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1.
The disposition kinetics and dosage regimen of enrofloxacin were investigated in breeding buffalo bulls following a single intramuscular administration of 5 mg/kg. The absorption half-life, half-life of the terminal phase, apparent volume of distribution and total body clearance were 0.262±0.099 h, 1.97±0.23 h, 0.61±0.13 L/kg and 210.2±18.6 ml/(kg.h), respectively. Therapeutic plasma levels (1 g/ml) were maintained for up to 6 h. A satisfactory intramuscular dosage regimen for enrofloxacin in buffalo bulls would be 8.5 mg/kg followed by 8.0 mg/kg at 8 h intervals.  相似文献   

2.
A two-way crossover study was conducted in crossbred male calves (6–8 months old) to determine the bioavailability, pharmacokinetics and dosage regimens for a long-acting formulation of oxytetracycline (OTC-LA). The half-lives of oxytetracycline after intravenous and intramuscular administration were 7.8 h and 24 h, respectively. The volume of distribution and total body clearance values of the drug were 0.86±0.07 L and 76.1±3.3 (ml/h)/kg, respectively. The maximum concentration of the drug in the serum (4.7–7.4 g/ml) was achieved 8–10 h after intramuscular administration. The minimum therapeutic serum concentration of drug of 0.5 g/ml was maintained between 15 min and 84 h after intramuscular administration. The intramuscular bioavailability of the drug was 89.1±4.2%. The dosage regimens to maintain the minimum therapeutic serum concentrations of OTC following intramuscular administration of OTC-LA were computed.  相似文献   

3.
The disposition kinetics, urinary excretion and a dosage regimen for ciprofloxacin after a single intravenous administration of 5 mg/kg was investigated in 5 healthy buffalo calves. The disposition kinetics were best fitted to a three-compartment open model. After 1 min, the concentration of ciprofloxacin in plasma was 8.50±0.39 g/ml and the minimum therapeutic concentration was maintained for 10 h. The elimination half-life and volume of distribution were 3.88 and 0.08 h and 3.97±0.22 L/kg, respectively. The total body clearance and T/P ratio were 0.709±0.025 L/kg per h and 6.13±0.54, respectively. Approximately 28.3% of the total administered dose of ciprofloxacin was recovered in urine within 24 h of administration. To maintain a minimum therapeutic plasma concentration of 0.10 g/ml, a satisfactory intravenous dosage regimen of ciprofloxacin, computed on the basis of disposition kinetic data obtained in healthy buffalo calves, would be 3 mg/kg repeated at 12 h intervals.  相似文献   

4.
A pharmacokinetic study of demeclocycline was carried out following intravenous administration at 5 mg/kg body weight in lactating goats. Demeclocycline appeared within 5 min in plasma, interstitial fluid (isf) and urine, while it appeared at 1 h in milk. Peak concentrations of 21.70±4.06, 2.67±0.23, 5.65±0.45 and 82.23±10.06 g/ml were attained at 5 min and at 6, 8 and 8 h in plasma, isf, milk and urine respectively. A potentially therapeutic concentration of 0.5 g/ml was maintained from 5 min–36 h, 30 min–30 h, 1–36 h and 5 min–48 h in plasma, isf, milk and urine respectively. The drug was detectable in all the above biological fluids for at least 48 h. A low distribution half life (t1/2) of 0.44±0.04 h and a high elimination half life (t1/2) of 19.24±1.22 h denote rapid distribution but very slow elimination of the drug in goats. A high tissue plasma concentration ratio [K12:(K2I–)] of 5.12±0.97 during the elimination phase and a Vdarea of 1.59±0.18 L/kg indicate uniform distribution of demeclocycline in the tissues and body fluids of goats. The dosage regimen for maintaining minimum plasma concentration (C min = MIC) of 0.5, 1.0 and 1.5 g/ml at selected dosage intervals of 12 and 24 h was also calculated.  相似文献   

