Transport characteristics of ginkgolide B by Caco-2 cells and examination of ginkgolide B oral absorption potential using rat in situ intestinal loop method.
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.
Lv
Hua
H
Key Laboratory of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, Nanjing, Jiangsu, China.
Wang
Guangji
G
Wu
Xiaolan
X
Xie
Lin
L
Huang
Chenrong
C
Li
Hao
H
Liang
Yan
Y
Hao
Haiping
H
Sun
Jie
J
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
D005343:Fibrinolytic Agents; D046934:Ginkgolides; D007783:Lactones; C045856:ginkgolide B