Pharmacokinetics of the absorption, distribution, and elimination of melphalan in the dog.
Pharmacokinetics of the absorption, distribution, and elimination of melphalan in the dog.
复制标题
马法兰在狗体内的吸收、分布和消除的药代动力学。
DOI：
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发表时间：
1977
期刊：
影响因子：
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通讯作者：
G. Duncan
中科院分区：
文献类型：
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作者：
R. Furner;R. Brown;G. Duncan
经口给药后，[14 C]美法仑（[14 C]L-PAM）从犬肠道中迅速吸收，并在30分钟内达到血清中的最大浓度。静脉给药后，L-PAM（完整药物）从血清中的消失是双相的，α和β相的半衰期分别为14和66分钟。尿排泄占总放射性的44%，粪便中占25%。约8%的剂量以原形经尿液排泄。胆汁排泄迅速，30分钟后胆汁中占剂量的11%;这些药物当量（含放射性物质）中约80%为母体化合物。由于大量的L-PAM出现在胆汁中，该药剂可能被证明对胆囊癌、胆管癌和十二指肠癌有活性。
[14C]melphalan ([14C]L-PAM) was rapidly absorbed from the gut of dogs after oral dosing and reached a maximum concentration in the serum by 30 minutes. The disappearance of L-PAM (intact drug) from the serum was biphasic after iv administration, with half-lives of 14 and 66 minutes for the alpha and beta phases, respectively. The urinary excretion accounted for 44% of the total radioactivity and 25% appeared in the feces. Approximately 8% of the dose was excreted unchanged in the urine. Biliary excretion was rapid, with 11% of the dose being accounted for in the bile after 30 minutes; approximately 80% of these drug equivalents (materials containing radioactivity) was parent compound. Since large amounts of L-PAM appeared in the bile, the agent may prove to be active against cancers of the gall bladder, bile ducts, and duodenum.