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1.
Twenty-two young cross-bred swine were treated either intravenously or orally with potassium penicillin G. The pharmacokinetics of penicillin G were determined in plasma and tissues. The plasma half-life of penicillin G in swine was found to be 19.45±1.69 min, and the distribution and elimination kinetics were found to fit a classical two-compartment model. The volume of distribution was found to be 0.53±0.12 1/kg, and the body clearance was found to be 19.06±5.06 ml/min/kg which exceeded the effective renal plasma flow of 16.50±2.73 ml/min/kg, suggesting that the drug was eliminated both by tubular excretion and glomerular filtration. The elimination rate constants (Beta) for the major organs were as follows: muscle, 0.00343 min-1; lung, 0.0310 min-1; fat, 0.0394 min-1; and kidney, 0.0213 min-1, which compared favorably with the elimination rate constant found in plasma (0.0320 min-1). These values were found to be significantly similar at the level of P < 0.005 in muscle, spleen and fat, and at a level of P < 0.025 in lung tissue. The data indicates that blood plasma would be a satisfactory body fluid for estimating this drug in tissue.  相似文献   

2.
A comparison of i.v., i.m. and s.c. administration erythromycin base in polyethylene glycol at 15 mg/kg and 30 mg/kg body weight was carried out in beef-type calves of approximately 200 kg body weight. Additional evaluations were carried out with oral administration of erythromycin phosphate and erythromycin stearate. Absorption of erythromycin was very slow by both the i.m. and s.c. routes of administration with a Kab of 0.0135 min-1 and 0.0185 min-1 for i.m. and 0.0032 min-1 and 0.0074 min-1 for s.c. at 15 mg/kg and 30 mg/kg, respectively. The bioavailability (32–42%) and peak serum concentrations were much lower with s.c. than with i.m. (60–65%) administration. The disposition of erythromycin administered i.v. appeared to be representative of dose-dependent kinetics rather than dose-independent first-order kinetics inasmuch as the elimination half-time ( t 1/2B) increased from 174.5 ± 13 min for the 15 mg/kg dosage to 239 ± 10.8 min with 30 mg/kg dosage. An acute apparent cardiovascular effect accompanied i.v. administration of erythromycin at 30 mg/kg dosage but not at 15 mg/kg. Severe diarrhea followed oral administration of either erythromycin phosphate or erythromycin stearate.  相似文献   

3.
The pharmacokinetics of sulphadiazine (SDZ) (100 mg/kg, body weight) were investigated in six camels ( Camelus dromedarius ) after intravenous (i.v.) and oral (p.o.) administration. Following i.v. administration, the overall elimination rate constant (β) was 0.029±0.001/h and the half-life ( t ½β) was 23.14±1.06 h. The apparent volume of distribution ( V d(area)) was 0.790±0.075 L/kg and the total body clearance ( Cl B) was 23.29±2.50 mL/h/kg. After p.o. administration, SDZ reached a peak plasma concentration ( C max(cal.)) of 62.93±2.79 μg/mL at a post injection time of ( T max(cal.)) 22.98±0.83 h. The elimination half-life was 19.79±1.22 h, not significantly different from that obtained by the i.v. route. The mean absorption rate constant (Ka) was 0.056±0.002 h−1 and the mean absorption half-life ( t ½Ka) was 12.33±0.37 h. The mean availability ( F ) of sulphadiazine was 88.2±6.2%.
  To achieve and maintain therapeutically satisfactory plasma SDZ levels of 50 μg/mL, the priming and maintenance doses would be 80 mg/kg and 40 mg/kg intravenously and 90 mg/kg and 45 mg/kg orally, respectively, to be repeated at 24 h intervals.  相似文献   

4.
Hens were given single intravenous or oral doses (30 mg/kg body weight) of metronidazole and the plasma concentrations of the drug were determined by high-performance liquid chromatography (HPLC) at intervals from 10 min to 24 h after drug administration. Pharmacokinetic variables were calculated by the Lagrange algorithm technique. The elimination half-life ( t 1/2β) after the intravenous injection was 4.2 ± 0.5 h, the volume of distribution ( V d(ss)) 1.1±0.2 L/kg and the total body clearance ( Cl B) 131.2 ± 20 mL/h.kg. Oral bioavailability of the metronidazole was 78 ± 16%. The plasma maximum concentration ( C max) 31.9 ± 2.3 μg/mL was reached 2 h after the oral administration and the oral elimination half-life ( t 1/2β) was 4.7 ± 0.2 h. The binding of metronidazole to proteins in hen plasma was very low (less than 3%). Whole body autoradiography of [3H] metronidazole in hens and quails showed an even distribution of labelled material in various tissues at short survival intervals (1-4 h) after oral or intravenous administration. A high labelling was seen in the contents of the small and large intestines. In the laying quails a labelling was also seen in the albumen and in a ring in the periphery of the yolk at long survival intervals. Our results show that a concentration twofold above the MIC is maintained in the plasma of hens for at least 12 h at an oral dose of 30 mg/kg metronidazole.  相似文献   

