Limits...
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.


Mean (±SD) plasma concentrations of enantiomers [(+)ABZ-SO and (−)ABZ-SO)] vs. time curves of ABZ-SO in 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
getmorefigures.php?uid=PMC4443604&req=5

Fig3: Mean (±SD) plasma concentrations of enantiomers [(+)ABZ-SO and (−)ABZ-SO)] vs. time curves of ABZ-SO in sheep following intravenous administrations at a dose of 5 mg/kg (n = 8)

Mentions: The plasma concentrations of (+) ABZ-SO and (−) ABZ-SO) vs. time curves of ABZ-SO in goats and sheep following IV administrations at a dose rate of 5 mg/kg BW are shown in Fig. 2 and 3, respectively. In addition, the comparative ratio of the percentage of enantiomers in goats and sheep following IV administrations is shown in Fig. 4 and kinetic parameters of each enantiomer are summarised in Table 3. Stereospecific disposition of enantiomers displayed similar disposition in sheep and goats. (+) ABZ-SO were predominant and displayed significantly higher plasma concentrations compared with (−) enantiomer. The AUC of (+) enantiomer was almost two times larger than that of (−) enantiomer in both species after IV administration of rac-ABZ-SO.Fig. 2


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)

Mean (±SD) plasma concentrations of enantiomers [(+)ABZ-SO and (−)ABZ-SO)] vs. time curves of ABZ-SO in 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

Fig3: Mean (±SD) plasma concentrations of enantiomers [(+)ABZ-SO and (−)ABZ-SO)] vs. time curves of ABZ-SO in sheep following intravenous administrations at a dose of 5 mg/kg (n = 8)
Mentions: The plasma concentrations of (+) ABZ-SO and (−) ABZ-SO) vs. time curves of ABZ-SO in goats and sheep following IV administrations at a dose rate of 5 mg/kg BW are shown in Fig. 2 and 3, respectively. In addition, the comparative ratio of the percentage of enantiomers in goats and sheep following IV administrations is shown in Fig. 4 and kinetic parameters of each enantiomer are summarised in Table 3. Stereospecific disposition of enantiomers displayed similar disposition in sheep and goats. (+) ABZ-SO were predominant and displayed significantly higher plasma concentrations compared with (−) enantiomer. The AUC of (+) enantiomer was almost two times larger than that of (−) enantiomer in both species after IV administration of rac-ABZ-SO.Fig. 2

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.