Literature DB >> 2100606

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

W J Underberg1, R M Goossen, B R Smith, J H Beijnen.   

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 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.

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Year:  1990        PMID： 2100606     DOI： 10.1016/0731-7085(90)80102-u

Source DB:  PubMed          Journal:  J Pharm Biomed Anal        ISSN： 0731-7085            Impact factor:   3.935


  13 in total

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Review 4.  Topotecan: a review of its efficacy in small cell lung cancer.

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5.  The pharmacokinetics of topotecan and its carboxylate form following separate intravenous administration to the dog.

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6.  Pharmacodynamics and pharmacokinetics of oral topotecan in patients with advanced solid tumours and impaired renal function.

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7.  Pharmacokinetics and pharmacodynamics of topotecan administered daily for 5 days every 3 weeks.

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Review 8.  Clinical pharmacokinetics of topotecan.

Authors:  V M Herben; W W ten Bokkel Huinink; J H Beijnen
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9.  Cerebrospinal fluid pharmacokinetics and penetration of continuous infusion topotecan in children with central nervous system tumors.

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10.  A novel approach for organelle-specific DNA damage targeting reveals different susceptibility of mitochondrial DNA to the anticancer drugs camptothecin and topotecan.

Authors:  M C Díaz de la Loza; R E Wellinger
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