Determination of sparsomycin in plasma and urine of the dog by means of reversed-phase high-performance liquid chromatography and first pharmacokinetic results

Winograd, B., Oosterbaan, M.J., van der Kleijn, E., Liskamp, R.M., Ottenheijm, H.C. and Wagener, D.J. (1983) Determination of sparsomycin in plasma and urine of the dog by means of reversed-phase high-performance liquid chromatography and first pharmacokinetic results. Journal of chromatography, 275(1), pp. 145-53.

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Abstract

Sparsomycin--an antibiotic with marked cytostatic activity--was the subject of a clinical Phase I study in 1964. The structure of sparsomycin was elucidated in 1970 and its first total synthesis was reported in 1981. Here we describe a sensitive high-performance liquid chromatographic method of determination. The detection limit was found to be 10 ng/ml of plasma and 20 ng/ml of urine. With this procedure sparsomycin and isosparsomycin can readily be separated. In addition, we performed a first pharmacokinetic study in the dog and found a half-life time t1/2 beta of 1.1 h. Only 25% of the administered dose could be recovered in the urine as sparsomycin. We consider that by now many prerequisites for further preclinical studies have been achieved, and the results of these studies will determine whether sparsomycin deserves reintroduction into clinical use.

Item Type:Articles
Status:Published
Refereed:Yes
Glasgow Author(s) Enlighten ID:Liskamp, Professor Robert
Authors: Winograd, B., Oosterbaan, M.J., van der Kleijn, E., Liskamp, R.M., Ottenheijm, H.C., and Wagener, D.J.
College/School:College of Science and Engineering > School of Chemistry
Journal Name:Journal of chromatography
ISSN:0021-9673
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