唑类抗真菌药物手性分离及药代动力学研究进展

郭凯欣; 石宽; 闻俊; 周婷婷; 范国荣

doi:10.3969/j.issn.1006-0111.2012.06.006

唑类抗真菌药物手性分离及药代动力学研究进展

doi: 10.3969/j.issn.1006-0111.2012.06.006

1.
第二军医大学药学院药物分析学教研室, 上海 200433;解放军75215部队卫生队, 广东惠州 516133
2.
第二军医大学药学院药物分析学教研室, 上海 200433;解放军95890部队卫生队, 湖北武汉 434000
3.
第二军医大学药学院药物分析学教研室, 上海 200433;上海市药物(中药)代谢产物研究重点实验室, 上海 200433

基金项目: 国家自然科学基金(81001420),上海市教委重点课程建设项目(药物分析学).

Advance in chiral separation and stereo selectivity pharmacokinetics of azole antifungal drugs

1.
School of Pharmacy, Second Military Medical University, Shanghai 200433, China;Medical Team, 75215 Force, Huizhou 516133, China
2.
School of Pharmacy, Second Military Medical University, Shanghai 200433, China;Medical Team, 95890 Force, Wuhan 434000, China
3.
School of Pharmacy, Second Military Medical University, Shanghai 200433, China;Shanghai Key Laboratory for Pharmaceutical Metabolite Research, Shanghai 200433, China

摘要: 唑类抗真菌药物具有手性特征,给药后体内对映体血药浓度及药动学参数显示出差异,具有立体选择性特点,代谢是导致该类药物呈现立体选择性变化的主要环节。而生物样本中对映体定量分析则依赖于手性拆分技术的不断发展。本文综述了近年来唑类抗真菌药物主要手性分析技术及酮康唑、伊曲康唑手性药代动力学研究进展,以期为唑类抗真菌新药研究提供参考。
- 唑类抗真菌药物 /
- 手性分离 /
- 药代动力学 /
- 立体选择性
Abstract: Generally azole antifungal drugs possessed chiral center. After administration of the racemate, the results indicated the differences in plasma concentrations and pharmacokinetic parameters between enantiomers were stereoselctive. The metabolism might be mainly responsible for the chiral pharmacikinetics of the enantiomers. The quantitation of enantiomers in biological matrix was based on the development of chiral separation techniques. In this paper, the chiral separation techniques of these agents and the advance in chiral pharmacokinetics of ketoconazole and itraconazole were reviewed, which could provide some references to the discovery of azole antifungal new agents.
- antifungal drugs /
- chiral separation /
- pharmacokinetics /
- stereo selectivity

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唑类抗真菌药物手性分离及药代动力学研究进展

doi: 10.3969/j.issn.1006-0111.2012.06.006

Advance in chiral separation and stereo selectivity pharmacokinetics of azole antifungal drugs

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唑类抗真菌药物手性分离及药代动力学研究进展

doi: 10.3969/j.issn.1006-0111.2012.06.006

English Abstract

Advance in chiral separation and stereo selectivity pharmacokinetics of azole antifungal drugs

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唑类抗真菌药物手性分离及药代动力学研究进展

doi: 10.3969/j.issn.1006-0111.2012.06.006

Advance in chiral separation and stereo selectivity pharmacokinetics of azole antifungal drugs

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唑类抗真菌药物手性分离及药代动力学研究进展

doi: 10.3969/j.issn.1006-0111.2012.06.006

English Abstract

Advance in chiral separation and stereo selectivity pharmacokinetics of azole antifungal drugs

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目录