Kinetics of intravenous melphalan

David S Alberts, Sai Y. Chang, H. S. George Chen, Thomas E. Moon, Thomas L. Evans, Raymond L. Furner, Kenneth Himmelstein, Joseph F. Gross

Research output: Contribution to journalArticle

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Abstract

We have studied the disposition and elimination of melphalan after intravenous administration in 9 patients with cancer. High-pressure liquid chromatography anti 14C-melphalan were used to assay drug concentration in plasma and urine. Composite plasma t 1 2α was 7.7 ± 3.3 and t 1 2β was 108 ± 20.8 min for 8 of the patients. The mean 24-hr urinary excretion of melphalan was 13.0 ± 5.4% of the administered dose. In 2 patients, 80% to 100% of the measured 14C counts in plasma and urine samples at each study interval, up to 24 hr after drug administration, could be accounted for by the sum of parent compound, monohydroxy and dihydroxy products, and methanol non extractable radioactivity (i.e., protein-bound activity). These data and evidence of rapid disappearance from plasma at 37° in vitro suggest that spontaneous degradation, and not enzymatic metabolism, is the major determinant of the t 1 2 of melphalan in vivo.

Original languageEnglish (US)
Pages (from-to)73-80
Number of pages8
JournalClinical Pharmacology and Therapeutics
Volume26
Issue number1
StatePublished - Jul 1979

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Melphalan
Urine
Pharmaceutical Preparations
Intravenous Administration
Radioactivity
Methanol
High Pressure Liquid Chromatography
Neoplasms
Proteins

ASJC Scopus subject areas

  • Pharmacology

Cite this

Alberts, D. S., Chang, S. Y., George Chen, H. S., Moon, T. E., Evans, T. L., Furner, R. L., ... Gross, J. F. (1979). Kinetics of intravenous melphalan. Clinical Pharmacology and Therapeutics, 26(1), 73-80.

Kinetics of intravenous melphalan. / Alberts, David S; Chang, Sai Y.; George Chen, H. S.; Moon, Thomas E.; Evans, Thomas L.; Furner, Raymond L.; Himmelstein, Kenneth; Gross, Joseph F.

In: Clinical Pharmacology and Therapeutics, Vol. 26, No. 1, 07.1979, p. 73-80.

Research output: Contribution to journalArticle

Alberts, DS, Chang, SY, George Chen, HS, Moon, TE, Evans, TL, Furner, RL, Himmelstein, K & Gross, JF 1979, 'Kinetics of intravenous melphalan', Clinical Pharmacology and Therapeutics, vol. 26, no. 1, pp. 73-80.
Alberts DS, Chang SY, George Chen HS, Moon TE, Evans TL, Furner RL et al. Kinetics of intravenous melphalan. Clinical Pharmacology and Therapeutics. 1979 Jul;26(1):73-80.
Alberts, David S ; Chang, Sai Y. ; George Chen, H. S. ; Moon, Thomas E. ; Evans, Thomas L. ; Furner, Raymond L. ; Himmelstein, Kenneth ; Gross, Joseph F. / Kinetics of intravenous melphalan. In: Clinical Pharmacology and Therapeutics. 1979 ; Vol. 26, No. 1. pp. 73-80.
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N2 - We have studied the disposition and elimination of melphalan after intravenous administration in 9 patients with cancer. High-pressure liquid chromatography anti 14C-melphalan were used to assay drug concentration in plasma and urine. Composite plasma t 1 2α was 7.7 ± 3.3 and t 1 2β was 108 ± 20.8 min for 8 of the patients. The mean 24-hr urinary excretion of melphalan was 13.0 ± 5.4% of the administered dose. In 2 patients, 80% to 100% of the measured 14C counts in plasma and urine samples at each study interval, up to 24 hr after drug administration, could be accounted for by the sum of parent compound, monohydroxy and dihydroxy products, and methanol non extractable radioactivity (i.e., protein-bound activity). These data and evidence of rapid disappearance from plasma at 37° in vitro suggest that spontaneous degradation, and not enzymatic metabolism, is the major determinant of the t 1 2 of melphalan in vivo.

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