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1.
J Vet Pharmacol Ther ; 33(1): 63-8, 2010 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-20444027

RESUMO

The pharmacokinetic behavior of marbofloxacin was studied in healthy (n = 12) and Pasteurella multocida infected rabbits (n = 12) after single intravenous (i.v.) and intramuscular (i.m.) administrations. Six rabbits in each group (control and diseased) were given a single dose of 2 mg/kg body weight (bw) of marbofloxacin intravenously. The other six rabbits in each group were given the same dose of the drug intramuscularly. The concentration of marbofloxacin in plasma was determined using high-performance liquid chromatography. The plasma concentrations were higher in diseased rabbits than in healthy rabbits following both routes of injections. Following i.v. administration, the values of the elimination half-life (t(1/2beta)), and area under the curve were significantly higher, whereas total body clearance was significantly lower in diseased rabbits. After i.m. administration, the elimination half-life (t(1/2el)), mean residence time, and maximum plasma concentration (C(max)) were higher in diseased rabbits (5.33 h, 7.35 h and 2.24 microg/mL) than in healthy rabbits (4.33 h, 6.81 h and 1.81 microg/mL, respectively). Marbofloxacin was bound to the extent of 26 +/- 1.3% and 23 +/- 1.6% to plasma protein of healthy and diseased rabbits, respectively. The C(max)/MIC (minimum inhibitory concentration) and AUC/MIC ratios were significantly higher in diseased rabbits (28 and 189 h) than in healthy rabbits (23 and 157 h), indicating the favorable pharmacodynamic characteristics of the drug in diseased rabbits.


Assuntos
Fluoroquinolonas/farmacocinética , Fluoroquinolonas/uso terapêutico , Infecções por Pasteurella/veterinária , Pasteurella multocida , Coelhos , Animais , Área Sob a Curva , Feminino , Fluoroquinolonas/administração & dosagem , Meia-Vida , Injeções Intramusculares , Injeções Intravenosas , Masculino , Infecções por Pasteurella/tratamento farmacológico , Infecções por Pasteurella/metabolismo
3.
Vet J ; 179(2): 282-6, 2009 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-18603456

RESUMO

Single-dose disposition kinetics of difloxacin (5mg/kg bodyweight) were determined in clinically normal male dromedary camels (n=6) following intravenous (IV) and intramuscular (IM) administration. Difloxacin concentrations were determined by high performance liquid chromatography with fluorescence detection. The concentration-time data were analysed by compartmental and non-compartmental kinetic methods. Following a single IV injection, the plasma difloxacin concentration-time curve was best described by a two-compartment open model, with a distribution half-life (t(1/2alpha)) of 0.22+/-0.02h and an elimination half-life (t(1/2beta)) of 2.97+/-0.31h. Steady-state volume of distribution (V(dss)) and total body clearance (Cl(tot)) were 1.02+/-0.21L/kg and 0.24+/-0.07L/kg/h, respectively. Following IM administration, the absorption half-life (t(1)(/)(2ab)) and the mean absorption time (MAT) were 0.44+/-0.03h and 1.53+/-0.22h, respectively. The peak plasma concentration (C(max)) of 2.84+/-0.34microg/mL was achieved at 1.42+/-0.21h. The elimination half-life (t(1/2el)) and the mean residence time (MRT) was 3.46+/-0.42h and 5.61+/-0.23h, respectively. The in vitro plasma protein binding of difloxacin ranged from 28-43% and the absolute bioavailability following IM administration was 93.51+/-11.63%. Difloxacin could be useful for the treatment of bacterial infections in camels that are sensitive to this drug.


Assuntos
Antibacterianos/farmacocinética , Camelus/sangue , Ciprofloxacina/análogos & derivados , Animais , Antibacterianos/efeitos adversos , Área Sob a Curva , Disponibilidade Biológica , Camelus/metabolismo , Ciprofloxacina/efeitos adversos , Ciprofloxacina/farmacocinética , Injeções Intramusculares/veterinária , Absorção Intestinal , Masculino
4.
J Vet Pharmacol Ther ; 31(5): 399-405, 2008 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-19000258

