Pharmacokinetic and metabolic studies of busulfan in rat plasma and brain.
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%).
Hassan
M
M
Karolinska Pharmacy, Stockholm, Sweden.
Ehrsson
H
H
Wallin
I
I
Eksborg
S
S
D000818:Animals; D001798:Blood Proteins / Q000378:metabolism; D001921:Brain / Q000378:metabolism*; D002066:Busulfan / Q000378:metabolism / Q000493:pharmacokinetics*; D008297:Male; D011485:Protein Binding; D051381:Rats; D011919:Rats, Inbred Strains
D001798:Blood Proteins; D002066:Busulfan