苏子油乳剂中α-亚麻酸的药物动力学与生物利用度研究

Study on the Pharmacokinetics and Bioavailability of αLNA in Perilla Oil Emulsion

采用气相色谱法研究了大鼠给予苏子油乳剂后α亚麻酸的药物动力学与生物利用度．恒速静滴苏子油乳剂，血浆中αＬＮＡ浓度时间曲线呈现开放性双隔室模型特征；静注３个不同剂量乳剂后（αＬＮＡ分别为９１４，１８２８，２７４２ｍｇ·ｋｇ－１），αＬＮＡ血药浓度时间曲线呈线性药物动力学特征，其中小剂量组符合开放性双隔室模型，３个剂量组消除半衰期之间无显著性差异（ｐ＞００５）；大鼠交叉灌胃苏子油乳剂及苏子油后，相对生物利用度为１８３１％；灌胃，幽门静脉、颈静脉交叉给予乳剂后，灌胃绝对生物利用度为７２７０％，幽门静脉注射绝对生物利用度为９３７９％，胃肠道代谢或未吸收部分共为２１０９％．灌胃及幽门静脉给药，αＬＮＡ血药浓度时间曲线为开放性单隔室一级吸收模型．

This paper was focused on the study of pharmacokinetics and bioavailability of αLNA in perilla oil emulsion in rats by the GC method. The experimental results showed that the concentrationtime curve of αLNA in plasma fit twocompartment open model after iv, infusion of the emulsion.The αLNA concentrationtime curve showed firstorderlinear kinetics properties after iv .injection of the three different doses of the emulsion and no marked differences were found among the three eliminationrate constants(P>005),while rats were administrated the emulsion via oral,iv ,and imtrapyloric vein injection crossly,the absolute availability was 7270%,fht first pass effect of the liver was 621%,The surplus parts of emulsion(2109%)were not absorpted or were metabilized by the GI tract. The relative bioavailability of the emulsion was 1831% compared with the oil via oral administrating crossly Both of the αLNA concentrationtime curves in plasma fit open oneompartment with firstorder absorption after oral administration and inrtopyloric vein injection of the emulsion.