Pharmacokinetics of a high-concentration formulation of buprenorphine (Simbadol) in male dogs.
Vet Anaesth Analg
; 48(4): 509-516, 2021 Jul.
Article
em En
| MEDLINE
| ID: mdl-34059460
OBJECTIVE: To describe the pharmacokinetics of buprenorphine in dogs following administration of a high-concentration formulation of buprenorphine. STUDY DESIGN: Prospective, randomized, crossover study. ANIMALS: A total of six healthy male intact Beagle dogs, aged 9-13 months and weighing 10.3 ± 1.4 kg (mean ± standard deviation). METHODS: Dogs were randomized to be administered buprenorphine (0.12 mg kg-1; Simbadol, 1.8 mg mL-1) via the intravenous (lateral saphenous) or subcutaneous (dorsal interscapular) route followed by the alternative route of administration after a 14 day interval. Blood was sampled before administration and at set times up to 72 hours after injection. Plasma buprenorphine concentration was measured using liquid chromatography-tandem mass spectrometry. RESULTS: A three-compartment model with zero or biphasic rapid and slow first-order input in (intravenous or subcutaneous data, respectively) and first-order elimination from the central compartment best fitted the data. The rapid first-order input accounted for 63% of the dosage absorption. Typical values (% interindividual variability) for the three compartment volumes were 900 (33), 2425 (not estimated) and 6360 (28) mL kg-1. The metabolic and two distribution clearances were 25.7 (21), 107.5 (74) and 5.7 (61) mL minute-1 kg-1. The absorption half-life for the fast absorption phase was 8.9 minutes with a 0.7 (103) minute delay. The absorption half-life for the slow absorption phase was 347 minutes with a 226 (42) minute delay. Median (range) bioavailability calculated from noncompartmental analysis was 143 (80-239)%. Calculated terminal half-life was 963 minutes. CONCLUSIONS AND CLINICAL RELEVANCE: The high-concentration formulation of buprenorphine administered subcutaneously had a large volume of distribution and a rapid absorption phase followed by slower, delayed absorption. The high estimate of bioavailability should be interpreted with caution as values above 100% are most commonly related to experimental issues.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Buprenorfina
/
Cães
Tipo de estudo:
Observational_studies
Limite:
Animals
Idioma:
En
Revista:
Vet Anaesth Analg
Assunto da revista:
ANESTESIOLOGIA
/
MEDICINA VETERINARIA
Ano de publicação:
2021
Tipo de documento:
Article
País de afiliação:
Estados Unidos