title: Pharmacokinetics of the gastroprokinetic agent mosapride citrate after single oral administration in horses.
abstract: The purpose of this study was to determine the pharmacokinetics and dose proportionality of mosapride citrate, a selective 5-HT4 agonist, after oral administration in horses. Seven healthy Thoroughbreds were dosed with distilled water and 0.5, 1.0, or 1.5 mg/kg mosapride citrate through a nasogastric tube. Serum mosapride concentrations were measured by a liquid chromatography/tandem mass spectrometry (LC/MS/MS) method. Mosapride showed the Cmaxs of 31, 60, and 104 ng/g and AUCs of 178, 357, and 566 ng.hr/g at doses of 0.5, 1.0, 1.5 mg/kg, respectively. The Cmaxs and AUCs increased in proportion to the dose, indicating linear pharmacokinetics of mosapride up to 1.5 mg/kg. The pharmacokinetic profiles of mosapride in horses are quite different from that in humans. The average t1/2 in horses was almost 2 fold longer than that reported in healthy adult humans. Therefore, it is thought that it is suitable to reduce the number of doses a day in horses compared to humans.
authors.affiliation: The United Graduate School of Veterinary Sciences, Gifu University, Gifu, Japan.
authors.forename: Koichi
authors.initials: K
authors.lastname: Okamura
authors.forename: Naoki
authors.initials: N
authors.lastname: Sasaki
authors.forename: Morito
authors.initials: M
authors.lastname: Fukunaka
authors.forename: Haruo
authors.initials: H
authors.lastname: Yamada
authors.forename: Hisashi
authors.initials: H
authors.lastname: Inokuma
mesh_terms: D000284:Administration, Oral; D000818:Animals; D019540:Area Under Curve; D001549:Benzamides / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D004305:Dose-Response Relationship, Drug; D005260:Female; D005765:Gastrointestinal Agents / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D006207:Half-Life; D006736:Horses; D007700:Kinetics; D008297:Male; D009025:Morpholines / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D009919:Orchiectomy / Q000662:veterinary
chemical_list: D001549:Benzamides; D005765:Gastrointestinal Agents; D009025:Morpholines; C062720:mosapride