RESUMO

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

Assuntos
Antibacterianos/farmacocinética , Levofloxacino , Ofloxacino/farmacocinética , Animais , Antibacterianos/sangue , Antibacterianos/metabolismo , Área Sob a Curva , Disponibilidade Biológica , Meia-Vida , Cavalos , Injeções Intramusculares , Injeções Intravenosas , Masculino , Taxa de Depuração Metabólica , Ofloxacino/sangue , Ofloxacino/metabolismo , Ligação Proteica
6.
Chemotherapy ; 53(3): 169-72, 2007.
Artigo em Inglês | MEDLINE | ID: mdl-17361077

RESUMO

BACKGROUND: Imipenem is a carbapenem antibiotic with a broad spectrum of activity. The aim of this study was to determine the pharmacokinetics of imipenem after single intravenous and intramuscular injections and the effect of repeated intramuscular injections on hepato-renal functions in sheep. METHODS: Imipenem concentrations in plasma and urine were determined by a microbiological agar plate assay. RESULTS: Following intramuscular injection, imipenem was rapidly absorbed and the peak plasma concentration was 9.99 microg ml(-1) and the systemic bioavailability was 65.97%. Urine concentrations of imipenem were much higher than in plasma. Light and electron microscopy evidenced little changes in the kidney and liver. CONCLUSION: Imipenem is likely to be efficacious in most urinary tract infections and has no adverse effects on hepato-renal structures and functions.


Assuntos
Antibacterianos/farmacocinética , Imipenem/farmacocinética , Alanina Transaminase/sangue , Animais , Antibacterianos/sangue , Antibacterianos/farmacologia , Antibacterianos/urina , Aspartato Aminotransferases/sangue , Feminino , Imipenem/sangue , Imipenem/farmacologia , Imipenem/urina , Injeções Intramusculares , Injeções Intravenosas , Rim/efeitos dos fármacos , Rim/ultraestrutura , Fígado/efeitos dos fármacos , Fígado/ultraestrutura , Ovinos
7.
Vet Res Commun ; 28(7): 599-607, 2004 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-15563107

RESUMO

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 (Cl(B)) of amoxycillin was 0.80 (L/h)/kg and the volume of distribution calculated as V(d(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 microg/ml for only 6 h after i.m. and oral routes of administration and consequently frequent dosing may be necessary daily.


Assuntos
Amoxicilina/farmacocinética , Antibacterianos/farmacocinética , Galinhas/metabolismo , Administração Oral , Amoxicilina/administração & dosagem , Amoxicilina/sangue , Animais , Antibacterianos/administração & dosagem , Antibacterianos/sangue , Área Sob a Curva , Disponibilidade Biológica , Galinhas/sangue , Cromatografia Líquida de Alta Pressão/veterinária , Meia-Vida , Injeções Intramusculares/veterinária , Injeções Intravenosas/veterinária , Masculino
8.
J Ethnopharmacol ; 95(2-3): 235-8, 2004 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-15507342

RESUMO

The antinociceptive effect of methanolic extracts (200 and 400 mg kg(-1)) of eight Egyptian medicinal plants was studied using acetic acid-induced writhing and tail-flick test in mice. Oral administration of 400 mg kg(-1) methanolic extracts of Convolvulus fatmensis, Alhagi maurorum, Plantago major seeds, Conyza dioscaridis significantly (P < 0.05) inhibited the nociception to acetic acid-induced writhes with a protection of 85.5-61.3%. Schouwia thebaica, Diplotaxis acris, Plantago major leaves and Mentha microphylla, in the large dose, showed a protection of 50.8-45.8%, which were significantly different as compared to control. The smaller dose of the tested plant extracts did not protect animals from painful acetic acid stimulation with the exception of Alhagi maurorum. In the tail-flick test, methanolic extracts of Mentha microphylla, Conyza dioscaridis, Alhagi maurorum, Plantago major leaves, Diplotaxis acris and Convolvulus fatmensis in a dose of 400 mg kg(-1) produced significant increase in the latency to response of tail to thermal stimulation. Mild or no effect was observed by the small dose with the exception of Diplotaxis acris that had significant antinociceptive effect at the dose of 200 mg kg(-1). The extracts of all tested plants in doses up to 2 g kg(-1) b.wt. did not cause any deaths or major signs of acute toxicity. Phytochemical screening indicated the presence of unsaturated sterols, triterpenes, tannins, flavonoids and carbohydrates and/or glycosides as major constituents.


