Equilibrium kinetics of the new experimental anti-tumour compound SK&F 104864-A in aqueous solution

The equilibrium kinetics of lactone ring hydrolysis in the new experimental anti-tumour compound SK&F 104864-A. (S)-dimethylaminomethyl-10-hydroxycamptothecin hydrochloride, have been studied. Only one product is formed, SK&F 105992. A stability-indicating HPLC method has been optimized to p...

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Bibliographic Details
Published in:	Journal of pharmaceutical and biomedical analysis Vol. 8; no. 8-12; p. 681
Main Authors:	Underberg, W J, Goossen, R M, Smith, B R, Beijnen, J H
Format:	Journal Article
Language:	English
Published:	England 1990
Subjects:	Camptothecin - analogs & derivatives Camptothecin - chemistry Chromatography, High Pressure Liquid Cyclodextrins - chemistry Hydrogen-Ion Concentration Hydrolysis Kinetics Solutions Temperature Topotecan
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Summary:	The equilibrium kinetics of lactone ring hydrolysis in the new experimental anti-tumour compound SK&F 104864-A. (S)-dimethylaminomethyl-10-hydroxycamptothecin hydrochloride, have been studied. Only one product is formed, SK&F 105992. A stability-indicating HPLC method has been optimized to perform the analysis. The pH is the main factor influencing equilibrium; at pH greater than or equal to 10 the lactone ring is quantitatively opened while at pH values less than or equal to 4 the lactone form is exclusively present. Other parameters, such as buffer ions and ionic strength, do not influence equilibrium. Complexation with dimethyl-beta-cyclodextrin stabilizes the lactone form. Other cyclodextrins do not show this stabilization.
ISSN:	0731-7085
DOI:	10.1016/0731-7085(90)80102-U