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高效液相色谱法分离抗炎2-芳基丙酸酯对映体:该方法用于体外代谢研究的适用性

High-performance liquid chromatographic separation of the enantiomers of anti-inflammatory 2-arylpropionates: suitability of the method for in vitro metabolic studies.

作者信息

Maître J M, Boss G, Testa B

出版信息

J Chromatogr. 1984 Sep 21;299(2):397-403. doi: 10.1016/s0021-9673(01)97855-0.

DOI:10.1016/s0021-9673(01)97855-0
PMID:6501476
Abstract

The enantiomers of 2-phenylpropionic acid, 2-(2-naphthyl)propionic acid, 2-(4-biphenyl)propionic acid and six anti-inflammatory congeners were separated by high-performance liquid chromatography via their diastereoisomeric derivatives with (S)-(-)-1-phenylethylamine. In agreement with a general rule, the diastereoisomers derived from the (R)-acids are less polar and elute first. Structural factors influencing the resolution are discussed. Good calibrations were obtained for R/S ratios and total (R + S) concentrations of flurbiprofen and naproxen added to inactivated rat liver preparations. The method is suitable for in vitro metabolic studies of chiral 2-arylpropionates.

摘要

通过与(S)-(-)-1-苯乙胺形成非对映体衍生物,利用高效液相色谱法分离了2-苯丙酸、2-(2-萘基)丙酸、2-(4-联苯基)丙酸的对映体以及六种抗炎同系物。与一般规律一致,由(R)-酸衍生的非对映体极性较小,先被洗脱。讨论了影响拆分的结构因素。对于添加到灭活大鼠肝脏制剂中的氟比洛芬和萘普生的R/S比值和总(R+S)浓度,获得了良好的校准曲线。该方法适用于手性2-芳基丙酸酯的体外代谢研究。

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High-performance liquid chromatographic separation of the enantiomers of anti-inflammatory 2-arylpropionates: suitability of the method for in vitro metabolic studies.高效液相色谱法分离抗炎2-芳基丙酸酯对映体:该方法用于体外代谢研究的适用性
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Clinical pharmacokinetics of flurbiprofen and its enantiomers.氟比洛芬及其对映体的临床药代动力学。
Clin Pharmacokinet. 1995 Feb;28(2):100-14. doi: 10.2165/00003088-199528020-00002.
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Chromatographic separation of enantiomers.对映体的色谱分离。
Pharm Weekbl Sci. 1988 Feb 19;10(1):1-11. doi: 10.1007/BF01966428.
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The pharmacokinetics of the enantiomers of flurbiprofen in patients with rheumatoid arthritis.氟比洛芬对映体在类风湿性关节炎患者中的药代动力学。
Br J Clin Pharmacol. 1991 Jan;31(1):102-4. doi: 10.1111/j.1365-2125.1991.tb03865.x.