Assuntos
Analgésicos/farmacologia , Medicina Tradicional , Medição da Dor/efeitos dos fármacos , Plantas Medicinais , Analgésicos/isolamento & purificação , Animais , Egito , Masculino , Camundongos , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Estruturas Vegetais
9.
Vet Res Commun ; 28(6): 515-24, 2004 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-15509025

RESUMO

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 with Bacillus 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 (t1/2beta) 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 microg/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%.


Assuntos
Antibacterianos/administração & dosagem , Antibacterianos/farmacocinética , Coelhos/metabolismo , Tianfenicol/análogos & derivados , Tianfenicol/administração & dosagem , Tianfenicol/farmacocinética , Administração Oral , Animais , Antibacterianos/sangue , Área Sob a Curva , Disponibilidade Biológica , Meia-Vida , Injeções Intramusculares/veterinária , Injeções Intravenosas/veterinária , Ligação Proteica , Tianfenicol/sangue
11.
Dtsch Tierarztl Wochenschr ; 111(4): 162-5, 2004 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-15171602

RESUMO

This study investigated the disposition kinetics and plasma availability of erythromycin in broiler chickens after single intravenous (i.v.), intramuscular (i.m.), subcutaneous (s.c.) and oral administrations (p.o.) of 30 mg kg(-1) b. wt. Tissue residue profiles were also studied after multiple intramuscular, subcutaneous, and oral administration of 30 mg kg(-1) b. wt., twice daily for three consecutive days. Plasma and tissue concentrations of erythromycin were determined using microbiological assay methods with Micrococcus luteus as the test organism. Following intravenous injection, plasma concentration-vs-time curves were best described by a two compartment open model. The decline in plasma drug concentration was bi-exponential with half-lives of (t(1/2alpha)) 0.19 h and (t(1/2beta)) 5.3 h for distribution and elimination phases, respectively. After intramuscular, subcutaneous and oral administration erythromycin at the same dose was detected in plasma at 10 min and reached its minimum level 8 h post-administration. The peak plasma concentration (Cmax) were 5.0, 5.3, and 6.9 microg x ml(-1) and were attained at 1.7, 1.4, and 1.3 h (Tmax), respectively. The elimination half-lives (T(1/2el)) were 3.9, 2.6, and 4.1 h and the mean residence times (MRT) were 3.5, 3.2, and 3.6 h, respectively. The systemic bioavailabilities were 92.5, 68.8, and 109.3%, respectively. In vitro protein binding percent of erythromycin in broiler plasma was ranged from 21 to 31%. The limit of quantification (LOQ) for the assay was 0.03 microg x ml(-1) in plasma and tissues. The tissue level concentrations were highest in the liver, and decreased in the following order: plasma > kidney > lung > muscle and heart. No erythromycin residues were detected in tissues and plasma after 24 h except in liver and kidney where it persisted during 48 h following intramuscular and oral administrations.


Assuntos
Antibacterianos/farmacocinética , Galinhas/metabolismo , Resíduos de Drogas/análise , Eritromicina/farmacocinética , Administração Oral , Animais , Antibacterianos/administração & dosagem , Eritromicina/administração & dosagem , Injeções Intramusculares/veterinária , Injeções Intravenosas/veterinária , Injeções Subcutâneas/veterinária , Distribuição Aleatória
12.
J Vet Pharmacol Ther ; 27(1): 27-30, 2004 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-14995963

RESUMO

The pharmacokinetics of meropenem was studied in five ewes after single i.v. and i.m. dose of 20 mg/kg bw. Meropenem concentrations in plasma and urine were determined using microbiological assay method. A two-compartment open model was best described the decrease of meropenem concentration in plasma after an i.v. injection. The drug was rapidly eliminated with a half-life of elimination (t1/2beta) of 0.39 +/- 0.30 h. Meropenem showed a small steady-state volume of distribution [Vd(ss)] 0.055 +/- 0.09 L/kg. Following i.m. injection, meropenem was rapidly absorbed with a t1/2ab of 0.25 +/- 0.04 h. The peak plasma concentration (Cmax) was 48.79 +/- 8.83 microg/mL was attained after 0.57 +/- 0.13 h (tmax). The elimination half-life (t1/2el) of meropenem was 0.71 +/- 0.12 h and the mean residence time (MRT) was 1.38 +/- 0.26 h. The systemic bioavailability (F) after i.m. injection was 112.67 +/- 10.13%. In vitro protein-binding percentage of meropenem in ewe's plasma was 42.80%. The mean urinary recoveries of meropenem over 24 h were 83% and 91% of the administered dose after i.v. and i.m. injections respectively. Thus, meropenem is likely to be efficacious in the eradication of many urinary tract pathogens in sheep.


