Preparation and evaluation of cefquinome-loaded gelatin microspheres and the pharmacokinetics in pigs.
J Vet Pharmacol Ther
; 41(1): 117-124, 2018 Feb.
Article
em En
| MEDLINE
| ID: mdl-28656695
Cefquinome (CEF) is widely used for veterinary clinical applications because of its broad spectrum and high efficiency. However, frequent administrations are required due to its short elimination half-life. In this study, cefquinome sulfate gelatin microspheres (CEF-GMS) were prepared as a sustained-release formulation using emulsion chemical cross-linking technique. Physical properties, stability, sustained-release property in vitro, and pharmacokinetics in pigs were assessed. The morphology of CEF-GMS showed a good sphericity with porous structure on the surface, and the mean diameter was 8.80 ± 0.78 µm, with 90.60 ± 3.98% of the total in the range of 5-20 µm. There were no significant changes of all estimated indexes in the stability tests. In vitro drug release study showed that the release of CEF from CEF-GMS was much slower than that from crude CEF in a release medium. Pharmacokinetic characteristics were evaluated following intramuscular administration of CEF-GMS or Cefquinome sulfate injection (CEF-Inj) in pigs at a dosage of 4 mg CEF/kg body weight. The plasma drug concentration-time data of CEF-GMS and CEF-Inj were both best fitted by two-compartment models with first-order absorption, and the elimination half-life of CEF-GMS was almost 10 times that of CEF-Inj. Overall, CEF-GMS might be used as a sustained-release formulation of CEF for veterinary clinical applications.
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Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Cefalosporinas
/
Antibacterianos
Tipo de estudo:
Prognostic_studies
Limite:
Animals
Idioma:
En
Ano de publicação:
2018
Tipo de documento:
Article