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Absolute bioavailability of caffeic acid in rats and its
intestinal absorption properties
ZENG Jie1， WANG Su-jun1*， YANG Ben-kun1， ZHONG Yun-ming1， ZANG Lin-quan1， WANG Ling-li2
（1.Clinical pharmacy Department of Guangdong Pharmaceutical University， Guangzhou ， China；
2.Mathematical Engineering Institute of Dongguan Guangzhou University of Traditional Chinese Medicine，
Guangdong ， China）
[Abstract] Objective： To investigate the absolute bioavailability of caffeic acid in rats and its intestinal absorption properties. Method： The absolute bioavailability （Fabs） of caffeic acid was obtained after iv （2 mg·kg-1） or ig （10 mg·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）. Result： A 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→Band 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. Conclusion： Caffeic acid was shown to have poor permeability across the Caco-2 cells， low intestinal absorption and low oral bioavailability in rats.
[Key words] caffeic acid； bioavailability； intestinal absorption； permeability
doi：10.4268/cjcmm