A method for the assay of R ( ) and S (+) mexiletine in rat liver microsomal incubates was developed. The method involved extraction of mexiletine from the microsomal incubates, and formation of mexiletine diast...A method for the assay of R ( ) and S (+) mexiletine in rat liver microsomal incubates was developed. The method involved extraction of mexiletine from the microsomal incubates, and formation of mexiletine diastereomeric derivatives with a chiral reagent S ( ) N trifluoroacetyl prolyl chloride. Separation and quantitation of the diastereomeric mexiletine derivatives were carried out by a capillary gas chromatographic system with flame ionization detection. The assay was linear from 5 to 500 μg/ml for each enantiomer. The average recoveries of analytical method were 93 31±5 59% and 93 10±5 11% for R ( ) and S (+) mexiletine, respectively. The limits of detection and quantitation for the method were 1 0 μg/ml and 5 0 μg/ml for the R ( ) and S (+) mexiletine isomers, respectively. The reproducibility in the assay was better than 16.5% (RSD). The method has been applied to the metabolism study of R ( ) and S (+) mexiletine in rat liver microsomal incubates.展开更多
Aim To establish a capillary electrophoresis method for enantiomericseparation of meptazinol hydrochlo-ride. Methods The separation conditions such ascyclodextrin(CD)type, buffer pH, concentration of 2,3,6-O-trimethyl...Aim To establish a capillary electrophoresis method for enantiomericseparation of meptazinol hydrochlo-ride. Methods The separation conditions such ascyclodextrin(CD)type, buffer pH, concentration of 2,3,6-O-trimethyl-β-cyclodextrin and organicadditives were optimized. An optimum concentration was 30 mmol· L^(-1) phosphate (pH 7.02) with 10%(W/V) TM-β-CD and 2% acetonitrile. Results Baseline resolution of the enantiomer was readilyachieved using 2, 3, 6-O-trimethyl-β-cyclodextrin. Conclusion This is a convenient method for fastenantiomeric resolution of meptazinol hydrochloride.展开更多
文摘A method for the assay of R ( ) and S (+) mexiletine in rat liver microsomal incubates was developed. The method involved extraction of mexiletine from the microsomal incubates, and formation of mexiletine diastereomeric derivatives with a chiral reagent S ( ) N trifluoroacetyl prolyl chloride. Separation and quantitation of the diastereomeric mexiletine derivatives were carried out by a capillary gas chromatographic system with flame ionization detection. The assay was linear from 5 to 500 μg/ml for each enantiomer. The average recoveries of analytical method were 93 31±5 59% and 93 10±5 11% for R ( ) and S (+) mexiletine, respectively. The limits of detection and quantitation for the method were 1 0 μg/ml and 5 0 μg/ml for the R ( ) and S (+) mexiletine isomers, respectively. The reproducibility in the assay was better than 16.5% (RSD). The method has been applied to the metabolism study of R ( ) and S (+) mexiletine in rat liver microsomal incubates.
文摘Aim To establish a capillary electrophoresis method for enantiomericseparation of meptazinol hydrochlo-ride. Methods The separation conditions such ascyclodextrin(CD)type, buffer pH, concentration of 2,3,6-O-trimethyl-β-cyclodextrin and organicadditives were optimized. An optimum concentration was 30 mmol· L^(-1) phosphate (pH 7.02) with 10%(W/V) TM-β-CD and 2% acetonitrile. Results Baseline resolution of the enantiomer was readilyachieved using 2, 3, 6-O-trimethyl-β-cyclodextrin. Conclusion This is a convenient method for fastenantiomeric resolution of meptazinol hydrochloride.
