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Pharmacokinetic behaviour of netobimin and its metabolites in sheep
Author(s) -
LANUSSE C. E.,
PRICHARD R. K.
Publication year - 1990
Publication title -
journal of veterinary pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.527
H-Index - 60
eISSN - 1365-2885
pISSN - 0140-7783
DOI - 10.1111/j.1365-2885.1990.tb00765.x
Subject(s) - pharmacokinetics , albendazole , urine , chemistry , area under the curve , metabolite , oral administration , pharmacology , high performance liquid chromatography , plasma concentration , chromatography , medicine , biochemistry , surgery
Lanusse, C.E. & Prichard, R.K. Pharmacokinetic behaviour of netobimin and its metabolites in sheep. J, vet. Pliarmacol. Therap. 13, 170–178. The pharmacokinetics and the profile of urine excretion of netobimin (NTB) and its metabolites were investigated after its intraruminal (i.r.) and subcutaneous (s.c.) administration to sheep at 20 mg/kg. Plasma and urine concentrations of NTB, albendazole (ABZ), albendazole sulphoxide (ABZSO) and albendazole sulphone (ABZSO 2 ) were measured serially over a 120‐h period by HPLC. NTB showed a similar pharmacokinetic profile in both treatments, being detected between 0.5 and 12 h post‐treatment, but the t max was achieved significantly earlier (P < 0.05) after s.c. treatment. ABZ was detected in plasma only after i.r. treatment, resulting in a low area under the curve ( AUC). The peak plasma concentration (C max ) and AUC for ABZSO and ABZSO 2 were significantly higher after i.r. administration of NTB. In both treatments, the ABZSO C max was reached earlier than the ABZSO 2 C max . The ratio of AUC ABZSO 2 :ABZSO was higher following s.c. administration (1.33) than following i.r. administration (0.35). The percentages of total dose excreted in the urine as NTB, ABZ, ABZSO and ABZSO 2 , were 17.05 (i.r.) and 8.16 (s.c). There was a less efficient conversion of NTB into ABZ metabolites after s.c. administration. The detection of ABZ in plasma and the high ABZSO AUC obtained after i.r. treatment may be of major importance for anthelmintic efficacy. C. E. Lanusse, Institute of Parasitology, McGill University, Macdonald College, 21 III Lakeshore Road, Ste‐Anne de Bellevue, Quebec, Canada H9X ICO.