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第2楼2007/02/08
Investigations on the in vitro racemization of thalidomide by high-performance liquid chromatography*1
B. Knoche and G. Blaschke
Institute of Pharmaceutical Chemistry, University of Münster, Hittorfstrasse 58-62, D-48149 Münster Germany
Available online 26 November 2001.
Abstract
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-cyclohexylethyl)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.
*1 This study was presented in part at the 3rd International Symposium on Chiral Discrimination, Tübingen, October 1992.
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