论文部分内容阅读
血卟啉单甲醚(代号PsD-044)是一种新的肿瘤光化学诊治剂。本文报道用荧光分光光度法测定PsD-044在S_(180)肉瘤荷瘤小鼠体内的分布及肿瘤与不同组织问的分布比。静注20 mg/kg的PsD-044 30 min后,不同组织中的药物浓度均达峰值。药后3 h,药物在肿瘤与皮肤及骨骼肌间的分布差距最大,肿瘤/皮肤和肿瘤/骨骼肌分布比分别为3和12.2。此时,各组织中的药物浓度依次为肝>肿瘤>肺>皮肤>肾>脾≈心肌≈骨骼肌。药物从组织中消除较快。实验结果表明,PsD-044未能透过血-脑屏障而进入脑组织。在小鼠体内的药物动力学符合三房室模型,所测的主要药物动力学参数与组织分布测定结果基本一致。
Hematoporphyrin monomethyl ether (code PsD-044) is a new tumor photochemical diagnosis and treatment agent. This paper reports the distribution of PsD-044 in S 180 tumor-bearing mice and the distribution ratio of tumor to different tissues by fluorescence spectrophotometry. After intravenous injection of 20 mg / kg PsD-044 for 30 min, the drug concentration peaked in different tissues. At 3 h after drug treatment, the difference in distribution of tumor between tumor and skin and skeletal muscle was the largest, with tumor / skin and tumor / skeletal muscle distribution ratios of 3 and 12.2, respectively. At this point, the concentrations of the drugs in each tissue were in the order of liver> tumor> lung> skin> kidney> spleen ≈ myocardium ≈ skeletal muscle. Drugs are eliminated quickly from the tissue. The experimental results show that PsD-044 failed to penetrate the blood-brain barrier into the brain tissue. The pharmacokinetics in mice were in accordance with the three-compartment model and the main pharmacokinetic parameters measured were in good agreement with the tissue distribution measurements.