5.
The disposition kinetics and urinary excretion of pefloxacin after a single intravenous administration of 5 mg/kg were investigated in crossbred calves and an appropriate dosage regimen was calculated. At 1 min after injection, the concentration of pefloxacin in the plasma was 18.95±0.892 g/ml, which declined to 0.13±0.02 g/ml at 10 h. The pefloxacin was rapidly distributed from the blood to the tissue compartment as shown by the high values for the initial distribution coefficient, (12.1±1.21 h–1) and the constant for the rate of transfer of drug from the central to the peripheral compartment, K 12 (8.49±0.99 h–1). The elimination half-life and volume of distribution were 2.21±0.111 h and 1.44±0.084 L/kg, respectively. The total body clearance (ClB) and the ratio of the drug present in the peripheral to that in the central compartment (P/C ratio) were 0.454±0.026 L/kg h) and 5.52±0.519, respectively. On the basis of the pharmacokinetic parameters obtained in the present study, an appropriate intravenous dosage regimen for pefloxacin in cattle for most of the bacteria sensitive to it would be 6.4 mg/kg repeated at 12 h intervals.  相似文献   

6.
The plasma levels, disposition kinetics and a dosage regimen for pralidoxime (2-PAM) were investigated in male buffalo calves following single intramuscular administration (15 or 30 mg/kg). The effects of 2-PAM on various blood enzymes were also determined. The absorption half-life, elimination half-life, apparent volume of distribution and total body clearance of 2-PAM were 1.08±0.19 h, 3.14–3.19 h, 0.83–1.01 L/kg and 184.9–252.1 ml/(kg h), respectively. At doses of 15 and 30 mg/kg body weight, a plasma concentration 4 g/ml was maintained for up to 4 and 6 h, respectively. Pralidoxime significantly lowered the serum level of transferases, phosphatases and lactate dehydrogenase but did not influence the acetylcholinesterase and carboxylesterase enzymes. The most appropriate dosage regimen for 2-PAM in the treatment of organophosphate toxicity in buffaloes would be 25 mg/kg followed by 22 mg/kg at 8 h intervals.  相似文献   

7.
The pharmacokinetics of sulphadimidine after a single dose (200 mg/kg i.v.) was studied in five healthy lactating buffaloes. The study revealed that the drug attained its peak concentration of 314.0±13.0, 242.4±3.0 and 100.2±2.5 g/ml at 15 min, 30 min and 12 h in plasma, milk and uterine fluid, respectively. The pharmacokinetic parameters calculated by a 2-compartment open model gave values for t1, t1 and vdarea of 2.10±0.36 h, 12.36±0.57 h and 1.23±0.07 L/Kg, respectively. A high vdarea as well as a value of 0.74±0.08 for K12:K21- (tissue Plasma) indicates better penetration of the drug into the different body fluids and tissues, which is further supported by a high concentration obtained in milk and uterine fluid. The therapeutic concentration (50 g/ml) was maintained for around 24 h in plasma and milk and 12 h in uterine fluid. The results suggest that, apart from its use in systemic infections, the drug can be effectively used by the i.v. route in uterine and mammary gland infections. The dosages for maintaining concentration of 50 g/ml, 100 g/ml and 150 g/ml at convenient dosage intervals of 12 and 24 h were also determined.  相似文献   

8.
The synthetic androgen 19-nortestosterone (-NT) has been used illegally as a growth promoter in cattle production in the European Union. Elimination of -NT and its metabolites in plasma, urine and bile was studied in three cattle with cannulated gallbladders following intramuscular injection at a single site of 500 mg of the laurate ester (NTL) containing 300.5 mg -NT. Using enzyme immunoassay quantification, plasma Cmax of free -NT was 0.5±0.15 g/L (mean±SEM). Concentrations of free -NT in plasma were consistently greater than the assay limit of quantification (0.12 g/L) for 32.7±13.42 days. Mean residence time for free -NT in plasma was 68.5±20.75 days. Following sample preparation by immunoaffinity chromatography, high-resolution GC-MS was used to quantify -NT and -NT in urine and bile. -NT was detected irregularly in urine from two of the three animals post injection. The principal metabolite present in the urine, -NT, was detected for 160.3±22.67 days post injection. Cmax for -NT in urine was 13.7±5.14 g/L. Mean urinary AUC0–183 days for -NT was 845.7±400.90 (g h)/L.In bile, -NT was the only metabolite detected for 174.3±8.67 days post treatment. Cmax for -NT in bile was 40.8±12.70 g/L and mean biliary AUC0–183 days for -NT was 1982.6±373.81 (g h)/L. Concentrations of -NT in bile samples were greater than those in urine samples taken at the same time. The mean ratio of biliary:urinary AUC0–183 days was 3.0±0.72. It is concluded that bile is a superior fluid for detection of -NT following injection of NTL, owing to the longer period during which residues may be detected after administration.  相似文献   

