title: Influence of Verapamil on Pharmacokinetics of Triptolide in Rats.
abstract: The aim of this study was to investigate the role of P-glycoprotein (P-gp) in the intestinal absorption of triptolide. In this research, the bidirectional transport of triptolide across Caco-2 cells was studied in vitro. Moreover, the pharmacokinetic profiles of orally administered triptolide with and without pretreatment with verapamil were determined in rats. A markedly higher transport of triptolide across Caco-2 cells was observed in the basolateral-to-apical direction and was abrogated in the presence of the P-gp inhibitor, verapamil. The result indicated that P-gp might be involved in the absorption of triptolide. When the rats were pretreated with verapamil, the C max of triptolide increased from 423.01 ± 19.59 to 565.33 ± 20.27 ng/mL (33.6 %), and the AUC0-6 h increased by approximately 57 % when co-administered with verapamil. It was demonstrated that P-gp was involved in the transport of triptolide, which might exhibit a role in limiting its absorption and attenuating the toxicity of triptolide.
authors: Department of Hepato-Biliary Surgery, Affiliated Hospital of Panzhihua College, Panzhihua, 617000, China.
authors: Yichuan
authors: Y
authors: Zhang
authors: Department of Hepato-Biliary Surgery, Affiliated Hospital of Panzhihua College, Panzhihua, 617000, China.
authors: Jin
authors: J
authors: Li
authors: Department of Oncology, Affiliated Hospital of Panzhihua College, Panzhihua, 617000, China.
authors: Xiaolin
authors: X
authors: Lei
authors: Department of Traditional Medicine, Affiliated Hospital of Panzhihua College, Panzhihua, 617000, China.
authors: Tianying
authors: T
authors: Zhang
authors: Department of Pharmacy, Affiliated Hospital of Panzhihua College, Panzhihua, 617000, China.
authors: Guangxian
authors: G
authors: Liu
authors: Department of Hepato-Biliary Surgery, Affiliated Hospital of Panzhihua College, Panzhihua, 617000, China.
authors: Maohui
authors: M
authors: Yang
authors: Department of Rheumatology, Affiliated Hospital of Panzhihua College, Panzhihua, 617000, China. YCZhang_KY@163.com.
authors: Min
authors: M
authors: Liu
mesh_terms: D018435:ATP Binding Cassette Transporter, Subfamily B / Q000378:metabolism; D000818:Animals; D001692:Biological Transport / Q000187:drug effects; D018938:Caco-2 Cells; D045744:Cell Line, Tumor; D004224:Diterpenes / Q000493:pharmacokinetics*; D004852:Epoxy Compounds / Q000493:pharmacokinetics; D005260:Female; D006801:Humans; D007408:Intestinal Absorption / Q000187:drug effects; D008297:Male; D010616:Phenanthrenes / Q000493:pharmacokinetics*; D051381:Rats; D017207:Rats, Sprague-Dawley; D014700:Verapamil / Q000494:pharmacology*
chemical_list: D018435:ATP Binding Cassette Transporter, Subfamily B; D004224:Diterpenes; D004852:Epoxy Compounds; D010616:Phenanthrenes; C001899:triptolide; D014700:Verapamil