Comparative study of pharmacokinetics and tissue distribution of 8-cetylberberine and berberine in rats / 药学学报
Acta Pharmaceutica Sinica
;
(12): 1582-1587, 2014.
Article
in Chinese
| WPRIM
| ID: wpr-299093
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.
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Berberine
/
Pharmacokinetics
/
Biological Availability
/
Tissue Distribution
/
Administration, Oral
/
Chromatography, High Pressure Liquid
Limits:
Animals
Language:
Chinese
Journal:
Acta Pharmaceutica Sinica
Year:
2014
Type:
Article
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