Pharmacokinetics and pharmacodynamics of a new reformulated microemulsion and the long-chain triglyceride emulsion of propofol in beagle dogs.

British Journal of Pharmacology
S-H LeeG-J Noh

Abstract

Microemulsion propofol was developed to eliminate lipid solvent-related adverse events of long-chain triglyceride emulsion (LCT) propofol. We compared dose proportionality, pharmacokinetic and pharmacodynamic characteristics of both formulations. The study was a randomized, two-period and crossover design with 7-day wash-out period. Microemulsion and LCT propofol were administered by zero-order infusion (0.75, 1.00 and 1.25 mg kg(-1) min(-1)) for 20 min in 30 beagle dogs (male/female = 5/5 for each rate). Arterial samples were collected at preset intervals. The electroencephalographic approximate entropy (ApEn) was used as a measure of propofol effect. Dose proportionality, pharmacokinetic and pharmacodynamic bioequivalence were evaluated by non-compartmental analyses. Population analysis was performed using nonlinear mixed effects modelling. Both formulations showed dose proportionality at the applied dose range. The ratios of geometric means of AUC(last) and AUC(inf) between both formulations were acceptable for bioequivalence, whereas that of C(max) was not. The pharmacodynamic bioequivalence was indicated by the arithmetic means of AAC (areas above the ApEn time curves) and E(0) (baseline ApEn)-E(max) (maximally decreased A...Continue Reading

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Citations

Nov 29, 2014·Veterinary Medicine International·Ana Paula PradosMarcela Rebuelto
Aug 26, 2014·Journal of Pharmacokinetics and Pharmacodynamics·Soo-Han LeeGyu-Jeong Noh
Jul 31, 2013·The Veterinary Clinics of North America. Small Animal Practice·Michael H Court
Mar 1, 2015·Journal of Pharmacokinetics and Pharmacodynamics·Byung-Moon ChoiGyu-Jeong Noh
Feb 1, 2012·The Journal of International Medical Research·Y-J ChaeH-B Cho
Mar 11, 2011·Korean journal of anesthesiology·Dong Hun ChungHee-Kyung Jo

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