OBJECTIVE To study the pharmacokinetic profiles of oral busulfan in Chinese patients undergoing allogeneic hematopoietic stem cell transplantation. METHODS Blood samples of 9 adult patients were collected following the first and the ninth dose of standard 16 doses of oral busulfan，4-day regimen. The plasma concentrations of busulfan were determined by HPLC, and the pharmacokinetic parameters of busulfan were calculated by DAS statistical software. RESULTS The plasma concentration- time curves after dose 1 and dose 9 of oral 1 mg·kg-1 busulfan in 9 patients were described by an one-compartment model，respectively. The main pharmacokinetic parameters were as follows：t1/2 （133.0±30.6）and（131.4±28.2）min, Ke （0.005±0.001）and（0.006±0.001）min-1, Vd/F（0.56±0.12）and（0.46±0.08）L·kg-1, CL/F（0.003±0.001）and（0.002±0.001）L·min-1·kg-1, AUC0-t（910.3±146.9）and（1 158.5±139.0）μmol·min·L-1, AUC0-∞（1 401.9±243.2）and（1 689.0±312.4） μmol·min·L-1，respectively. Busulfan average steady state plasma concentration was （3.29±0.39）μmol·L-1. CONCLUSION The pharmacokinetic profiles of oral busulfan are fitted to an one-compartment model，and the main pharmacokinetic parameters are significant difference between dose 1 and dose 9.
Key words
busulfan /
allogeneic hematopoietic stem cell transplantation /
preparative regimen /
pharmacokinetics
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References
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（ 收稿日期 ： 2008-12-11 ）
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