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

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Abstract

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 ⩾10 the lactone ring is quantitatively opened while at pH values ⩽4 the lactone form is exclusively present. Other parameters, such as buffer ions and ionic strength, do not influence equilibrium. Complexation with dimethyl-β-cyclodextrin stabilizes the lactone form. Other cyclodextrins do not show this stabilization.

References (2)

  • EORTC Protocol No. ND 02891, Version No. 2, August...
  • A.N. Martin et al.

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Presented at the Second International Symposium on “Pharmaceutical and Biomedical Analysis”, April 1990, York, UK.

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