Equilibrium kinetics of the new experimental anti-tumour compound SK&F 104864-A in aqueous solution
| Autor: | Willy J. M. Underberg, R.M.J. Goossen, B.R. Smith, Jos H. Beijnen |
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| Rok vydání: | 1990 |
| Předmět: |
Stereochemistry
Clinical Biochemistry Kinetics Pharmaceutical Science Ring (chemistry) Medicinal chemistry Analytical Chemistry Ion Hydrolysis Drug Discovery Chromatography High Pressure Liquid Spectroscopy chemistry.chemical_classification Cyclodextrins Aqueous solution Temperature Hydrogen-Ion Concentration Solutions chemistry Ionic strength Degradation (geology) Camptothecin Topotecan Lactone |
| Zdroj: | Journal of Pharmaceutical and Biomedical Analysis. 8:681-683 |
| ISSN: | 0731-7085 |
| DOI: | 10.1016/0731-7085(90)80102-u |
| Popis: | The equilibrium kinetics of lactone ring hydrolysis in the new experimental anti-tumour compound SKF 104864-A. (S)-dimethylaminomethyl-10-hydroxycamptothecin hydrochloride, have been studied. Only one product is formed, SKF 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. |
| Databáze: | OpenAIRE |
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