Comparative study of pharmacokinetics and tissue distribution of 8-cetylberberine and berberine in rats.
- Author:
Yu-Li HU
;
Chao CHEN
;
Zong-Yao ZOU
;
Xue-Gang LI
;
Xiao-Li YE
- Publication Type:Journal Article
- MeSH:
Administration, Oral;
Animals;
Berberine;
analogs & derivatives;
pharmacokinetics;
Biological Availability;
Chromatography, High Pressure Liquid;
Rats;
Tissue Distribution
- From:
Acta Pharmaceutica Sinica
2014;49(11):1582-1587
- CountryChina
- Language:Chinese
-
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.
