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

Aksit D, Yalinkilinc HS, Sekkin S, Boyacioğlu M, Cirak VY, Ayaz E, Gokbulut C - BMC Vet. Res. (2015)

Bottom Line: The study was designed according to two-phase crossover study protocol.The plasma concentrations of ABZ-SO and its metabolites were analysed by high performance liquid chromatography.Consequently, ABZ-SO might be used at higher doses to provide higher plasma concentration and thus to achieve greater efficacy against the target parasites.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmacology and Toxicology, Faculty of Veterinary Medicine, Balikesir University, Balikesir, Turkey. dilekaksit@balikesir.edu.tr.

ABSTRACT

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 g/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.

No MeSH data available.


Comparative mean (±SD) plasma concentration vs. time curves of ABZ-SO and ABZ-SO2 in goats and sheep following intravenous administrations at a dose of 5 mg/kg (n = 8)
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Fig1: Comparative mean (±SD) plasma concentration vs. time curves of ABZ-SO and ABZ-SO2 in goats and sheep following intravenous administrations at a dose of 5 mg/kg (n = 8)

Mentions: The analytical procedures for the determination of plasma concentrations of ABZ, albendazole-2-aminosulfone (ABZ-NH3), ABZ-SO and ABZ-SO2 were validated before analysing of the experimental samples and the validation parameters for all molecules are summarised in Table 1. ABZ and ABZ-NH3 were not detected in any plasma samples of sheep and goats following either IV or SC administrations. The plasma concentration vs. time curves of ABZ-SO and ABZ-SO2 are shown in Fig. 1 and the pharmacokinetic data are summarized in Table 2 following IV administration in goats and sheep. Although the absorption phase and peak plasma concentrations (Cmax) of ABZ-SO were similar in both species, the area under the curve (AUC), terminal half-life (T1/2) and plasma persistence (MRT) values were smaller and shorter, respectively, in goats compared with those observed in sheep after SC administration at a dose of 5 mg/kg BW.Table 1


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

Aksit D, Yalinkilinc HS, Sekkin S, Boyacioğlu M, Cirak VY, Ayaz E, Gokbulut C - BMC Vet. Res. (2015)

Comparative mean (±SD) plasma concentration vs. time curves of ABZ-SO and ABZ-SO2 in goats and sheep following intravenous administrations at a dose of 5 mg/kg (n = 8)
© Copyright Policy - open-access
Related In: Results  -  Collection

License 1 - License 2
Show All Figures
getmorefigures.php?uid=PMC4443604&req=5

Fig1: Comparative mean (±SD) plasma concentration vs. time curves of ABZ-SO and ABZ-SO2 in goats and sheep following intravenous administrations at a dose of 5 mg/kg (n = 8)
Mentions: The analytical procedures for the determination of plasma concentrations of ABZ, albendazole-2-aminosulfone (ABZ-NH3), ABZ-SO and ABZ-SO2 were validated before analysing of the experimental samples and the validation parameters for all molecules are summarised in Table 1. ABZ and ABZ-NH3 were not detected in any plasma samples of sheep and goats following either IV or SC administrations. The plasma concentration vs. time curves of ABZ-SO and ABZ-SO2 are shown in Fig. 1 and the pharmacokinetic data are summarized in Table 2 following IV administration in goats and sheep. Although the absorption phase and peak plasma concentrations (Cmax) of ABZ-SO were similar in both species, the area under the curve (AUC), terminal half-life (T1/2) and plasma persistence (MRT) values were smaller and shorter, respectively, in goats compared with those observed in sheep after SC administration at a dose of 5 mg/kg BW.Table 1

Bottom Line: The study was designed according to two-phase crossover study protocol.The plasma concentrations of ABZ-SO and its metabolites were analysed by high performance liquid chromatography.Consequently, ABZ-SO might be used at higher doses to provide higher plasma concentration and thus to achieve greater efficacy against the target parasites.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmacology and Toxicology, Faculty of Veterinary Medicine, Balikesir University, Balikesir, Turkey. dilekaksit@balikesir.edu.tr.

ABSTRACT

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 g/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.

No MeSH data available.