白消安在大鼠血浆和脑组织中的药代动力学及代谢研究。
Pharmacokinetic and metabolic studies of busulfan in rat plasma and brain.
作者信息
Hassan M, Ehrsson H, Wallin I, Eksborg S
机构信息
Karolinska Pharmacy, Stockholm, Sweden.
出版信息
Eur J Drug Metab Pharmacokinet. 1988 Oct-Dec;13(4):301-5. doi: 10.1007/BF03190094.
Busulfan kinetics were studied in the rat plasma and brain after an I.P. dose of 14C-busulfan or busulfan (15 mg/kg). The distribution of busulfan to the brain was rapid and the ratio brain/plasma concentration was 0.74 during the time-course of busulfan. The elimination half-lives in plasma and brain were 3h for intact busulfan and 8h for the 14C-radioactivity. The radioactivity remaining in plasma and brain after 24h was mostly busulfan metabolites e.g. sulfolane, 3-hydroxysulfolane and tetrahydrothiophene-1-oxide as identified by gas chromatography-mass spectrometry. The protein binding to rat plasma was low (9.2 +/- 4.4%).
腹腔注射14C-白消安或白消安（15毫克/千克）后，在大鼠血浆和脑中研究了白消安的动力学。白消安向脑内的分布迅速，在整个白消安作用过程中，脑/血浆浓度比为0.74。血浆和脑中完整白消安的消除半衰期为3小时，14C放射性的消除半衰期为8小时。24小时后血浆和脑中残留的放射性主要是白消安代谢产物，如通过气相色谱-质谱法鉴定的环丁砜、3-羟基环丁砜和四氢噻吩-1-氧化物。白消安与大鼠血浆的蛋白结合率较低（9.2±4.4%）。
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