Pharmacokinetic and metabolic studies of busulfan in rat plasma and brain
- 1 October 1988
- journal article
- research article
- Published by Springer Nature in European Journal of Drug Metabolism and Pharmacokinetics
- Vol. 13 (4) , 301-305
- https://doi.org/10.1007/bf03190094
Abstract
Summary Busulfan kinetics were studied in the rat plasma and brain after an I.P. dose of14C-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 the14C-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%).Keywords
This publication has 22 references indexed in Scilit:
- Hydrophobicity and Central Nervous System Agents: On the Principle of Minimal Hydrophobicity in Drug DesignJournal of Pharmaceutical Sciences, 1987
- The selective barrier between blood and brainTrends in Biochemical Sciences, 1986
- Degradation of busulfan in aqueous solutionJournal of Pharmaceutical and Biomedical Analysis, 1986
- Gas chromatographic determination of busulfan in plasma with electron-capture detectionJournal of Chromatography B: Biomedical Sciences and Applications, 1983
- Marrow Transplantation for Acute Nonlymphocytic Leukemia after Treatment with Busulfan and CyclophosphamideNew England Journal of Medicine, 1983
- RADIATION-RELATED DISTURBANCE OF BLOOD/BRAIN BARRIER DURING THERAPY OF ACUTE LYMPHOBLASTIC LEUKAEMIAThe Lancet, 1983
- Aspects of Blood-Brain Barrier in Clinical Brain ImagingPublished by Springer Nature ,1983
- Degradation of Melphalan in Aqueous Solutions—Influence of Human Albumin BindingJournal of Pharmaceutical Sciences, 1982
- Degradation of chlorambucil in aqueous solution—influence of human albumin bindingJournal of Pharmacy and Pharmacology, 1981
- Dimethanesulphonoxybutane (Myleran): Preliminary studies on distribution and metabolic fate in the ratBiochemical Pharmacology, 1959