학술논문

Pharmacokinetic and pharmacodynamic effects of 2 registered omeprazole preparations and varying dose rates in horses
Document Type
article
Source
Journal of Veterinary Internal Medicine, Vol 35, Iss 1, Pp 620-631 (2021)
Subject
bioavailability
enteric‐coated omeprazole
gastric ulcer healing
gastric ulcers
Veterinary medicine
SF600-1100
Language
English
ISSN
1939-1676
0891-6640
Abstract
Abstract Background Omeprazole preparations vary in bioavailability in horses. Hypothesis/Objectives To characterize the pharmacokinetics and pharmacodynamics of an existing enteric‐coated oral omeprazole paste (REF) and a novel, in‐feed, enteric‐coated dry granule preparation (NOV). Animals Twelve Standardbred/Thoroughbred mares free from clinical disease. Methods A prospective, blinded randomized interventional study was trial, conducted in 3 parts: (a) bioavailability study, (b) dose titration study, and (c) comparative clinical pharmacodynamic study, each using a blocked crossover design. Results Consistent with the larger dose administered, Cmax (median, 1032 ng/mL; range, 576‐1766) and AUC0‐24 (median, 63.9 μg/mL*min; range, 42.4‐152.4) were greater after single oral administration of NOV than REF (282.7 ng/mL; range, 94.8‐390.2, and 319 23.8 μg/mL*min; range, 8.2‐42.3, respectively; both P = .004). No differences were observed between products for absolute oral bioavailability (NOV 55% range, 15‐88; REF 17% range, 10‐77; P = .25). Treatment with both preparations was associated with reduced gastric squamous ulcer scores and increased pH of gastric fluid. Bioequivalence was demonstrated for pharmacodynamic measures with the exception of % time pH