Assuntos
Ovinos/metabolismo , Tienamicinas/farmacocinética , Animais , Feminino , Injeções Intramusculares/veterinária , Injeções Intravenosas/veterinária , Meropeném , Tienamicinas/administração & dosagem , Tienamicinas/sangue , Tienamicinas/urina
13.
J Vet Med A Physiol Pathol Clin Med ; 50(4): 196-200, 2003 May.
Artigo em Inglês | MEDLINE | ID: mdl-12948156

RESUMO

The pharmacokinetics of gentamicin was studied in lambs, calves and foals, respectively after single intravenous (i.v.) injections of 5 mg kg(-1) body weight. The plasma concentration-time curves of gentamicin sulphate were best fitted to follow a two-compartment open model in calves and foals and a three-compartment open model in lambs. Gentamicin showed high plasma level at 5 min post-injection. Then its concentration decreased gradually until its minimum detectable level at 10 and 12 h post-injection in foals and calves, respectively, was reached. In contrast, the plasma concentrations were much higher in lambs and persisted up to 48 h from the onset of injection. Values of pharmacokinetic parameters for gentamicin sulphate in different animals after i.v. injections were calculated. Pharmacokinetic data in lambs demonstrated a triphasic decline in plasma gentamicin concentration with slow terminal elimination phase (washout phase) with (t(1/2y)) of 7.7 h. Gentamicin showed a small volume of distribution Vd(ss) (80.3 ml kg(-1)) in lambs indicating that the drug is slightly distributed in extra-vascular tissues. The overall rate of total body clearance ClB in lambs was (0.46 ml kg(-1)) slower than in calves (1.5 ml kg(-1)) and foals (2.7 ml kg(-1)). In vitro protein binding per cent of gentamicin sulphate in plasma were 16.80, 11.03 and 7.98% in lambs, calves and foals. The results of this study emphasize the importance of determining the pharmacokinetics of gentamicin in each species of young animals separately.


Assuntos
Animais Domésticos/fisiologia , Antibacterianos/farmacocinética , Gentamicinas/farmacocinética , Animais , Antibacterianos/administração & dosagem , Área Sob a Curva , Sítios de Ligação , Bovinos , Gentamicinas/administração & dosagem , Cavalos , Injeções Intravenosas , Ligação Proteica , Ovinos , Especificidade da Espécie
14.
Pharmacol Res ; 48(4): 389-95, 2003 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-12902210

RESUMO

The pharmacokinetics of single intravenous and intramuscular administrations and milk antimicrobial equivalent activity of enrofloxacin at a dose of 5 mg per kilogram body weight were studied in clinically healthy lactating goats which were either not treated or had received 7.5 mg per kilogram body weight of albendazole orally. The concentrations of enrofloxacin in serum and milk were determined using microbiological assay. Following intravenous injection, enrofloxacin antimicrobial equivalent activity versus time data in serum was described by a two-compartmental open model. Albendazole treatment significantly decreased the elimination half-life (t(1/2beta)) (P>or=0.05) and the mean residence time (MRT) (P>or=0.05), whereas, the rate of enrofloxacin return to central compartment from peripheral tissue (K(21)) was significantly increased (P>or=0.01). In contrast, the volumes of distribution V(d(area)) and V(d(SS)) were significantly decreased (P>or=0.01 and P>or=0.05, respectively) in albendazole-treated goats. After intramuscular injection, enrofloxacin was rapidly absorbed in control and albendazole-treated lactating goats with absorption half-lives (t(1/2ab)) 0.43 and 0.39 h, respectively. The mean peaks of serum concentration (C(max)) were 0.68 and 0.65 mcg ml(-1) attained at (t(max)) 1.08 and 1.12 h, before and after albendazole dosing, respectively. The elimination half-life (t(1/2el)) and (MRT) following intramuscular injections were also shorter in the albendazole-treated lactating goats. The systemic bioavailability of enrofloxacin was significantly decreased from 110.16 to 84.38% in albendazole-treated lactating goats. Concomitant administration of albendazole with enrofloxacin resulted in significant alterations in the disposition kinetic of enrofloxacin and significant decrease in enrofloxacin concentrations in milk. Consequently, the interaction between albendazole and enrofloxacin could be of clinical significance and may require monitoring and adjustment of enrofloxacin dosage.


