共 2 条
[1]
MARTIN AN, 1969, PHYSICAL PHARM, P365
[2]
1989, EORTC ND02891 PROT
EQUILIBRIUM KINETICS OF THE NEW EXPERIMENTAL ANTITUMOR COMPOUND SK-AND-F 104864-A IN AQUEOUS-SOLUTION
被引：81
作者：
UNDERBERG, WJM
GOOSSEN, RMJ
SMITH, BR
BEIJNEN, JH
机构：
[1] SMITH KLINE & BEECHAM LABS,DEPT DRUG METAB,KING OF PRUSSIA,PA 19406
[2] NETHERLANDS CANC INST,SLOTERVAART HOSP,1066 EC AMSTERDAM,NETHERLANDS
关键词：
ANTITUMOR AGENTS;
SK-AND-F;
104864-A;
DEGRADATION;
EQUILIBRIUM KINETICS;
STABILIZATION;
D O I：
10.1016/0731-7085(90)80102-U
中图分类号：
O65 [分析化学];
学科分类号：
070302 ;
081704 ;
摘要：
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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页码：681 / 683
页数：3
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