinsic clearance rate of triptolide was decreased by the pretreatment with puerarin (38.8 ± 4.7 vs. 32.9 ± 6.5 μL/min/mg protein). Discussion and conclusions: Puerarin could significantly change the pharmacokinetic profiles of triptolide in rats, and it might exert these effects through increasing the absorption of triptolide by inhibiting the activity of P-gp, or through inhibiting the metabolism of triptolide in rat liver. The results also showed that the dose of triptolide should be decreased when these drugs were co-administered.Qingfa WangYanping WuFengting XiangYan FengZhenghao LiYufeng DingTaylor & Francis Grouparticlecaco-2 cellsp-gpmetabolismTherapeutics. PharmacologyRM1-950ENPharmaceutical Biology, Vol 57, Iss 1, Pp 407-411 (2019)
institution	DOAJ
collection	DOAJ
language	EN
topic	caco-2 cells p-gp metabolism Therapeutics. Pharmacology RM1-950
spellingShingle	caco-2 cells p-gp metabolism Therapeutics. Pharmacology RM1-950 Qingfa Wang Yanping Wu Fengting Xiang Yan Feng Zhenghao Li Yufeng Ding Effects of puerarin on the pharmacokinetics of triptolide in rats
description	Context: Puerarin and triptolide are sometimes used together for the treatment of disease in Chinese clinics; however, the drug–drug interaction between puerarin and triptolide is still unknown. Objective: This study investigates the effects of puerarin on the pharmacokinetics of triptolide in rats and clarifies its main mechanism. Materials and methods: The pharmacokinetic profiles of oral administration of triptolide (1 mg/kg) in Sprague-Dawley rats with (test group, n = 6) or without pretreatment (control group, n = 6) with puerarin (100 mg/kg/day for seven days) were investigated. The effects of puerarin on the transport and metabolic stability of triptolide were also investigated using Caco-2 cell transwell model and rat liver microsomes. Results: The results showed that puerarin could significantly increase the peak plasma concentration (from 187.25 ± 15.36 to 219.67 ± 21.52 ng/mL), and decrease its oral clearance (from 4.92 ± 0.35 to 62.46 ± 3.75 ± 0.19 L/h/kg). The Caco-2 cell transwell experiments indicated that puerarin could decrease the efflux ratio of triptolide from 2.70 to 1.33, and the intrinsic clearance rate of triptolide was decreased by the pretreatment with puerarin (38.8 ± 4.7 vs. 32.9 ± 6.5 μL/min/mg protein). Discussion and conclusions: Puerarin could significantly change the pharmacokinetic profiles of triptolide in rats, and it might exert these effects through increasing the absorption of triptolide by inhibiting the activity of P-gp, or through inhibiting the metabolism of triptolide in rat liver. The results also showed that the dose of triptolide should be decreased when these drugs were co-administered.
format	article
author	Qingfa Wang Yanping Wu Fengting Xiang Yan Feng Zhenghao Li Yufeng Ding
author_facet	Qingfa Wang Yanping Wu Fengting Xiang Yan Feng Zhenghao Li Yufeng Ding
author_sort	Qingfa Wang
title	Effects of puerarin on the pharmacokinetics of triptolide in rats
title_short	Effects of puerarin on the pharmacokinetics of triptolide in rats
title_full	Effects of puerarin on the pharmacokinetics of triptolide in rats
title_fullStr	Effects of puerarin on the pharmacokinetics of triptolide in rats
title_full_unstemmed	Effects of puerarin on the pharmacokinetics of triptolide in rats
title_sort	effects of puerarin on the pharmacokinetics of triptolide in rats
publisher	Taylor & Francis Group
publishDate	2019
url	https://doaj.org/article/e5f3d490926b42039ec13101186d9bf0
work_keys_str_mv	AT qingfawang effectsofpuerarinonthepharmacokineticsoftriptolideinrats AT yanpingwu effectsofpuerarinonthepharmacokineticsoftriptolideinrats AT fengtingxiang effectsofpuerarinonthepharmacokineticsoftriptolideinrats AT yanfeng effectsofpuerarinonthepharmacokineticsoftriptolideinrats AT zhenghaoli effectsofpuerarinonthepharmacokineticsoftriptolideinrats AT yufengding effectsofpuerarinonthepharmacokineticsoftriptolideinrats
_version_	1718425516963266560

Effects of puerarin on the pharmacokinetics of triptolide in rats

Ejemplares similares