title: Transport characteristics of ginkgolide B by Caco-2 cells and examination of ginkgolide B oral absorption potential using rat in situ intestinal loop method.
abstract: The intestinal absorptive characteristics of ginkgolide B were investigated. The Caco-2 cells and the in situ closed loop were used as models of the intestinal mucosa to assess transepithelial transport of ginkgolide B. The determination of ginkgolide B was performed by HPLC-MS. In the Caco-2 cells, the absorptive transepithelial transport of ginkgolide B was pH dependent and the transport was enhanced at weakly acidic pH on the apical side. No concentration dependence and saturation were observed for the absorptive transport of ginkgolide B at concentrations up to 50 microM. In the in situ closed loop, the absorption of ginkgolide B was intestinal segment-selective. The results indicate that the intestinal absorption of ginkgolide B in the upper intestine was significantly higher than that in the lower intestine.
authors.affiliation: Key Laboratory of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, Nanjing, Jiangsu, China.
authors.forename: Hua
authors.initials: H
authors.lastname: Lv
authors.forename: Guangji
authors.initials: G
authors.lastname: Wang
authors.forename: Xiaolan
authors.initials: X
authors.lastname: Wu
authors.forename: Lin
authors.initials: L
authors.lastname: Xie
authors.forename: Chenrong
authors.initials: C
authors.lastname: Huang
authors.forename: Hao
authors.initials: H
authors.lastname: Li
authors.forename: Yan
authors.initials: Y
authors.lastname: Liang
authors.forename: Haiping
authors.initials: H
authors.lastname: Hao
authors.forename: Jie
authors.initials: J
authors.lastname: Sun
mesh_terms: D000818:Animals; D001692:Biological Transport; D018938:Caco-2 Cells; D004305:Dose-Response Relationship, Drug; D005343:Fibrinolytic Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D020441:Ginkgo biloba / Q000737:chemistry; D046934:Ginkgolides / Q000008:administration & dosage / Q000493:pharmacokinetics*; D006801:Humans; D006863:Hydrogen-Ion Concentration; D007408:Intestinal Absorption; D007413:Intestinal Mucosa; D007420:Intestine, Large / Q000378:metabolism; D007421:Intestine, Small / Q000378:metabolism; D007783:Lactones / Q000008:administration & dosage / Q000493:pharmacokinetics*; D008297:Male; D008954:Models, Biological; D051381:Rats; D017207:Rats, Sprague-Dawley
chemical_list: D005343:Fibrinolytic Agents; D046934:Ginkgolides; D007783:Lactones; C045856:ginkgolide B