9.
The pharmacokinetics of thiamphenicol in lactating cows   总被引：2，自引：0，他引：2  
The pharmacokinetics of thiamphenicol were studied after intravenous and intramuscular administration of 25 mg/kg body weight in lactating cows. Distribution (t 1/2) and elimination (t 1/2) half-lives of 6.10±1.39 min and 1.60±0.30 h, respectively, were obtained after intravenous administration. The body clearance was 3.9±0.077 ml/kg per min and the apparent volume of distribution was 1220.79±256.67 ml/kg. The rate at which thiamphenicol appeared in the milk, as indicated by the penetration half-life (t 1/2P) (serum to quarters), was found to be 36.89±11.14 min. The equivalent elimination half-life (t 1/2E) (quarters to serum) from the milk was 3.62±1.06 h and the peak thiamphenicol concentration in the milk was 23.09±3.42 µg/ml at 2.5±0.32 h.After intramuscular injection, the elimination half-life was 2.2±0.40 h, the absorption half-life was 4.02±1.72 min and the peak concentration in the serum was 30.90±5.24 µg/ml at 23±8.4 min. The bioavailability after intramuscular administration approached 100%. The penetration half-life was 50.59±6.87 min, the elimination half-life was 5.91±4.97 h and the mean peak concentration in the milk was 17.37±2.20 µg/ml at 3.4±0.22 h.Abbreviations AUC area under the concentration-time curve - CAP chloramphenicol - C max peak concentration - IM intramuscular - IV intravenous - TAP thiamphenicol - t 1/2 distribution half-life - t 1/2 elimination half-life - V c volume of central compartment - V d volume of distribution  相似文献   

10.
The aim of this study was to elucidate some of the pharmacokinetic parameters of pefloxacin in lactating goats (n = 5) following intravenous (i.v.) or intramuscular (i.m.) injections of 10 mg/kg bw. Serially obtained serum, milk and urine samples were collected at precise time intervals, and the drug concentrations were assayed using a microbiological assay. A two-compartment open model best described the decrease of pefloxacin concentration in the serum after intravenous administration. The maximum serum concentration (C p 0 ) was 8.4±0.48 g/ml; elimination half-life (t 1/2) was 1.6±0.3 h; total body clearance (Cltot) was 3.6±0.3 L/kg/h; steady-state volume of distribution (V dss) was 5.14±0.21 L/kg; and the area under the curve (AUC) was 2.78±0.22 g.ml/h. Pefloxacin was absorbed rapidly after i.m. injection with an absorption half-life (t 1/2ab) of 0.32±0.02 h. The peak serum concentration (C max) of 0.86±0.08 g/ml was attained at 0.75 h (T max). The absolute bioavailability after i.m. administration was 70.63±1.13% and the serum protein-bound fraction ranged from 7.2% to 14.3%, with an average value of 9.8±1.6%. Penetration of pefloxacin from the blood into the milk was rapid and extensive, and the pefloxacin concentration in milk exceeded that in serum from 1 h after administration. The drug was detected in milk and urine for 10 and 72 h, respectively; no samples were taken after 72 h.  相似文献   

