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saterinone 外消旋体1-[4-氰基-1,2-二氢-6-甲基-2-氧代吡啶基-5)-苯氧基]-3-(4-(2-甲氧苯基)哌嗪-1]丙烷-2-醇,是治疗慢性心脏闭锁不全的新药,已在实验动物和人体进行了药动学研究。为了检查药理活性,合成了R-(+)(Ⅰ)和S-(-)(Ⅱ)对映体。近期有应用了灵敏方法测定体液中saterinone 外消旋体的报道。本文介绍用HPLC 法直接分离和测定其对映体纯度及服用外消旋体药物后人体血浆中对映体的比率。测定条件:合成样品用甲醇溶解并稀释到5μg/ml,直接进样;血浆样品取血浆1 ml加1 mol/L NaOH 50μl,用二氯甲烷3 ml萃取15 min 并离心10 min,将二氯甲烷层移入另一瓶中蒸干,用100μl 甲醇溶解进样。色谱条件:Chiralcel OD~(TM)柱250×4.6 mm
saterinone Racemic 1- [4-Cyano-1,2-dihydro-6-methyl-2-oxopyridyl-5-phenoxy] -3- Phenyl) piperazine-1] propan-2-ol, a new drug for the treatment of chronic cardiac insufficiency, has been studied pharmacokinetics in experimental animals and humans.In order to examine the pharmacological activity, R - (+) ) And S - (-) (Ⅱ) enantiomers.Recently, the sensitive method for the determination of saterinone in body fluids has been reported.In this paper, the separation and determination of the enantiomeric purity and the racemate The ratio of enantiomers in human plasma after the drug was measured.Determination conditions: The synthetic sample was dissolved in methanol and diluted to 5 μg / ml, and the sample was directly injected. Plasma samples were obtained by adding 1 ml of plasma and 1 ml of NaOH 50 μl, ml for 15 min and centrifuge for 10 min, transfer the dichloromethane layer to another vial and evaporate, and dissolve the sample in 100 μl of methanol. Chromatography conditions: Chiralcel OD ~ (TM) column 250 × 4.6 mm