5.
Simultaneous pharmacokinetic-pharmacodynamic (PK-PD) models of meperidine in Soats were established by utilizing the P3 wave of the cerebral evoked potentials as an analgesic measurement. An effect compartment linked to the central compartment was postulated in the models. The hypothetical drug amount in the effect compartment was related to the observed analgesia through the Hill equation. After intramuscular (i. m., n = 16) and intravenous (i. v., n = 13) dosing (5 mg/kg), the elimination rate constants of meperidine in the effect compartment ( K eO) were 0.3744 ± 0.2546 and 0.1123 ± 0.0428 min-1, drug concentrations in the effect compartment generating half maximal analgesia (EC(50)) were 0.70 ± 0.33 and 0.41 ± 0.26 μg/ml, the maximal effects (Emax) were 89.63 ± 15.63 and 85.92 ± 9.64%, and the Hill coefficients (S) were 2.61 ± 1.21 and 2.37 ± 1.15, respectively. K eO and EC(50) with i.m. dosing were significantly greater than with i.v. injection. However, administration route had no influence on S, Emax and the total amount of effect ( AUE ). The predicted peak effect (Emax^) of 64.44 ± 14.64 and 66.02 ± 11.51% were achieved at 14.7 ± 7.4 and 8.5 ± 2.2 min after i.m. and i.v. dosing, respectively. Peak analgesia appeared much later than peak plasma concentration, but simultaneously with peak CSF level both after i.m. and i.v. dosing. An obvious hysteresis was demonstrated between plasma concentration and analgesic effect. This study demonstrates that meperidine analgesia can be predicted using a PK-PD model, but not by PK data alone. Both i.m. and i.v. administration routes were evaluated kinetically and dynamically.  相似文献   

6.
Pharmacokinetics of chloramphenicol in the neonatal horse   总被引：1，自引：0，他引：1  
Chloramphenicol sodium succinate was administered as an intravenous bolus (50 mg/kg) to eight foals which weighed 49–57 kg (mean ± 1 standard deviation = 53.19 ± 2.66) each, and were 1–9 days (4.5 ± 2.56) of age. The drug was rapidly distributed and followed first-order elimination. Mean pharmacokinetic values were: zero-time serum concentration (C0) = 36.14 μg/ml (±14.80); apparent specific volume of distribution ( Vd ) = 1.614 1/kg (±0.669); and elimination rate constant ( K ) = 0.7295 h-1 (±0.3066) which corresponds to a biological half-life ( t 1/2) = 0.95 h. These values do not differ greatly from those reported for adult horses and ponies.
A suspension of chloramphenicol was administered by nasogastric tube (50 mg/kg) to a second group of seven foals which weighed 49 to 57 kg (51.34 ± 2.82) each and were 1 to 7 days (4.43 ± 1.90) of age. A mean peak serum chloramphenicol concentration of 23.97 μg/ml (±7.06) was achieved 1.14h (±0.63) after administration. The bioavailability of this preparation was 83.27 percent.  相似文献   

7.
Concentrations of the non-steroidal anti-inflammatory drug (NSAID) alclofenac were determined by a sensitive high performance liquid chromatographic procedure in plasma and urine of horses following oral administration of a dose of 3 g. In plasma, alclofenac was present in detectable concentrations for 72 h. The plasma disposition in individual horses was best described by a bi-compartmental model with two successive rate constants ka1= 0.05 ± 0.06 h-1 and ka2= 0.06 ± 0.01 h-l. Alclofenac half-lives t ½ and t 1/2β were 1.0 ± 0.8 h and 6.9 ± 1.5 h, respectively. Maximal concentrations (38.9 ± 16.2 μg/ml) were obtained after 8.5 ± 2.4 h. Alclofenac was detected in urine for at least 48 h after dosing. The percentage of the dose excreted as unchanged alclofenac in 12 h was very low (0.68 ± 0.19%), total (free + conjugated) alclofenac accounted for 2.16 ± 0.55% of the dose.  相似文献   

