Pharmacokinetic Pattern of Menbutone in Calves after Single Intravenous and Intramuscular Administration

[EN] Menbutone is a choleretic agent currently used in Europe to treat digestive disorders in livestock and dogs. Pharmacokinetic parameters were established in 4-month Holstein calves after intravenous (IV) and intramuscular (IM) administration. The drug was administered to 12 animals (10 mg/kg) fo...

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Bibliographic Details
Authors: Díez Láiz, Raquel, Rodríguez Lago, José Manuel, López Cadenas, Cristina, Puente García, Raúl de la, Sierra Vega, Matilde, Diez Liébana, María José, Fernández Martínez, María Nélida, García Viéitez, Juan José, Sahagún Prieto, Ana María
Format: article
Status:Published version
Publication Date:2024
Country:España
Institution:Universidad de León
Repository:BULERIA. Repositorio Institucional de la Universidad de León
OAI Identifier:oai:buleria.unileon.es:10612/22560
Online Access:https://www.mdpi.com/2076-2615/14/17/2540
https://hdl.handle.net/10612/22560
Access Level:Open access
Keyword:Farmacología
Veterinaria
Choleretic
Intramuscular
Intravenous
Menbutone
Pharmacokinetics
Calves
Description
Summary:[EN] Menbutone is a choleretic agent currently used in Europe to treat digestive disorders in livestock and dogs. Pharmacokinetic parameters were established in 4-month Holstein calves after intravenous (IV) and intramuscular (IM) administration. The drug was administered to 12 animals (10 mg/kg) for both IV and IM routes following a crossover design. Plasma samples were collected at various time points over 24 h and analyzed by reverse-phase high-performance liquid chromatography with a photodiode-array detector, following a method validated according to European Medicines Agency guidelines. Pharmacokinetic parameters were calculated using compartmental and non-compartmental methods. Menbutone followed a two-compartment open model after IV injection, with a total clearance (Cl) of 71.9 ± 13.5 mL/h/kg, an elimination half-life (t½β) of 4.53 ± 2.45 h, and a volume of distribution at steady-state (Vss) of 310.4 ± 106.4 mL/kg. Non-compartmental elimination half-life (t½λ) was 4.2 ± 1.1 h. After IM administration, drug pharmacokinetics was best described by a one-compartment open model. The peak plasma concentration (Cmax) was 15.1 ± 4.3 µg/mL; the time to reach Cmax (tmax), 1.66 ± 0.55 h; and the mean absorption time (MAT), 2.50 ± 1.42 h. Absorption was high, with a fraction of the dose absorbed (F) of 83.5 ± 22.4%. Menbutone was rapidly eliminated from plasma for both routes of administration, with a fast and high IM bioavailability.