A novel β-cyclodextrin derivative, 2, 6-di-O-butyl-3-O-acetyl-β-cyclodex- trin, was prepared and used as chiral stationary phase for capillary gas chromato- graphic resolution of enantiomers, lhe glass capillary col...A novel β-cyclodextrin derivative, 2, 6-di-O-butyl-3-O-acetyl-β-cyclodex- trin, was prepared and used as chiral stationary phase for capillary gas chromato- graphic resolution of enantiomers, lhe glass capillary columns with the derivative having low melting point and high thermal stability could produce more than 3000 plates per column meter and have proven to be good chlral columns to separate the enantiomers of some amino acids, derivatives of epoxy ethane and alkyl halide, etc.展开更多
Stereoselectivity in drug metabolism can not only influence the pharmacological activities, tolerability, safety, and bioavailability of drugs directly, but also cause different kinds of drug-drug interactions. Thus, ...Stereoselectivity in drug metabolism can not only influence the pharmacological activities, tolerability, safety, and bioavailability of drugs directly, but also cause different kinds of drug-drug interactions. Thus, assessing stereoselectivity in drug metabolism is of great significance for pharmaceutical research and development （R＆D） and rational use in clinic. Although there are various methods available for assessing stereoselectivity in drug metabolism, many of them have shortcomings. The indirect method of chro- matographic methods can only be applicable to specific samples with functional groups to be derivatized or form complex with a chiral selector, while the direct method achieved by chiral stationary phases （CSPs） is expensive. As a detector of chromatographic methods, mass spectrometry （MS） is highly sen- sitive and specific, whereas the matrix interference is still a challenge to overcome. In addition, the use of nuclear magnetic resonance （NMR） and immunoassay in chiral analysis are worth noting. This review presents several typical examples of drug stereoselective metabolism and provides a literature-based evaluation on current chiral analytical techniques to show the significance and challenges of stereo- selectivity assessing methods in drug metabolism.展开更多
In this paper,the concept of reversed-or normal-phase chiral stationary phase liquid chromatography has been put forward according to the polar strength of mobile and stationary phases. The statistical model developed...In this paper,the concept of reversed-or normal-phase chiral stationary phase liquid chromatography has been put forward according to the polar strength of mobile and stationary phases. The statistical model developed in HPLC has been used to investigate the separation mechanism of D-and L-enantiomer in chiral stationary phase liquid chromatography.It has been observed that the variation of capacity factor of enantiomers with mobile phase composition in both reversed-phase and normal-phase chiral stationary phase liquid chromatography can be described by the fundamental elution equation lnk'=a+blnC_b+cC_b.The effect of mobile phase composition on the selec- tivity of enantiomers D and L in normal-phase chiral stationary phase liquid chromatography cam be described by the equation lnα=⊿a+⊿blnC_b,but in reversed-phase chiral stationary phase liquid chromatography the selectivity is almost independant of the mobile phase composition.展开更多
文摘A novel β-cyclodextrin derivative, 2, 6-di-O-butyl-3-O-acetyl-β-cyclodex- trin, was prepared and used as chiral stationary phase for capillary gas chromato- graphic resolution of enantiomers, lhe glass capillary columns with the derivative having low melting point and high thermal stability could produce more than 3000 plates per column meter and have proven to be good chlral columns to separate the enantiomers of some amino acids, derivatives of epoxy ethane and alkyl halide, etc.
基金financial support from the National Major Projects of China(2011CB710800)the International Science&Technology Cooperation Program of China(2014DFE30050)the Program for Zhejiang Leading Team of S&T Innovation(2011R50014)
文摘Stereoselectivity in drug metabolism can not only influence the pharmacological activities, tolerability, safety, and bioavailability of drugs directly, but also cause different kinds of drug-drug interactions. Thus, assessing stereoselectivity in drug metabolism is of great significance for pharmaceutical research and development （R＆D） and rational use in clinic. Although there are various methods available for assessing stereoselectivity in drug metabolism, many of them have shortcomings. The indirect method of chro- matographic methods can only be applicable to specific samples with functional groups to be derivatized or form complex with a chiral selector, while the direct method achieved by chiral stationary phases （CSPs） is expensive. As a detector of chromatographic methods, mass spectrometry （MS） is highly sen- sitive and specific, whereas the matrix interference is still a challenge to overcome. In addition, the use of nuclear magnetic resonance （NMR） and immunoassay in chiral analysis are worth noting. This review presents several typical examples of drug stereoselective metabolism and provides a literature-based evaluation on current chiral analytical techniques to show the significance and challenges of stereo- selectivity assessing methods in drug metabolism.
基金This work was supported by the National Natural Science Foundation of China.
文摘In this paper,the concept of reversed-or normal-phase chiral stationary phase liquid chromatography has been put forward according to the polar strength of mobile and stationary phases. The statistical model developed in HPLC has been used to investigate the separation mechanism of D-and L-enantiomer in chiral stationary phase liquid chromatography.It has been observed that the variation of capacity factor of enantiomers with mobile phase composition in both reversed-phase and normal-phase chiral stationary phase liquid chromatography can be described by the fundamental elution equation lnk'=a+blnC_b+cC_b.The effect of mobile phase composition on the selec- tivity of enantiomers D and L in normal-phase chiral stationary phase liquid chromatography cam be described by the equation lnα=⊿a+⊿blnC_b,but in reversed-phase chiral stationary phase liquid chromatography the selectivity is almost independant of the mobile phase composition.
