Cho Woon-Ki, Seo Hyewon, Choi Sung Heum, Kwak Hyun Jeong, Cheon Hyae Gyeong, Jeon Dong Ju, Kim Sang Kyum, Bae Myung Ae, Song Jin Sook
Drug Discovery Platform Technology Group, Drug Discovery Division, Korea Research Institute of Chemical Technology, Daejeon, Republic of Korea; College of Pharmacy, ChungNam National University, Daejeon, Republic of Korea.
Biomed Chromatogr. 2015 Mar;29(3):321-4. doi: 10.1002/bmc.3280. Epub 2014 Jul 26.
A method for determining a novel phosphodiesterase-4 inhibitor, 3-[1-(3cyclopropylmethoxy-4-difluoromethoxybenzyl)-1H-pyrazol-3-yl]-benzoic acid (PDE-423), in rat plasma was developed and validated using liquid chromatography-tandem mass spectrometry for further pharmacokinetic study for development as a novel anti-asthmatic drug. PDE-423 in the concentration range of 0.02-10 µg/mL was linear with a correlation coefficient of >0.99, and the mean intra- and inter-assay precisions of the assay were 7.50 and 3.86%, respectively. The validated method was used successfully for a pharmacokinetic study of PDE-423 in rats.
建立了一种使用液相色谱-串联质谱法测定大鼠血浆中新型磷酸二酯酶-4抑制剂3-[1-(3-环丙基甲氧基-4-二氟甲氧基苄基)-1H-吡唑-3-基]-苯甲酸(PDE-423)的方法，并进行了验证，以用于其作为新型抗哮喘药物开发的进一步药代动力学研究。浓度范围为0.02-10μg/mL的PDE-423呈线性，相关系数>0.99，该测定方法的批内和批间平均精密度分别为7.50%和3.86%。验证后的方法成功用于PDE-423在大鼠体内的药代动力学研究。