Assuntos
Albendazol/farmacocinética , Fluoroquinolonas/farmacologia , Leite/química , Leite/metabolismo , Quinolonas/farmacologia , Administração Oral , Albendazol/administração & dosagem , Albendazol/sangue , Animais , Disponibilidade Biológica , Resíduos de Drogas/química , Resíduos de Drogas/metabolismo , Resíduos de Drogas/farmacocinética , Quimioterapia Combinada , Enrofloxacina , Feminino , Fluoroquinolonas/antagonistas & inibidores , Fluoroquinolonas/sangue , Cabras , Meia-Vida , Injeções Intramusculares , Injeções Intravenosas , Lactação/fisiologia , Leite/efeitos dos fármacos , Quinolonas/antagonistas & inibidores , Quinolonas/sangue , Fatores de Tempo
15.
Dtsch Tierarztl Wochenschr ; 108(9): 393-6, 2001 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-11599443

RESUMO

The pharmacokinetic parameters of thiamphenicol (TAP) were studied in New Zealand white rabbits. Five rabbits were each given thiamphenicol as a single 30 mg/kg of body weight dosage by intravenous (i.v.), intramuscular (i.m.) and oral routes. Serum antibacterial concentrations were determined for 72 h after dosing. Compartmental modeling of the i.v. administration indicated that a 2-compartment open model best described the disposition of thiamphenicol in rabbits. Serum thiamphenicol concentrations after i.m. and oral dosing were best described by a 1- and 2-compartment model, respectively. Overall elimination half-lives for i.v., i.m. and oral routes of administration were 1.39, 2.45, and 1.44 h, respectively. The half-life of absorption for oral dosing was 1.2 times the half-life of absorption after i.m. dosing (0.49 h vs 0.40 h). The calculated time to maximal serum concentration was 1.25 h after i.m. dosing and 1.17 h after oral administration. The calculated serum concentrations at these times were 80.4 and 69.8 micrograms/ml, respectively. Mean residence time's were 1.89 h for i.v. injection, 2.78 h for i.m. dosing and 4.11 h for oral administration. Thiamphenicol was widely distributed in the rabbit as suggested by the volume of distribution value at steady state of 1.47 l/kg calculated from the i.v. study. Bioavailability was 101.4% after i.m. dosing and 64.2% for oral absorption.


Assuntos
Antibacterianos/farmacocinética , Coelhos/metabolismo , Tianfenicol/farmacocinética , Administração Oral , Animais , Antibacterianos/administração & dosagem , Disponibilidade Biológica , Meia-Vida , Injeções Intramusculares/veterinária , Injeções Intravenosas/veterinária , Modelos Biológicos , Coelhos/sangue , Tianfenicol/administração & dosagem
16.
Dtsch Tierarztl Wochenschr ; 108(4): 168-71, 2001 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-11370478

RESUMO

This study investigated the disposition kinetics and plasma availability of ceftazidime in rabbits after single intravenous (i.v.) and intramuscular (i.m.) injections of 50 mg kg-1 b.wt. Tissue residue profiles were studied after repeated intramuscular injections of 50 mg kg-1 b. wt, twice daily for five consecutive days. A microbiological assay with Bacillus subtilis as the test organism was used to measure its concentrations in plasma and tissues. The plasma concentration-vs-time curves were best described by a two compartment open model. The decline in plasma drug concentration was biexponential with half-lives of 0.258 h for t1/2 alpha, 2.22 h for t1/2 beta, for distribution and elimination phases, respectively, following i.v. injection. After intramuscular injection of ceftazidime at the same dose, it was detected in plasma at 5 min and reached its minimum level 12 h post-injection. The peak plasma concentration (Cmax) 66.3 micrograms.ml-1 was attained at 0.779 h (Tmax). The elimination half-life (T1/2el,) was 2.12 h, the mean residence time (MRT) was 3.06 h and the systemic bioavailability was 96.6%. In vitro protein binding percent of ceftazidime in rabbit's plasma was ranged from 13.3 to 21.6%. The limit of quantification (LOQ) for the assay was 0.01 microgram.ml-1 in plasma and tissues. The tissue level concentrations were highest in the kidneys, and decreased in the following order: liver > heart > muscles and plasma. No ceftazidime residues were detected in tissues and plasma after 72 h. It is concluded that tissue kinetics is an important tool in predicting and controlling drug residues in edible tissues of food producing animal.