11.
The study elucidated the pharmacokinetics of streptomycin in healthy lactating she-buffaloes after a single intramuscular (IM) injection (10 mg/kg). The drug attained its peak concentrations of 24.39±2.67, 0.45±0.05 and 5.06±0.18 g/ml at 1, 4 and 1 hour in plasma, milk and uterine fluid respectively. Calculations based on the assumption of a 2-compartment model gave a plasma t1/2 () of 4.01±0.44 h and an apparent volume of distribution [Vd(area)] of 0.47±0.06 l/kg. The drug was detectable in the plasma, milk and uterine fluid for 30, 8 and 12 hours, respectively. A therapeutic concentration of the drug was maintained for 6 to 7 hours in the plasma and for around 1 hour only in the uterine fluid. However, a therapeutic level could not be achieved in milk at any time. The results suggest that the drug can be used clinically by the IM route against streptomycin susceptible systemic infections but not those in the uterus and mammary gland.  相似文献   

12.
The pharmacokinetics of a slow-release theophylline formulation was investigated following intravenous and oral administration at 10 mg/kg in horses. A tricompartmental model was selected to describe the intravenous plasma profile. The elimination half-life (t1/2) was 16.91 ± 0.93 h, the apparent volume of distribution (V d) was 1.35 ± 0.18 L/kg and the body clearance (ClB) was 0.061 ± 0.009 L kg–1 h. After oral administration the half-life of absorption was 1.24 ± 0.30 h, and the calculated bioavailability was above 100%. Thet1/2 after oral administration was 18.51 ± 1.75 h, only a little longer than that after intravenous administration. The slow release formulation did not exhibit any advantage in prolonging thet1/2 of theophylline in the horse.  相似文献   

13.
This paper reports the milk protein polymorphism, the allele frequencies of variants and the possible linkages among various combinations of milk protein phenotypes in the Kangayam cattle of south India. Milk samples from 156 Kangayam cows were typed by starch gel and polyacrylamide gel electrophoresis for caseins and whey proteins, respectively. All the four milk protein components studied, s1-casein, -casein, -lactoglobulin and -lactalbumin, exhibited polymorphism with high allele frequencies of 0.9231±0.0151 for s1-casein C, 0.9263±0.0148 for -casein A, 0.9135±0.0159 for -lactoglobulin B and a relatively high frequency of 0.6218±0.0275 for -lactalbumin A. The mean heterozygosity estimated over all the four milk protein loci was 0.2420. Genetic equilibrium was observed among all the loci studied, except -lactalbumin. Linkage analysis confirmed the non-independence between s1- and -caseins and between caseins and -lactalbumin phenotypes.  相似文献   

14.
The effect of endotoxin-induced fever on the pharmacokinetics and dosage regimen of cefuroxime was investigated in buffalo calves following a single intravenous dose of 10 mg/kg body weight. The fever was induced by intravenous administration of E. coli endotoxin at a dose of 1 g/kg body weight. The distribution and elimination half-lives were 0.100 h and 1.82 h, respectively, in healthy and 0.109 h and 2.28 h, respectively, in febrile buffalo calves. About 91% of the administered dose was excreted in the urine within 24 h. There was no effect of fever on the plasma protein binding of cefuroxime. The dosage regimen for intravenous administration of cefuroxime may be reduced in febrile conditions but the probability of this was only 0.3.  相似文献   

15.
The purpose of the present investigation was to test the hypothesis that drug-induced changes in rumen contractions influence feed intake in dwarf goats. Intravenous (i.v.) administration of clonidine (1 g kg-1 min-1 for 10 min), xylazine (1 g kg-1 min-1 for 10 min), and PGF-2 (10 g kg-1 min-1 for 15 min) caused bradycardia and inhibition of rumen contractions. However, no appetite-stimulating effect of these drugs was observed. Other clinical changes induced by the 2-adrenergic agonists included slight sedation and a decrease in body temperature; all clinical effects of clonidine and xylazine were partly antagonized by tolazoline pretreatment (10 g kg-1 min-1 for 30 min). These results suggest that the CNS control of feeding differs in ruminants and monogastric species.In dwarf goats fasted for 2 h, i.v. administration of oxytocin (0.01 IU kg-1 min-1 for 15 min), vasopressin (0.01 IU kg-1 min-1 for 15 min), octapressin (0.003 IU kg-1 min-1 for 15 min) or PGE (0.8 g kg-1 min-1 for 15 min) did not change feeding behaviour during the two observation periods (0–30 min and 180–210 min after drug infusion, respectively). In previous studies, similar doses of these drugs induced changes in heart rate and inhibition of rumen contraction in goats. These findings demonstrate that drug-induced changes in forestomach contractions do not simply cause changes in feeding behaviour. The i.v. infusion of the PGF2 analogues etiproston (10 g kg-1 min-1 for 15 min), luprostiol (30 g kg-1 min-1 for 15 min), cloprostenol (1 g kg-1 min-1 for 15 min) and tiaprost (1 g kg-1 min-1 for 15 min) induced hypophagic effects and stimulated intestinal propulsion.  相似文献   

