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目的研究1,2-二(2-氨基苯氧基)乙烷-N,N,N’,N’-四乙酸四乙酰氧甲基酯(BAPTA-AM)脂质体注射液在大鼠体内的组织分布和胆汁排泄。方法 Sprague-Dawley大鼠24只,每组6只,每只大鼠尾静脉注射BAPTA-AM脂质体注射液3.0 mg.kg-1。给药后10 min、1.5 h、9 h各处死一组动物,采集各组织制作匀浆,测定各组织中的BAPTA-AM浓度。另一组大鼠收集给药后12 h内各时间段内胆汁,测定胆汁中的BAPTA浓度。结果大鼠静脉注射BAPTA-AM脂质体3.0 mg.kg-1后,药物在组织中浓度显著高于血浆中浓度,主要分布在肺、肝、脾和肾。大鼠静脉注射BAPTA-AM脂质体后BAPTA胆汁排泄较为缓慢,12 h后仍未达平台期。结论大鼠注射BAPTA-AM脂质体后大量分布在组织中,以水解产物BAPTA的形式排出体外。
Objective To investigate the effect of BAPTA-AM injection of 1,2-bis (2-aminophenoxy) ethane-N, N, N ’, N’-tetraacetic acid liposome injection in rats Tissue distribution and biliary excretion. Methods Twenty-four Sprague-Dawley rats, 6 rats in each group, were injected with BAPTA-AM liposomal injection of 3.0 mg · kg-1 into tail vein of each rat. One group of animals were sacrificed 10 min, 1.5 h and 9 h after administration. The tissues were collected and homogenized. The concentration of BAPTA-AM in each tissue was determined. The other group of rats were collected within 12 h after administration of bile within each time period, the determination of BAPTA concentration in bile. Results After intravenous injection of BAPTA-AM liposome 3.0 mg.kg-1, the concentration of the drug in the tissue was significantly higher than that in the plasma, mainly in the lung, liver, spleen and kidney. After BAPTA-AM liposomes were intravenously injected into rats, BAPTA bile excretion was slow, and still not reached the plateau after 12 h. Conclusion The rats were injected with BAPTA-AM liposomes and distributed in large quantities in tissues. The BAPTA-AM liposomes were excreted in the form of hydrolyzate BAPTA.