title: Intramuscular bioavailability of ketoprofen lysine salt in horses.
abstract: Lysine salts are often used in human pharmaceuticals to increase the solubility and absorption of acidic drugs when these are administered parenterally. In this study the intramuscular bioavailability of ketoprofen administered as the lysine salt was evaluated in horses (n = 5) treated intravenously and intramuscularly (2.2 mg/kg active substance) in a cross-over study. The absorption rate of ketoprofen administered as the lysine salt was rather low: the mean residence time increased from 31.7 min after IV injection to 128.9 min (after IM injection), and the bioavailability was high (mean 92.4%). The calculated steady state plasma concentrations of ketoprofen during multiple dosage were much higher after intramuscular (0.106 g/ml) than after intravenous (0.066 microgram/ml) administration. Intramuscular injections of the ketoprofen lysine salt can therefore be given to horses, which are particularly prone to develop soft tissue reactions, since use of the lysine salt markedly reduced local irritation at the injection site.
authors.affiliation: Department of Public Veterinary Health and Animal Pathology, Faculty of Veterinary Medicine, University of Bologna, Italy.
authors.forename: P
authors.initials: P
authors.lastname: Anfossi
authors.forename: R
authors.initials: R
authors.lastname: Villa
authors.forename: C
authors.initials: C
authors.lastname: Montesissa
authors.forename: S
authors.initials: S
authors.lastname: Carli
mesh_terms: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000493:pharmacokinetics*; D019540:Area Under Curve; D001682:Biological Availability; D018592:Cross-Over Studies; D005260:Female; D006207:Half-Life; D006736:Horses; D007273:Injections, Intramuscular; D007275:Injections, Intravenous; D007660:Ketoprofen / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D008239:Lysine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000493:pharmacokinetics
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; C029946:ketoprofen lysine; D007660:Ketoprofen; D008239:Lysine