16.
Florfenicol, a monofluorinated analogue of thiamphenicol, has a broad antibacterial spectrum. The pharmacokinetics of florfenicol was studied following a single intravenous (i.v.) or intramuscular (i.m.) injection at a dose of 20 mg/kg body weight in healthy male camels, sheep and goats. The concentration of florfenicol in plasma was determined using a microbiological assay. Pharmacokinetic analysis was performed using a two-compartment open model. Following i.m. administration, the maximum plasma concentration of florfenicol (C max) reached in camels, sheep and goats was 0.84±0.08, 1.04±0.10 and 1.21±0.10 g/ml, respectively, the the time required to reach C max (t max) in the same three respective species was 1.51±0.14, 1.44±0.10 and 1.21±0.10 h. The terminal half-life (t 1/2) and the fraction of the drug absorbed (F%) in camels, sheep and goats were 151.3±16.33, 137.0±12.16 and 127.4±11.0 min, and 69.20%±7.8%, 65.82%±6.7% and 60.88%±5.9%, respectively. The MRT in the same three respective species was 4.01±0.45, 3.42±0.39 and 2.98±0.32 h. Following i.v. administration, the terminal half-life (t 1/2) and total body clearance (ClB) in camels, sheep and goats were 89.5±9.2, 78.8±8.3 and 71.1±8.9 min and 0.33±0.04, 0.30±0.03 and 0.27±0.03 L/h per kg, respectively. The area under the curve (AUC0–) and the mean residence time (MRT) in the same three respective species were 60.61±6.98, 62.45±6.56 and 74.07±7.85 g/ml per h, and 2.71±0.31, 2.34±0.25 and 2.11±0.23 h. These data suggest that sheep and goats absorb and clear florfenicol to a broadly similar extent, but the rate and extent of absorption of the drug tends to be higher in camels. Drug treatment caused no clinically overt adverse effects. Plasma enzyme activities and metabolites indicative of hepatic and renal functions measured 1, 2, 4 and 7 days following the drug treatment were within the normal range, indicating that the drug is safe at the dose used.  相似文献   

17.
The plasma concentrations and pharmacokinetics of the fluoroquinolone antimicrobial agent pefloxacin, following the administration of a single intravenous (10 mg/kg) or oral (20 mg/kg) dose, were investigated in healthy female goats. The antimicrobial activity in plasma was measured at predetermined times after drug administration by an agar well diffusion microbiological assay, using Escherichia coli (ATCC 25922) as the test organism. Concentrations of the drug 0.25 g/ml were maintained in plasma for up to 6 and 10 h after intravenous (IV) or oral administration of pefloxacin, respectively. The concentration–time data for pefloxacin in plasma after IV or oral administration conformed to two- and one-compartment open models, respectively. Plasma pefloxacin concentrations decreased rapidly during the initial phase after IV injection, with a distribution half-life (t 1/2 ) of 0.10±0.01 h. The terminal phase had a half-life (t 1/2 ) of 1.12±0.21 h. The volume of distribution at steady state (V dss), mean residence time (MRT) and total systemic clearance (ClB) of pefloxacin were 1.08±0.09 L/kg, 1.39±0.23 h and 821±88 (ml/h)/kg, respectively. Following oral administration of pefloxacin, the maximum concentration in the plasma (C max) was 2.22±0.48 g/ml and the interval from administration until maximum concentration (t max) was 2.3±0.7 h. The absorption half-life (t 1/2 ka), mean absorption time (MAT) and elimination half-life of pefloxacin were 0.82±0.40, 4.2±1.0 and 2.91±0.50 h, respectively. The oral bioavailability of pefloxacin was 42%±5.8%. On the basis of the pharmacokinetic data, a dosage regimen of 20 mg/kg, IV at 8 h intervals or orally twice daily, is suggested for treating infections caused by drug-sensitive pathogens in goats.  相似文献   

