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Relative oral bioavailability of 3-MCPD from 3-MCPD fatty acid esters in rats

机译:3-MCPD脂肪酸酯对大鼠3-MCPD的相对口服生物利用度

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摘要

In order to quantify the relative oral bioavailability of 3-chloropropane-1,2-diol (3-MCPD) from 3-MCPD fatty acid diesters in vivo, 1,2-dipalmitoyl-3-chloropropane-1,2-diol (3-MCPD diester) and 3-MCPD were orally applied to rats in equimolar doses. In both cases, the time courses of 3-MCPD concentrations were measured in blood, various organs, tissues and intestinal luminal contents. The results show that 3-MCPD is released by enzymatic hydrolysis from the 3-MCPD diester in the gastrointestinal tract and distributed to blood, organs and tissues. Based on the measurements in blood, the areas under the curve (AUC) for 3-MCPD were calculated. By comparing both AUC, the relative amount of 3-MCPD bioavailable from the 3-MCPD diester was calculated to be 86 % on average of the amount bioavailable following administration of 3-MCPD. In view of limited experimental data, it is justified for the purpose of risk assessment to assume complete hydrolysis of the diesters in the gastro-intestinal tract. Therefore, assessment of the extent of exposure to 3-MCPD released from its fatty acid esters should be performed in the same way as exposure to the same molar quantity of 3-MCPD.
机译:为了量化体内3-MCPD脂肪酸二酯中3-氯丙烷-1,2-二醇(3-MCPD)的相对口服生物利用度,1,2-二棕榈酰-3-氯丙烷-1,2-二醇(3 -MCPD二酯)和3-MCPD以等摩尔剂量口服施用于大鼠。在这两种情况下,均在血液,各种器官,组织和肠腔内含量中测量了3-MCPD浓度的时程。结果表明3-MCPD通过酶水解从胃肠道中的3-MCPD二酯释放并分布到血液,器官和组织。根据血液中的测量值,计算3-MCPD的曲线下面积(AUC)。通过比较两个AUC,从3-MCPD二酯可生物利用的3-MCPD的相对量经计算为平均施用3-MCPD后可生物利用的量的86%。鉴于有限的实验数据,出于风险评估的目的,假定二酯在胃肠道中完全水解是合理的。因此,应以与暴露于相同摩尔量的3-MCPD相同的方式评估其脂肪酸酯释放的3-MCPD的暴露程度。

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