8.
The ability of the SAV 6 high-frequency jet ventilator to effectively ventilate three anesthetized, paralyzed cats (3.2–4.2 kg), two small dogs (7.2 and 10.0 kg), six medium-sized dogs (20.5–25.0 kg), and three large dogs (36.0–43.0 kg) via a 14-gauge (dogs) or a 16-gauge (cats) catheter placed percutaneously into the trachea via the cricothyroid membrane or into a preplaced endotracheal tube was evaluated. The lowest driving pressure within the range of 0.25 to 2.0 kg/cm2 (1 kg/cm2= 14.2 psi) and the highest cycle rate within the range of 60 to 240 per minute that would generate a PaCO2 of 30 ± 3 mm Hg were determined.
All animals could be ventilated to a PaC02 of 30 ± 3 mm Hg by the endotracheal tube and transtracheal route, except the largest dogs, which couid be ventilated to an average PaC02 of 36 mm Hg by the transtracheal route. The transtracheal route consistently required higher driving pressures and lower cycle rates than did the endotracheal tube route. Cats could be ventilated with a driving pressure of 0.25 kg/cm2; small dogs could be ventilated with 0.5 to 1.0 kg/cm2; medium-sized dogs with 1.0 to 1.5 kg/cm2; and large dogs with 1.5 to 2.0 kg/cm2.
The SAV 6 high-frequency jet ventilator can effectively ventilate cats and dogs (7.2–43.0 kg) via a transtracheal catheter and an endotracheal tube.  相似文献   

9.
Objective  We hypothesized that propofol can produce rapidly-reversible, dose-dependent standing sedation in horses.
Study design  Prospective randomized, blinded, experimental trial.
Animals  Twelve healthy horses aged 12 ± 6 years (mean ± SD), weighing 565 ± 20 kg, and with an equal distribution of mares and geldings.
Methods  Propofol was administered as an intravenous bolus at one of three randomized doses (0.20, 0.35 and 0.50 mg kg−1). Cardiovascular and behavioral measurements were made by a single investigator, who was blinded to treatment dose, at 3 minute intervals until subjective behavior scores returned to pre-sedation baseline values. Continuous data were analyzed over time using repeated-measures anova and noncontinuous data were analyzed using Friedman tests.
Results  There were no significant propofol dose or temporal effects on heart rate, respiratory rate, vertical head height, or jugular venous blood gases (pHv, PvO2, PvCO2). The 0.35 mg kg−1 dose caused mild sedation lasting up to 6 minutes. The 0.50 mg kg−1 dose increased sedation depth and duration, but with increased ataxia and apparent muscle weakness.
Conclusions and clinical relevance  Intravenous 0.35 mg kg−1 propofol provided brief, mild sedation in horses. Caution is warranted at higher doses due to increased risk of ataxia.  相似文献   

10.
Pharmacokinetic parameters which describe the distribution and elimination of sulphadimidine were determined in normal dogs and dogs in which fever was produced by an intravenous injection of escherichia and staphylococcal species of bacteria. Sulphadimidine was injected as a single intravenous bolus at the dose of 100 mg/kg and the kinetics of the drug were described in terms of the bi-exponential expression: Cp = Ae -α t + Be -β t . The distribution half-times of the drug were 1.52 h in the normal and 0.81 h in the febrile dogs. The drug distribution was significantly more rapid ( P < 0.05) in febrile than in normal dogs. Average ± SD values for the half-lives of the drug were 16.2 ± 5.7 h in normal and 16.7 ± 4.7 h in the febrile dogs. The apparent volume of distribution ( V ' d (area)) was 628 ± 251 ml/kg in the normal dogs, and was not statistically different from 495 ± 144 ml/kg in the febrile dogs. The volume of the central compartment ( V ' c ) was 445 ± 55 ml/kg in normal dogs and this was significantly higher ( P < 0.01) than the V ' c of 246 ± 72 ml/kg in the febrile dogs. The body clearance was 22.4 ± 4.8 and 20.2 ± 3.6 ml/hour. kg in the normal and febrile dogs, respectively. The investigation revealed that the dosage regimen of sulphadimidine did not differ significantly between normal and febrile dogs.  相似文献   

