Absolute bioavailability of caffeic acid in rats and its intestinal absorption properties.
- Author:
Jie ZENG
;
Su-Jun WANG
;
Ben-Kun YANG
;
Yun-Ming ZHONG
;
Lin-Quan ZANG
;
Ling-Li WANG
- Publication Type:Journal Article
- MeSH: Animals; Biological Availability; Caco-2 Cells; Caffeic Acids; metabolism; pharmacokinetics; Humans; Intestinal Absorption; Male; Rats; Rats, Sprague-Dawley
- From: China Journal of Chinese Materia Medica 2013;38(23):4152-4156
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVETo investigate the absolute bioavailability of caffeic acid in rats and its intestinal absorption properties.
METHODThe absolute bioavailability (Fabs) of caffeic acid was obtained after iv (2 mg x kg(-1)) or ig (10 mg x kg(-1)) administration to rats. The intestinal absorption of caffeic acid was explored by the recirculating vascularly perfused rat intestinal preparation. Caco-2 cell model was applied to measure the permeability of caffeic acid from apical to basolateral said (A-B) and from basolateral to apical said (B-A).
RESULTA two-compartment pharmacokinetic model was best to describe the pharmacokinetics of caffeic acid following iv or ig administration. The Fabs of caffeic acid was 14. 7% , and its intestinal absorption was 12.4%. The values of Papp A-->B and Papp B-->A of caffeic acid were retained stable while its concentration was changed. The efflux ratio values in this study surveyed were above 2.0, and suggesting caffeic acid was active transport.
CONCLUSIONCaffeic acid was shown to have poor permeability across the Caco-2 cells, low intestinal absorption and low oral bioavailability in rats.