18.
A pharmacokinetic study of ampicillin (6 mg/kg intravenous) revealed that the peak concentrations of 17.81±1.25, 5.64±2.24 and 1.09±0.10 g/ml of the drug were attained at 15 min, 30 min and 2 h in plasma, milk and uterine fluid respectively. A therapeutic concentration of 0.1 g/ml was maintained from 15 min–8 h, 15 min–6 h and 30 min–6 h in plasma, milk and uterine fluid. Hence, the drug may be used effectively in mammary gland and uterine infections apart from its use in other systemic infections.  相似文献   

19.
A pharmacokinetic study of doxycycline after intravenous administration at 5 mg/kg body weight in goats revealed that a concentration of 0.5 g/ml was maintained for 5 min-2 h, 4–12 h, 2–12 h and 5 min- >48 h in plasma, interstitial fluid, milk and urine respectively. The low t1/2 of 0.73±0.11 h and high t1/2 of 16.63±1.58 h show that the drug is rapidly distributed but slowly eliminated from the body. The tissue:plasma concentration of 4.86±1.06 during the elimination phase [K12/(K21-)] indicates a high expected tissue concentration, which is supported by similarly increased drug concentration in interstitial fluid and milk. The high Vdarea of 9.78±0.86 L/kg observed denotes that, apart from its wide distribution, the drug may be stored in fat depots as it is known to be highly lipophilic. As the drug maintained a therapeutic concentration for a shorter time in plasma, and the calculated dose rate for maintaining a minimal plasma concentration of 0.5–1.5 g/ml is relatively high, it may not be of much use in treating septicaemia in this species. Since the observed tissue:plasma concentration was higher and a therapeutic concentration was maintained in interstitial fluid and milk for longer, the drug can be used for other systemic infections at a lower dose rate than that required for treating septicaemia. As the drug maintained a very high concentration in urine, it may be of particular value in treating urinary tract infections caused by sensitive micro-organisms.  相似文献   

20.
Muscarinic and -adrenoceptors were identified in airway epithelium, smooth muscle and lung parenchyma from Holstein-Friesian calves and cows and were characterized with [3H]quinuclidinyl benzilate and [3H]dihydroalprenolol, respectively. The muscarinic receptor density in the smooth muscle of cows (B max=4803±245 fmol/mg protein) was 33% greater (p<0.01) than in calves. Low receptor numbers were detected in the epithelium and parenchyma. In both calves and cows, the density of epithelial -adrenoceptors was twice as high as in smooth muscle and parenchyma. The quantity of -adrenoceptors in the tracheal epithelium (B max=994±83 fmol/mg protein) and smooth muscle (B max=492±41 fmol/mg protein) in cows was respectively 37% (p<0.001) and 35% (p<0.01) lower than in calves. Adenylate cyclase (AC) assays indicated that the basal and the (–)-isopropylnoradrenaline- (ISO-) stimulated cAMP production were not significantly different between the calves and cows. After stimulation with NaF, significantly higher cAMP production was found in all tissues from cows. Significant correlations were found between absolute AC responses to NaF and -adrenoceptor density in epithelium (r=–0.75,p<0.001) and smooth muscle (r=–0.63,p<0.01). It seems that, in older animals, the production of cAMP is independent of the number of receptors, indicating the presence of fully active compensatory mechanisms.Abbreviations AC adenylate cyclase - cAMP intra-cellular adenosine monophosphate - G-protein GTP binding protein - GTP guanosine 5-triphosphate - ISO isopropylnoradrenaline - M muscarine - QNB quinuclidinyl benzilate  相似文献   

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