[Studies on the pharmacokinetic-pharmacodynamic model of ketoprofen beta-CD inclusion complex in rabbits].
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.
Lu
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W
Department of Pharmaceutics, School of Pharmaceutical Sciences, Beijing Medical University, Beijing 100083.
Tu
X
X
Wu
G
G
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry / Q000493:pharmacokinetics* / Q000494:pharmacology; D002851:Chromatography, High Pressure Liquid / Q000379:methods; D003505:Cyclodextrins / Q000737:chemistry / Q000493:pharmacokinetics* / Q000494:pharmacology; D005260:Female; D007660:Ketoprofen / Q000737:chemistry / Q000493:pharmacokinetics* / Q000494:pharmacology; D008297:Male; D011817:Rabbits; D047392:beta-Cyclodextrins
D000894:Anti-Inflammatory Agents, Non-Steroidal; D003505:Cyclodextrins; D047392:beta-Cyclodextrins; D007660:Ketoprofen; C031215:betadex