Assuntos
Ceftazidima/farmacocinética , Cefalosporinas/farmacocinética , Resíduos de Drogas/farmacocinética , Coelhos/metabolismo , Absorção , Animais , Disponibilidade Biológica , Ceftazidima/administração & dosagem , Cefalosporinas/administração & dosagem , Resíduos de Drogas/análise , Injeções Intramusculares/veterinária , Injeções Intravenosas/veterinária , Masculino , Distribuição Tecidual
17.
Res Vet Sci ; 69(3): 219-24, 2000 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-11124092

RESUMO

The pharmacokinetics of cefuroxime sodium, 20 and 40 mg kg(-1), were studied after i.v. and intramuscular injections in goats. Following single i.v. injections the serum concentration time curves of cefuroxime sodium were best fitted to a two-compartment open model. The drug was rapidly distributed with half-lives of distribution (t(1/2 alpha)) of 0.250 hours and 0.266 hours, and rapidly eliminated with half-lives of elimination (t(1/2 beta)) of 1.482 hours and 1.416 hours, respectively, following single i.v. injections of 20 and 40 mg kg(-1)body weight. After single intramuscular injections of cefuroxime sodium at the same doses, the mean absorption time (MAT) values were 1.379 and 1.716 hours and the peak serum concentration, C(max), was 12.965 and 38.50 microg ml(-1), attained after 0.515 and 0.608 hours (t(max)), respectively. The elimination half-lives (t(1/2el)) were 2.088 and 2.114 hours and the mean residence times (MRT) were 3.198 and 3.237 hours for 20 and 40 mg kg(-1)body weight, respectively. After both i.v. and intramuscular injections of cefuroxime sodium, the concentrations of cefuroxime in urine were much higher than that in serum. Urinary drug concentrations decreased gradually to reach their lowest levels at 24 and 48 hours post-injection, respectively. The systemic bioavailability of cefuroxime sodium in goats after intramuscular injections of 20 and 40 mg kg(-1)body weight was 88.4 per cent and 103.5 per cent, respectively. In vitro protein binding of cefuroxime sodium in goat's serum was low, ranging from 13.3 per cent to 21.6 per cent with an average of 17.0 per cent.


Assuntos
Cefuroxima/farmacocinética , Cefalosporinas/farmacocinética , Cabras/metabolismo , Animais , Disponibilidade Biológica , Cefuroxima/administração & dosagem , Cefalosporinas/administração & dosagem , Creatinina/sangue , Creatinina/urina , Injeções Intramusculares/veterinária , Injeções Intravenosas/veterinária , Taxa de Depuração Metabólica , Ligação Proteica
18.
Dtsch Tierarztl Wochenschr ; 106(7): 291-4, 1999 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-10481373

RESUMO

Tilmicosin was injected subcutaneously to lactating ewes once at a dose of 10 mg kg-1 b.wt. to determine its plasma, milk, urine and ruminal juice concentrations. Tilmicosin could be detected in all those fluids 30 minutes after injection. Milk and urine concentrations were higher than those of plasma and ruminal juice. The drug was detectable in milk, urine and plasma for 9, 4 and 3 days after injection, respectively. No amount of tilmicosin could be detected in ruminal juice 12 hours following administration. The mean peak concentration of tilmicosin in plasma and milk (Cmax) were 1.29 and 9.5 micrograms ml-1 and were obtained at (Tmax) 5.235 and 15.093 hours, respectively. The drug was slowly eliminated from plasma and milk as indicated by its long half-life (t1/2el) of 15.4 and 26.2 hours, respectively. The mean binding of tilmicosin to plasma and milk proteins in vitro was 16.8% and 26.8%, respectively. The drug was not bound to ruminal juice at any extent. The rate of tilmicosin renal clearance revealed that it was correspondingly increased with higher blood concentrations. While creatinine clearance showed no significant change after tilmicosin administration. The ratio (fractional clearance) between tilmicosin renal clearance to creatinine clearance was less than one indicating that the glomerular filtration is the main pathway of elimination through kidneys. The rate of ruminal gas fermentation in ewes was inhibited after subcutaneous injection of tilmicosin at a dose of 10 mg kg-1 b.wt. The tested samples taken at different time intervals from the rumen of ewes showed a subsequent reduction in the rate of fermentation as compared to control samples. The reduction was correspondingly increased with the increase of tilmicosin concentration in ruminal juice and returned to normal thereafter.


