title: [Comparative study of pharmacokinetics and tissue distribution of 8-cetylberberine and berberine in rats].
abstract: The concentrations of berberine (BBR) and 8-cetylberberine (8-BBR-C16) in rat plasma and tissue were determined by RP-HPLC. Both the plasma pharmacokinetics characteristic and tissue distribution differences of BBR and 8-BBR-C16 were compared to provide experimental data for the mechanism research and further drug development. After the oral administrations of BBR and 8-BBR-C16 at the dose of 80 mg x kg(-1) for rats, the pharmacokinetics result showed that compared with BBR, the C(max) and AUC(0-t), of 8-BBR-C16 increased by 2.8 times and 12.9 times respectively, t1/2 extended from 3.61 h to 11.90 h. The tissue distribution result showed that compared with BBR, the concentration of 8-BBR-C16 in various organizations increased and the retention time extended remarkably. The maximum concentration was achieved in lung and the highest concentration in it was 3 731.82 ng x g(-1). After being derived, the C(max) in plasma and bioavailability of 8-BBR-C16 increased remarkably and the circulation time in vivo extended. The drug concentration in tissue increased remarkably, and the distribution ratio changed too, with strong targeting selection in lung.
authors.forename: Yu-Li
authors.initials: YL
authors.lastname: Hu
authors.forename: Chao
authors.initials: C
authors.lastname: Chen
authors.forename: Zong-Yao
authors.initials: ZY
authors.lastname: Zou
authors.forename: Xue-Gang
authors.initials: XG
authors.lastname: Li
authors.forename: Xiao-Li
authors.initials: XL
authors.lastname: Ye
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001599:Berberine / Q000031:analogs & derivatives* / Q000493:pharmacokinetics*; D001682:Biological Availability; D002851:Chromatography, High Pressure Liquid; D051381:Rats; D014018:Tissue Distribution
chemical_list: C000604411:8-cetylberberine; D001599:Berberine