匹美诺芬

应用制备生物活性体外研究体内研究匹美诺芬试剂级价格

匹美诺芬

CAS号:64622-45-3
英文名:Ibuprofen Piconol
中文名:匹美诺芬
CBNumber:CB9923096
分子式:C19H23NO2
分子量:297.4
MOL File:64622-45-3.mol

匹美诺芬化学性质

沸点 :438.9°C (rough estimate)
密度 :1.0971 (rough estimate)
折射率 :1.5000 (estimate)
储存条件 :Sealed in dry,Room Temperature
溶解度 :Acetone (Slightly), Chloroform (Slightly), Methanol (Sparingly)
形态 :Oil
酸度系数(pKa) :3.36±0.12(Predicted)
颜色 :Colourless

匹美诺芬性质、用途与生产工艺

应用布洛芬的消旋体拆分主要是以布洛芬甲酯为原料，经脂肪酶催化选择性水解，是有机合成的中间体和医药中间体，可用于实验室研发和化工医药合成过程中。
制备 3L三口反应瓶中加入DMF(1L)，2-氯甲基吡啶盐酸盐(144.3g)，碳酸钠(243g)，室温反应半小时。加入布洛芬钠(200g)，升温至60℃，反应24h，降至室温，抽滤，减压蒸干DMF，残留物用二氯甲烷溶解，水洗两次，无水硫酸钠干燥，抽滤，50℃蒸干得油状物210g，得到的油状物经过高真空蒸馏(170-172℃/0.133kPa)得到布洛芬吡甲酯纯品180g，HPLC纯度为99.7％。
生物活性 Ibuprofen piconol (U75630) 是一种非甾体抗炎药 (NSAID)，可局部缓解主要的热灼伤和晒伤。
体外研究

Ibuprofen piconol is a chemically stable, slightly hygroscopic liquid that strongly partitions into the oil phase and shows no indication of surface activity. This drug has very limited solubility in water (16.5 ppm), modest solubility in glycerol (16.4 mg/mL), and is miscible with less polar organics except for silicone fluids. Varying the initial concentration of ibuprofen piconol does not alter the hydrolysis half-life (concentration range from 50 to 200 μg/mL). The anticoagulant used alters the hydrolysis half-life. For plasma, the half-life is shortest when no anticoagulant is present (t _1/2 =2.5 h) and longer with the presence of anticoagulants; t _1/2 =8.0 h for citrate, t _1/2 =15.5 h for heparin and t _1/2 =161.8 h for EDTA. Red blood cell uptake of ibuprofen piconol is minimal and ranges from 0.4 to 4.1% over the ibuprofen piconol concentrations used in the study.
体内研究

When ibuprofen piconol is applied topically, only ibuprofen and its metabolites are observed in plasma and urine. The conversion of ibuprofen piconol to ibuprofen appears to be extremely rapid in vivo .