Assuntos
Antibacterianos/farmacocinética , Lactação , Macrolídeos , Tilosina/análogos & derivados , Animais , Antibacterianos/administração & dosagem , Antibacterianos/sangue , Proteínas Sanguíneas/metabolismo , Feminino , Suco Gástrico/química , Injeções Subcutâneas , Leite/química , Proteínas do Leite/metabolismo , Rúmen , Ovinos , Tilosina/administração & dosagem , Tilosina/sangue , Tilosina/farmacocinética
19.
Zentralbl Veterinarmed A ; 46(4): 239-46, 1999 May.
Artigo em Inglês | MEDLINE | ID: mdl-10399483

RESUMO

The pharmacokinetics of amikacin was studied in five lactating goats after single intravenous and intramuscular administrations of 7.5 mg kg-1 body weight. After intravenous injection, the plasma concentration-time curve of amikacin was characteristic of a two-compartment open model with a distribution half-life of 11.03 min and an elimination half-life of 114.81 min. The mean residence time was 142.96 min and the volume of the central compartment was 0.061 kg-1. Following intramuscular injection, amikacin was rapidly absorbed with an absorption half-life of 20.39 min. The peak plasma concentration was 34.48 micrograms ml-1 and was attained at 62.15 min. The elimination half-life of amikacin after intramuscular administration was 122.86 min and the corresponding mean residence time was 205.51 min. The systemic bioavailability of amikacin after intramuscular administration was 98.27%. Amikacin was not bound to plasma and milk proteins in vitro. Amikacin was detected only at low concentrations in the goat's milk 2-6 h after intravenous and intramuscular injections. Amikacin urine concentrations were much higher than those of plasma. Thus, amikacin is likely to be efficacious in the eradication of many Gram-negative urinary tract pathogens.


Assuntos
Amicacina/farmacocinética , Antibacterianos/farmacocinética , Cabras/metabolismo , Lactação/metabolismo , Amicacina/administração & dosagem , Amicacina/urina , Animais , Antibacterianos/administração & dosagem , Antibacterianos/urina , Área Sob a Curva , Feminino , Meia-Vida , Injeções Intramusculares/veterinária , Injeções Intravenosas/veterinária , Leite/metabolismo
20.
Zentralbl Veterinarmed A ; 46(1): 49-57, 1999 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-10085767

RESUMO

The pharmacokinetic aspects of diminazene aceturate were studied in lactating goats and sheep after single intravenous and intramuscular administrations of 3.5 mg/kg b.wt. Plasma and milk concentrations were determined by use of reversed phase high-performance liquid chromatography (HPLC) after ion-pair extraction. Following intravenous injection, the disposition of diminazene in goats and sheep conformed to a two-compartment model with rapid distribution and slower elimination phases. Values of (t1/2 beta) were obtained indicating a slower final disappearance of the drug from plasma of sheep (21.17 h) than in goats (16.39 h). Diminazene concentrations were maintained for more than 4 days in the plasma of goats and sheep. In both species of animals, diminazene was rapidly absorbed following intramuscular administration of 3.5 mg/kg b.wt. The peak plasma concentrations (Cmax) were 7.00 and 8.11 micrograms/ml and were attained at (Tmax) 0.92 and 1.12 hours in goats and sheep, respectively. The elimination half-life (t1/2el) of diminazene after intramuscular administration was shorter in goats (16.54 h) than in sheep (18.80 h). Systemic bioavailabilities (F%) of diminazene after intramuscular administration were 94.94% and 82.64% in goats and sheep, respectively. Diminazene could be detected in milk of goats and sheep within 10 min post-injection. Milk concentrations of the drug were lower in goats than in sheep and were detected for 5 and 6 days following both routes of administration, respectively.


Assuntos
Diminazena/farmacocinética , Lactação/metabolismo , Tripanossomicidas/farmacocinética , Animais , Diminazena/administração & dosagem , Feminino , Cabras , Injeções Intramusculares , Injeções Intravenosas , Taxa de Depuração Metabólica , Leite/metabolismo , Modelos Biológicos , Ovinos , Especificidade da Espécie , Tripanossomicidas/administração & dosagem
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