Lu W, Tu X, Wu G
Department of Pharmaceutics, School of Pharmaceutical Sciences, Beijing Medical University, Beijing 100083.
Yao Xue Xue Bao. 1998 Nov;33(11):855-9.
A simple HPLC-UV method was established to determine concentrations of ketoprofen (KP) in rabbit plasma following oral administration. Twelve rabbits were selected and divided into three groups. KP beta-CD inclusion complex suspension, KP entity suspension (in 0.5% CMC-Na) and 0.5% CMC-Na suspension (as a placebo group) were administered orally to the three groups of rabbits, respectively. Differences in the pharmacokinetics-pharmacodynamics (PK-PD) parameters between KP beta-CD inclusion complex and KP entity were examined. The results indicate that the established HPLC-UV method could be used to assay the concentrations of KP in rabbit plasma with good precision. The distribution phase T1/2 alpha of the complexated KP was 0.4 h, while that of the KP entity was 0.56 h, KP in beta-CD inclusion complex could be absorbed more rapidly. The early effect values of the KP inclusion complex were higher than those of the KP entity. The maximal antipyretic effect occurred after the peak of plasma concentration. The phenomenon indicates that the effect compartment of ketoprofen is in the peripheral compartment.
建立了一种简单的高效液相色谱-紫外法,用于测定家兔口服给药后血浆中酮洛芬(KP)的浓度。选取12只家兔,分为三组。分别给三组家兔口服KP-β-环糊精包合物混悬液、KP原料药混悬液(溶于0.5%羧甲基纤维素钠)和0.5%羧甲基纤维素钠混悬液(作为安慰剂组)。考察了KP-β-环糊精包合物与KP原料药之间药代动力学-药效学(PK-PD)参数的差异。结果表明,所建立的高效液相色谱-紫外法可用于测定家兔血浆中KP的浓度,精密度良好。包合后KP的分布相T1/2α为0.4小时,而KP原料药的为0.56小时,β-环糊精包合物中的KP吸收更快。KP包合物的早期效应值高于KP原料药。最大解热效应出现在血浆浓度峰值之后。该现象表明酮洛芬的效应室在外周室。