INVESTIGATIONS ON THE IN-VITRO RACEMIZATION OF THALIDOMIDE BY HIGH-PERFORMANCE LIQUID-CHROMATOGRAPHY

被引:100
作者
KNOCHE, B [1 ]
BLASCHKE, G [1 ]
机构
[1] UNIV MUNSTER,INST PHARMACEUT CHEM,D-48149 MUNSTER,GERMANY
关键词
D O I
10.1016/0021-9673(94)80385-4
中图分类号
Q5 [生物化学];
学科分类号
071010 ; 081704 ;
摘要
The racemization of thalidomide enantiomers was examined in various aqueous media. The determination of the enantiomeric ratio was carried out by high-performance liquid chromatography (HPLC) on a poly[(S)-N-(1-cydohexylethyl)methacrylamide] stationary phase. A significant increase in the rate of thalidomide racemization was observed in human citric plasma when compared with incubations in buffer. Further investigations using physiological concentrations of human serum albumin (HSA) in phosphate buffer (0.067 M, pH 7.4) demonstrated the influence of albumin on racemization. This observation was confirmed by inhibition experiments with capric acid anions.
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页码:235 / 240
页数:6
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