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作 者:杨本坤[1,2] 王素军[1,2] 莫李立[2] 曾洁[2] 钟运鸣[2] 藏林泉[2]
机构地区:[1]广东药学院临床药学系,广东广州510006 [2]广东药学院药科学院,广东广州510006
出 处:《解放军药学学报》2013年第3期185-188,共4页Pharmaceutical Journal of Chinese People's Liberation Army
基 金:国家自然科学基金;No.81073141;广东省自然科学基金;No.9152402301000007;2010年科技部新药重大专项;No.2011zx09102-001-31
摘 要:目的研究大鼠体内单体肉桂酸的绝对生物利用度及其肠道吸收特性。方法 LC-MS/MS法检测大鼠灌胃和静注肉桂酸后的血药浓度,分析其药代动力学特征并计算绝对生物利用度;建立Caco-2细胞模型计算表观通透系数分析其转运特性;建立大鼠原位肠血管灌流模型分析肉桂酸在肠道的吸收率及吸收特点。结果肉桂酸的绝对生物利用度为81.10%;Caco-2细胞模型中不同浓度时其表观通透系数无显著性差异;在肠血管灌流模型中低、中、高剂量组的吸收率分别为80.8%、85.3%、82.9%。结论肉桂酸吸收良好,分布、消除较快,其肠道吸收机制为被动转运。Objective To study the absolute bioavailability of cinnamic acid in rats in vivo and its absorption properties. Methods Based on the LC-MS/MS method, the absolute bioavailability was calculated by measuring the plasma concentration after iv or ig administration of cinnamic acid in rats. Caco-2 cell monolayer model was applied to studying the transport of cinnamic acid. The in situ vascularly perfused intestine preparation was used to investigate the intestinal absorption rate. Results The absolute bioavailability was 81.10% in rats. There was no significant differ- ence between different concentrations in the apparent permeability coefficient ( P app ) of cinnamic. The intestinal ab- sorption rate of high dose group,middle dose group and low dose group was 80.8% ,85.3% and 82.9% in the in situ vascularly perfused intestine preparation, respectively. Conclusion Cinnamic acid is well absorbed and distributed and eliminated quickly. Furthermore,the absorption pattern of intestines is passive transport.
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