• YAKHAK HOEJI
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• v.53 no.2
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• pp.60-68
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• 2009

In terms of chiral issue, two enantiomers of chiral drugs often differ significantly in their pharmacological, toxicological and pharmacokinetic profile. Chiral switches of racemic drugs have been redeveloped as single enantiomers. Several chiral resolution techniques in chirotechnology are introduced and the most used chiral HPLC chromatographic method among several chiral analysis techniques is described with its several advantages. Several types of chiral HPLC columns derived from their chiral selectors are discussed with their property and applications for enantiomer separation.

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.167-168
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• 2002

Because of the differences between biological and pharmacological properties of chiral drugs in human body, accurate determinations of their optical purities have been in great need. There are two major approaches in chiral separation: indirect method performed under achiral condition, and direct method under the chiral environment. We have been conducting chiral separation of acidic chiral compounds and also amino acidic chiral compounds employing indirect GC methods and direct CE enantiomeric separation methods. (omitted)

• KSBB Journal
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• v.15 no.5
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• pp.415-422
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• 2000

Enzymatic resolution is becoming increasingly important in the production of optically active pharmaceutical drugs and is now challenging the traditional synthetic methods for production of a variety of chiral intermediates and products. This article reviews the recent advances in chirotechnology using enzymes as a catalyst to resolve chiral compounds. The review focuses on the recent trends in chirotechnology and the application of enzymes to the production of industrially valuable pharmaceutical drugs.

• Archives of Pharmacal Research
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• v.27 no.10
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• pp.1009-1015
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• 2004

Quantitative Structure-Resolution Relationship (QSRR) using the Comparative Molecular Field Analysis (CoMFA) software was applied to predict the chromatographic behaviors of chiral drugs with an amine moiety on the chiral cellobiohydrolase (CBH) columns. As a result of the Quantitative CoMFA-Resolution Relationship study, using the partial least square method, prediction of the behavior of drugs with amine moiety upon chiral separation became possible from their three dimensional molecular structures. When a mixed mobile phase of 10 mM aqueous phosphate buffer (pH 7.0) - isopropanol (95 : 5) was employed, the best Quantitative CoMFA-Resolution Relationship, derived from the study, provided a cross-validated $q^2$ = 0.933, a normal $r^2$ = 0.995, while the best Quantitative CoMFA-Separation Factor Relationship, also derived from the study, yielded a cross-validated $q^2$ = 0.939, a normal $r^2$ = 0.991. When all of these results are considered, this QSRR-CoMFA analysis appears to be a very useful tool for the preliminary prediction on the chromatographic behaviors of drugs with an amine moiety inside chiral CBH columns.

• Bulletin of the Korean Chemical Society
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• v.25 no.5
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• pp.747-750
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• 2004

• Journal of Pharmaceutical Investigation
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• v.35 no.1
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• pp.57-63
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• 2005

Numerous drugs are chiral because they possess one or more chiral centers. Enantiomers may differ in their pharmacokinetic, pharmacological and toxicological properties. However, the significance of stereochemistry of drugs in their therapeutic uses has received relatively little attention until recently. The US FDA issued a guideline on stereoisomeric drugs in 1992, and the European agency describes tests for new drug substances which are optically active in an ICH(International Conference of Harmonization) guideline. According to the guidance, enantiomers may differ in their pharmacokinetic, pharmacological and toxicological properties. Therefore, in this paper, we examined the recently published Canadian guidance, stereochemical issues in chiral drug development, which will be references to make a guidance on stereochemical issues in chiral drug development in Korea.

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.165-166
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• 2002

• Bulletin of the Korean Chemical Society
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• v.8 no.1
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• pp.45-47
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• 1987

After conversion to their 3,5-dinitrobenzoyl or 3,5-dinitroanilide derivatives, the enantiomers of a number of drugs may be chromatographically separated on various ${\alpha}$-arylalkylamine-derived chiral stationary phases (CSPs). While each CSP used in this study is useful, CSP 1 is best able to resolve the 3,5-dinitroanilide derivative of Ibuprofen while CSP 9 generally gives rather large ${\alpha}$ values for the resolution of 3,5-dinitrobenzoyl derivatives of the enantiomers of ${\beta}$-adrenergic blocking drugs.

• Clean Technology
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• v.22 no.2
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• pp.75-81
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• 2016

As the quality of life has improved, the desire for the safety and quality of the foods and drugs has been gradually increasing. For safety and quality management in foods, drugs, health management, agriculture, environmental conservation, and the industrial fields, the demand for quickly and accurately measuring various chemicals has been increasing. As well, the desire for self-diagnosis of one's own health state and self-examining the safety of environment has been gradually increasing. Optical Isomers can have very different physiological effects on human beings. One isomer can exhibit desirable pharmacological, pharmacodynamic, pharmacokinetic and physiological properties, while the other isomer can exhibit undesirable and toxic properties toward living organisms, especially human beings. And they can exhibit different activities in chemical and biotechnological processes. Although the majority of commercially available drugs are now both synthetic and chiral materials, a most chiral drugs are still marketed as racemic drugs. Thus, to avoid possible undesirable side effects from chiral drugs, more effective methods for separating and recognizing chiral compounds are urgently needed. In this report, we investigated the overall developing trends of the chiral drug separation and analysis technology by using molecular recognition.

• Proceedings of the PSK Conference
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• 2003.04a
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• pp.278.3-279
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• 2003

A chiral stationary phase (CSP) prepared by bonding (18-crown-6)-2,3,11,12-tetracarboxylic acid (18-C-6-TA) to aminopropyl silica gel by HPLC was used in resolving several racemic drugs containing primary amino moiety. Most compounds used in this study were resolved on the CSP using 80％ methanol in water (V/V) containing 10mM sulfuric acid as a mobile phase. These results on the CSP were compared to those on the similar CSP derived from 18-C-6-TA of the same chiral selector by different connecting method.