A bioavailability and pharmacokinetics study of powder and liquid tilmicosin formulations was carried out in 18 healthy chickens according to a single-dose, two-period, two-sequence, crossover randomized design. The two formulations were Provitil and Pulmotil AC. Both drugs were administered to each chicken after an overnight fast on two treatment days separated by a 2-week washout period. A modified rapid and sensitive HPLC method was used for determination of tilmicosin concentrations in chicken plasma. Various pharmacokinetic parameters including area under plasma concentration-time curve (AUC(0-72)), maximum plasma concentration (C(max)), time to peak concentration (t(max)), elimination half-life (t(1/2beta)), elimination rate (k(el)), clearance (Cl(B)), mean residence time (MRT) and volume of distribution (V(d,area)) were determined for both formulations. The average means of AUC(0-72) for Provitil and Pulmotil AC were very close (24.24 +/- 3.86, 21.82 +/- 3.14 (microg x h)/ml, respectively), with no significant differences based on ANOVA. The relative bioavailability of Provitil as compared to Pulmotil AC was 111%. In addition, there were no significant differences in the C(max) (2.09 +/- 0.37, 2.12 +/- 0.40 microg/ml), tmax (3.99 +/- 0.84, 5.82 +/- 1.04 h), t(1/2beta) (47.4 +/- 9.32, 45.0 +/- 5.73 h), k(el) (0.021 +/- 0.0037, 0.022 +/- 0.0038 h(-1)), Cl(B) (19.73 +/- 3.73, 21.37 +/- 4.54ml/(min/kg)), MRT (71.20 +/- 12.87, 67.15 +/- 9.01 h) and V(d,area) (1024.8 +/- 87.5, 1009.8 +/- 79.5 ml/kg) between Pulmotil AC and Provitil, respectively. In conclusion, tilmicosin was rapidly absorbed and slowly eliminated after oral administration of single dose of tilmicosin aqueous and powder formulations. Provitil and Pulmotil AC can be used as interchangeable therapeutic agents.
The pharmacokinetics and oral bioavailability of two tylosin formulations was carried out in broiler chickens according to a single dose, randomized, parallel design. The two formulations of tylosin (Tylosina® and Tylan®) were given orally at a dose level of 25 mg/kg b.w. after an overnight fasting (n=15 chicken/group). To calculate tylosin bioavailability, fifteen more chickens was assigned as group 3 and was given a single intravenous dose of tylosin (25 mg/kg b.w.). Serial blood samples were collected at different time points up to 24 hour post-drug administration. A high performance liquid chromatography (HPLC) method was used for the determination of tylosin concentrations in chicken plasma. The pharmacokinetics analysis of the data was performed using non-compartmental analysis based on statistical moment theory with the help of commercially available software (WinNonlin®, Pharsight Corporation, Cary, NC, USA). There were no significant differences in the Cmax (3.05±0.63, 2.63±0.74 μg/ml), tmax (2.36±0.42, 2.30±0.38 h), t1/2β (1.99±0.38, 2.67±0.60 h), AUC0-12h (6.11±0.97, 5.37±1.16 μg.h/ml), AUC0-∞ (6.38±0.94, 5.57±1.15 μg.h/ml), MRT (3.53±0.24, 3.67±0.32 h), ClB/F (90.59±13.81, 169.38±54.44 ml/min/kg) and Vdz/F (16.85±4.74, 43.96±18.24 l/kg) between Tylosina® and Tylan®, respectively. The calculated oral bioavailability (F) for Tylosina® and Tylan® were 40.56 and 35.41%, respectively. Moreover, the relative bioavailability of Tylosina® was 113.9% when compared to Tylan®. In conclusion, Tylosina® is comparable to Tylan® and both formulations can be used for treatment of susceptible microorganisms in veterinary medicine practice at a dose level of 25 mg/kg b.w.
