Metabolism is an important route of pentamidine elimination in the rat: disposition of 14C-pentamidine and identification of metabolites in urine using liquid chromatography-tandem mass spectrometry.
Metabolism is an important route of pentamidine elimination in the rat: disposition of 14C-pentamidine and identification of metabolites in urine using liquid chromatography-tandem mass spectrometry.
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代谢是大鼠体内喷他脒消除的重要途径：14C-喷脒脒的处置和利用液相色谱-串联质谱法鉴定尿液中的代谢物。
DOI：
10.1111/j.1600-0773.1995.tb00999.x
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发表时间：
1995
期刊：
影响因子：
--
通讯作者：
Gustafsson,LL
中科院分区：
文献类型：
--
作者：
Bronner,U;Ericsson,O;Nordin,J;Wikström,I;Abdi,YA;Hall,JE;Tidwell,RR;Gustafsson,LL
This study assesses the contribution of metabolism for the disposition of pentamidine in the rat. With the use of14C‐labelled compound, the excretion of radioactivity in urine and faeces has been studied in four rats during 44 days after a single intravenous injection of the drug. The urinary and faecal excretion of the radioactivity were of equal importance; 22±2% (mean±S.D.) and 25±4% being detected in urine and faeces, respectively. The activity in organs and tissues at 44 days after drug administration was also measured and amounted to 21±5% of the administered dose. Using HPLC the proportion of metabolites in urine in relation to unchanged pentamidine increased with time after dose, being 76±15% (mean±S.D.) of the total excreted radioactivity on day 1 and 97±1% on day 6. HPLC ‐ tandem mass spectrometry was used for identification of metabolites in urine obtained from four rats given unlabelled pentamidine. Using synthetic reference compounds and the selective MS/MS mode four oxidized metabolites of pentamidine were identified either by direct injection into the system or by analyses of extracted urine. Thus, a substantial part of pentamidine is excreted as metabolites in urine.
