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目的:研究咖啡酸在大鼠体内的绝对生物利用度及其在肠道的吸收特性。方法:大鼠分别采用静脉(2 mg·kg-1)、灌胃(10 mg·kg-1)给药研究咖啡的绝对生物利用度;建立大鼠原位肠血管灌流模型研究咖啡酸在肠道的吸收率;采用Caco-2细胞模型研究咖啡酸的双向转运情况。结果:咖啡酸静脉(2 mg·kg-1)、灌胃(10 mg·kg-1)给药后,在大鼠体内的药动学行为均符合二室模型,咖啡酸的绝对生物利用度为14.7%;咖啡酸在肠血管灌流模型中的吸收率为12.4%;咖啡酸的P appAP→BL及P appBL→AP不随浓度的变化而变化,且在实验浓度的范围内,P appBL→AP/P appAP→BL均大于2。结论:咖啡酸绝对生物利用度低,肠道吸收率少,在Caco-2细胞单层模型中的转运途径可能为主动转运。
Objective: To study the absolute bioavailability of caffeic acid in rats and its intestinal absorption characteristics. Methods: The rats were given intravenous (2 mg · kg-1), intragastric administration (10 mg · kg-1) to study the absolute bioavailability of coffee; Establishment of rat model of intestinal perfusion in situ caffeic acid in the intestine Road absorption rate; Caffeic acid bidirectional transport studies using Caco-2 cell model. Results: The pharmacokinetics of caffeic acid intravenous (2 mg · kg -1) and gavage (10 mg · kg -1) in rats were in accordance with the two compartment model. The absolute bioavailability of caffeic acid Was 14.7%. The absorption rate of caffeic acid in the model of intestinal vascular perfusion was 12.4%. The changes of caffeic acid P appAP → BL and P appBL → AP did not change with the concentration, and in the experimental concentration range, P appBL → AP / P appAP → BL are greater than two. CONCLUSION: Caffeic acid has low absolute bioavailability and low intestinal absorption, which may be the active transporter in Caco-2 monolayer model.