A pharmacokinetic and bioavailability study of sulfadiazine combined with trimethoprim (sulfadiazine/trimethoprim) was carried out in fifteen healthy young ostriches after intravenous (i.v.), intramuscular (i.m.) and oral administration at a total dose of 30 mg/kg body weight (bw) (25 and 5 mg/kg bw of sulfadiazine and trimethoprim, respectively). The study followed a single dose, three periods, cross-over randomized design. The sulfadiazine/trimethoprim combination was administered to ostriches after an overnight fasting on three treatment days, each separated by a 2-week washout period. Blood samples were collected at 0 (pretreatment), 0.08, 0.25, 0.50, 1, 2, 4, 6, 8, 12, 24 and 48 h after drug administration. Following i.v. administration, the elimination half-life (t(1/2beta)), the mean residence time (MRT), volume of distribution at steady-state (V(d(ss))), volume of distribution based on terminal phase (V(d(z))), and the total body clearance (Cl(B)) were (13.23 +/- 2.24 and 1.95 +/- 0.19 h), (10.06 +/- 0.33 and 2.17 +/- 0.20 h), (0.60 +/- 0.08, and 2.35 +/- 0.14 L/kg), (0.79 +/- 0.12 and 2.49 +/- 0.14 L/kg) and (0.69 +/- 0.03 and 16.12 +/- 1.38 mL/min/kg), for sulfadiazine and trimethoprim, respectively. No significant difference in C(max) (35.47 +/- 2.52 and 37.50 +/- 3.39 microg/mL), t(max) (2.47 +/- 0.31 and 2.47 +/- 0.36 h), t((1/2)beta) (11.79 +/- 0.79 and 10.96 +/- 0.56 h), V(d(z))/F (0.77 +/- 0.06 and 0.89 +/- 0.07 L/kg), Cl(B)/F (0.76 +/- 0.04 and 0.89 +/- 0.07) and MRT (12.39 +/- 0.40 and 12.08 +/- 0.36 h) were found in sulfadiazine after i.m. and oral dosing, respectively. There were also no differences in C(max) (0.71 +/- 0.06 and 0.78 +/- 0.10 microg/mL), t(max) (2.07 +/- 0.28 and 3.27 +/- 0.28 h), t((1/2)beta) (3.30 +/- 0.25 and 3.83 +/- 0.33 h), V(d(z))/F (6.2 +/- 0.56 and 6.27 +/- 0.77 L/kg), Cl(B)/F (21.9 +/- 1.46 and 18.83 +/- 1.72) and MRT (3.68 +/- 0.19 and 4.34 +/- 0.14 h) for trimethoprim after i.m. and oral dosing, respectively. The absolute bioavailability (F) was 95.41% and 86.20% for sulfadiazine and 70.02% and 79.58% for trimethoprim after i.m. and oral administration, respectively.
The pharmacokinetics and bioavailability of gentamicin sulphate (5 mg/kg body weight) were studied in 50 female broiler chickens after single intravenous (i.v.), intramuscular (i.m.), subcutaneous (s.c.) and oral administration. Blood samples were collected at time 0 (pretreatment), and at 5, 15 and 30 min and 1, 2, 4, 6, 8, 12, 24 and 48 h after drug administration. Gentamicin concentrations were determined using a microbiological assay and Bacillus subtillis ATCC 6633 as a test organism. The limit of quantification was 0.2 microg/ml. The plasma concentration-time curves were analysed using non-compartmental methods based on statistical moment theory. Following i.v. administration, the elimination half-life (t (1/2beta)), the mean residence time (MRT), the volume of distribution at steady state (V (ss)), the volume of distribution (V (d,area)) and the total body clearance (Cl(B)) were 2.93 +/- 0.15 h, 2.08 +/- 0.12 h, 0.77 +/- 0.05 L/kg, 1.68 +/- 0.39 L/kg and 5.06 +/- 0.21 ml/min per kg, respectively. After i.m. and s.c. dosing, the mean peak plasma concentrations (C (max)) were 11.37 +/- 0.73 and 16.65 +/- 1.36 microg/ml, achieved at a post-injection times (t (max)) of 0.55 +/- 0.05 and 0.75 +/- 0.08 h, respectively. The t (1/2beta) was 2.87 +/- 0.44 and 3.48 +/- 0.37 h, respectively after i.m. and s.c. administration. The V (d,area) and Cl(B) were 1.49 +/- 0.21 L/kg and 6.18 +/- 0.31 ml/min per kg, respectively, after i.m. administration and were 1.43 +/- 0.19 L/kg and 4.7 +/- 0.33 ml/min per kg, respectively, after s.c. administration. The absolute bioavailability (F) of gentamicin after i.m. administration was lower (79%) than that after s.c. administration (100%). Substantial differences in the resultant kinetics data were obtained between i.m. and s.c. administration. The in vitro protein binding of gentamicin in chicken plasma was 6.46%.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.
hi@scite.ai
10624 S. Eastern Ave., Ste. A-614
Henderson, NV 89052, USA
Copyright © 2024 scite LLC. All rights reserved.
Made with 💙 for researchers
Part of the Research Solutions Family.