Comparative Pharmacokinetics of Chlorambucil and Prednimustine after Oral Administration
作者:
Ulrich Loos,
Eugen Musch,
Mouhammad Malek,
Eberhard Riedel,
期刊:
Oncology
(Karger Available online 1991)
卷期:
Volume 48,
issue 4
页码: 334-342
ISSN:0030-2414
年代: 1991
DOI:10.1159/000226953
出版商: S. Karger AG
关键词: Chlorambucil;Phenylacetic acid mustard;Prednisolone;Prednimustine;Plasma concentrations;Comparative pharmacokinetics;Bioavailability
数据来源: Karger
摘要:
The pharmacokinetics of chlorambucil, phenylacetic acid mustard (the β-oxidation product of chlorambucil), and prednisolone were investigated in a cross-over study after oral administration of chlorambucil (30 mg) + prednisolone (50 mg) versus prednimustine (300 mg), the ester of chlorambucil and prednisolone. Intact prednimustine could not be detected in plasma at any time. After administration of prednimustine, the plasma concentration-time curves of chlorambucil, phenylacetic acid mustard, and prednisolone showed a retarded profile compared to the administration of the single components. The mean bioavailability was 14% for chlorambucil, 21% for phenylacetic acid mustard, and 22% for prednisolone, when given as prednimustine, compared to the administration of free compounds in stoichiometrically equivalent doses. When given in the oral dosages mentioned above, the average dose-intensity was 62% for chlorambucil, 95% for phenylacetic acid mustard, and 72% for prednisolone, indicating sufficient therapeutic concentrations of the detectable agents
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