K. Abo El-Sooud

Pharmacokinetics and bioavailability of florfenicol following intravenous, intramuscular and oral administrations in rabbits.

This study examined the disposition kinetics and bioavailability of florfenicol after intravenous (i.v.), intramuscular (i.m.) and oral administration to rabbits at a dose of 30 mg/kg BW. Serial blood samples were collected through an indwelling catheter intermittently for 24 h for various routes. Plasma antibacterial concentrations were determined using a microbiological assay method withBacillus subtilis ATCC 6633 as a reference organism. Plasma concentration–time data generated in the present study were analysed by non-compartmental methods based on statistical moment theory. Following i.v. administration, the overall elimination half-life (t1/2β) was 1.54 h, mean residence time (MRT) was 1.69 h, mean volume of distribution at steady-state (Vdss) was 0.57 L/kg, and total body clearance (Cltot) was 0.34 L/kg/h. After i.m. and oral dosing, the terminal part of the curve should correspond to the absorption phase, instead of to the elimination phase, with terminal half-lives of 3.01 and 2.57 h, respectively. The mean absorption time (MAT) was 2.65 h for i.m. and 2.01 h for oral administration. Elimination rate constants differed with i.v., i.m. and oral administrations, suggesting a flip-flop situation. The observed mean peak plasma concentrations (Cmax obs) were 21.65 and 15.14 μg/ml achieved at a post-injection time (Tmax obs) of 0.5 h following i.m. and oral dosing, respectively. The absolute systemic availabilities were 88.25% and 50.79%, respectively, and the extent of plasma protein binding percent was 11.65%.

Comparative Pharmacokinetics and Bioavailability of Amoxycillin in Chickens after Intravenous, Intramuscular and Oral Administrations

The pharmacokinetics and systemic bioavailability of amoxycillin were investigated in clinically healthy, broiler chickens (n = 10 per group) after single intravenous (i.v.), intramuscular (i.m.), and oral administrations at a dose of 10 mg/kg body weight. The plasma concentrations of amoxycillin were determined using high-performance liquid chromatography (HPLC) and the data were subjected to compartmental and non-compartmental kinetic analyses. Following single i.v. injection, all plasma amoxycillin data were described by a two compartment-open model. The elimination half-lives of amoxycillin were 1.07 h, 1.09 h and 1.13 h after single i.v., i.m. and oral administration, respectively. The total body clearance (ClB) of amoxycillin was 0.80 (L/h)/kg and the volume of distribution calculated as Vd(area) was 1.12 L/kg, respectively after i.v. administration. Substantial differences in the resultant kinetic data were obtained by comparing the plasma concentration profiles after i.m. injection with that after oral administration. The systemic i.m. bioavailability of amoxycillin was higher (77.21%) than after oral (60.92%) dosing.In vitro, the mean plasma protein binding of amoxycillin amounted to 8.27%. Owing to high clearance of amoxycillin in birds in our study, a plasma level was maintained above 0.25 μg/ml for only 6 h after i.m. and oral routes of administration and consequently frequent dosing may be necessary daily.

Kinetic disposition, systemic bioavailability and tissue distribution of salinomycin in chickens

Salinomycin was administered to chickens orally and intravenously to determine blood concentration, kinetic behaviour, bioavailability and tissue residues. The drug was given by intracrop and intravenous routes in a single dose of 20 mg kg-1 body-weight. The highest serum concentrations of salinomycin were reached half an hour after oral dosage with an absorption half-life (t0.5(ab)) of 3.64 hours and elimination half-life (t0.5(beta)) of 1.96 hours. The systemic bioavailability percentage was 73.02 per cent after intracrop administration, indicating the high extent of salinomycin absorption from this route in chickens. Following intravenous injection the kinetics of salinomycin can be described by a two-compartment open model with a t1/2(alpha) of 0.48 hours, Vd ss (volume of distribution) of 3.28 litre kg-1 and Cl(beta) (total body clearance) of 27.39 ml kg-1 min-1. The serum protein-binding tendency of salinomycin as calculated in vitro was 19.78 per cent. Salinomycin concentrations in the serum and tissues of birds administered salinomycin premix (60 ppm) for two weeks were lower than those after administration of a single intracrop dose of pure salinomycin (20 mg kg-1 bodyweight). The highest concentration of salinomycin residues were present in the liver followed by the kidneys, muscles, fat, heart and skin. No salinomycin residues were detected in tissues after 48 hours except in the liver and these had disappeared completely by 72 hours.

Anticoccidial efficacy of toltrazuril and halofuginone against Eimeria tenella infection in broiler chickens in Egypt

The anticoccidial activities of toltrazuril and halofuginone against Eimeria tenella were tested in broiler chickens. Comparisons were made between ummedicated infected and uninfected control birds in addition to infected groups given either toltrazuril at 37.5, 75 and 150 ppm in the drinking water, or halofuginone at 1.5, 3 and 6 ppm in the feed. Both drugs were highly efficacious against E tenella. Treatment improved the bodyweight gain and survival percentage in comparison with the unmedicated, infected group. Intestinal lesions, faecal and oocyst scores and oocyst shedding in dropping were significantly reduced by both drugs. Toltrazuril gave better protection than halofuginone; 75 and 150 ppm toltrazuril in drinking water gave good protection when administered four and five days after inoculation.

Characterization of the pharmacokinetic disposition of levofloxacin in stallions after intravenous and intramuscular administration

The target of the present study was to investigate the plasma disposition kinetics of levofloxacin in stallions (n = 6) following a single intravenous (i.v.) bolus or intramuscular (i.m.) injection at a dose rate of 4 mg/kg bwt, using a two-phase crossover design with 15 days as an interval period. Plasma samples were collected at appropriate times during a 48-h administration interval, and were analyzed using a microbiological assay method. The plasma levofloxacin disposition was best fitted to a two-compartment open model after i.v. dosing. The half-lives of distribution and elimination were 0.21 +/- 0.13 and 2.58 +/- 0.51 h, respectively. The volume of distribution at steady-state was 0.81 +/- 0.26 L/kg, the total body clearance (Cl(tot)) was 0.21 +/- 0.18 L/h/kg, and the areas under the concentration-time curves (AUCs) were 18.79 +/- 4.57 microg.h/mL. Following i.m. administration, the mean t(1/2el) and AUC values were 2.94 +/- 0.78 h and 17.21 +/- 4.36 microg.h/mL. The bioavailability was high (91.76% +/- 12.68%), with a peak plasma mean concentration (C(max)) of 2.85 +/- 0.89 microg/mL attained at 1.56 +/- 0.71 h (T(max)). The in vitro protein binding percentage was 27.84%. Calculation of efficacy predictors showed that levofloxacin might have a good therapeutic profile against Gram-negative and Gram-positive bacteria, with an MIC <or= 0.1 microg/mL.