Comparative pharmacokinetics and bioavailability of albendazole sulfoxide in sheep and goats, and dose-dependent plasma disposition in goats

BMC Veterinary Research

Cengiz Gokbulut¹  Erol Ayaz⁴  Veli Yilgor Cirak²  Murat Boyacioğlu⁵  Selim Sekkin⁵  Hande Sultan Yalinkilinc⁵  Dilek Aksit³ 

[1] Department of Pharmacology, Faculty of Medicine, Balikesir University, Balikesir, Turkey;Department of Parasitology, Faculty of Veterinary Medicine, University of Uludag, Bursa, Turkey;Department of Pharmacology and Toxicology, Faculty of Veterinary Medicine, Balikesir University, Balikesir, Turkey;Department of Parasitology, Faculty of Medicine, Abant Izzet Baysal University, Bolu, Turkey;Department of Pharmacology and Toxicology, Faculty of Veterinary Medicine, University of Adnan Menderes, Aydin, Turkey

关键词: Goat;    Sheep;    Enantiomers;    Pharmacokinetics;    Albendazole Sulfoxide;    Albendazole;    Benzimidazoles;   

Others  :  1206100
DOI  :  10.1186/s12917-015-0442-5

 received in 2015-02-12, accepted in 2015-05-18,  发布年份 2015

【 摘 要 】

Background

The aims of this study were to compare the pharmacokinetics of albendazole sulfoxide (ABZ-SO, ricobendazole) in goats and sheep at a dose of 5 mg/kg bodyweight (BW), after intravenous (IV) and subcutaneous (SC) administrations, and to investigate the effects of increased doses (10 and 15 mg/kg BW) on the plasma disposition of ABZ-SO in goats following SC administration. A total of 16 goats (Capra aegagrus hircus, eight males and eight females) and 8 sheep (Ovis aries, four males and four females) 12–16 months old and weighing 20–32 kg, were used. The study was designed according to two-phase crossover study protocol. In Phase-1, eight sheep were assigned as Group I and 16 goats were allocated into two groups (Group II and Group III). ABZ-SO was applied to Group I (sheep) and Group II (goats) animals subcutaneously, and to Group III (goats) animals intravenously, all at a dose rate of 5 mg/kg BW. In Phase-2, the sheep in the Group I received ABZ-SO intravenously in a dose of 5 mg/kg BW; the goats in Group II and Group III received ABZ-SO subcutaneously at a dose of 10 mg/kg and 15 mg/kg BW, respectively. Blood samples were collected from the jugular vein at different times between 1 and 120 h after drug administrations. The plasma concentrations of ABZ-SO and its metabolites were analysed by high performance liquid chromatography.

Results

In goats, the area under the curve, terminal half-life and plasma persistence of ABZ-SO were significantly smaller and shorter, respectively, compared with those observed in sheep following both IV and SC administrations at a dose of 5 mg/kg BW. On the other side, dose-dependent plasma dispositions of ABZ-SO were observed following SC administration at increased doses (10 and 15 mg/kg) in goats.

Conclusions

Consequently, ABZ-SO might be used at higher doses to provide higher plasma concentration and thus to achieve greater efficacy against the target parasites.

【 授权许可】

   
2015 Aksit et al.; licensee BioMed Central.

【 图 表 】

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