11.
Tissue distribution and elimination kinetics of oxytetracycline in sixteen organs and body fluids were determined in young pigs following intravenous and oral administration. Seventeen non-fasted pigs, 8–10 weeks of age, weight range 16.4–34.5 kg were dosed intravenously at a dose rate of 11 mg/kg bodyweight. An additional seventeen weaning pigs, 12–14 weeks of age, weight range 27.2–36.3 kg were dosed orally at a dose rate of 48–65 mg/kg bodyweight. Oxytetracycline was rapidly distributed (half-life, 6.71 ± 1.13 min) in swine. The mean volume of distribution was 1.26 ± 0.18 l/kg and overall body clearance was 3.82 ± 0.59 ml/kg/min. The elimination half-life of oxytetracycline in pigs was 3.87 ± 0.62 h, which is shorter than has been observed in other domestic animal species. Oxytetracycline became rapidly and efficiently involved in enterohepatic cycling, with as much as 70% of a total intravenous dose being available for reabsorption from the gastrointestinal tract within 1 h after administration. This high degree of enterohepatic recycling prolonged the half-life, and the large amount of drug that entered the enteric tract contributed to the high volumes of distribution and high k 12/ k 21 ratios. The excellent tissue penetration of this drug further contributed to the high volume of distribution and high k 12/ k 21 ratios obtained. Relationships between plasma and tissue depletion for several major edible organs were found to be statistically significant. Blood plasma is proposed as a body fluid for monitoring oxytetracycline tissue residues.  相似文献   

12.
The bioavailability of levamisole in rabbits was determined after subcutaneous and oral administration at three dose levels of 12.5, 16.0 and 20.0 mg/kg. After non-compartmental analysis the mean values obtained were: C max=3.54, 4.51 and 5.39 μg/ml; t max= 12.0, 22.0 and 20.0 min; F = 134.8, 105.4 and 124.1% after subcutaneous administration for each dose, respectively, and C max= 0.71, 1.32 and 1.77 μg/ml; t max= 46.0, 96.0 and 84.0 min; F = 53.0, 62.0 and 80.7% after oral administration. The extent and rate of absorption from the two routes differed significantly, except for t max at the 12.5 mg/kg dose. After compartmental analysis the pharmacokinetics of levamisole was characteristic of a two-compartment open model in 13 rabbits and of a one-compartment open model in two rabbits after subcutaneous administration, while it was two compartmental in nine and one compartmental in six rabbits after oral administration. The ka values were 0.321, 0.145 and 0.145 min-1 after subcutaneous administration and 0.054, 0.023 and 0.027 min1 after oral administration. There were no significant differences between the values of C max, t max and AUC calculated by compartmental and non-compartmental analysis.  相似文献   

13.
Objective  To investigate the effects of a low-dose constant rate infusion (LCRI; 50 μg kg−1 minute−1) and high-dose CRI (HCRI; 200 μg kg−1 minute−1) lidocaine on arterial blood pressure and on the minimum alveolar concentration (MAC) of sevoflurane (Sevo), in dogs.
Study design  Prospective, randomized experimental design.
Animals  Eight healthy adult spayed female dogs, weighing 16.0 ± 2.1 kg.
Methods  Each dog was anesthetized with sevoflurane in oxygen and mechanically ventilated, on three separate occasions 7 days apart. Following a 40-minute equilibration period, a 0.1-mL kg−1 saline loading dose or lidocaine (2 mg kg−1 intravenously) was administered over 3 minutes, followed by saline CRI or lidocaine LCRI or HCRI. The sevoflurane MAC was determined using a tail clamp. Heart rate (HR), blood pressure and plasma concentration of lidocaine were measured. All values are expressed as mean ± SD.
Results  The MAC of Sevo was 2.30 ± 0.19%. The LCRI reduced MAC by 15% to 1.95 ± 0.23% and HCRI by 37% to 1.45 ± 0.21%. Diastolic and mean pressure increased with HCRI. Lidocaine plasma concentration was 0.84 ± 0.18 for LCRI and 1.89 ± 0.37 μg mL−1 for HCRI. Seventy-five percent of HCRI dogs vomited during recovery.
Conclusion and clinical relevance  Lidocaine infusions dose dependently decreased the MAC of Sevo, did not induce clinically significant changes in HR or arterial blood pressure, but vomiting was common during recovery in HCRI.  相似文献   

14.
The pharmacokinetic properties of norfloxacin were determined in healthy pigs after single intramuscular (i.m.) and intravenous (i.v.) dosage of 8 mg/kg body weight After i.m. and i.v. administration, the plasma concentration-time graph was characteristic of a two-compartment open model. After single i.m. administration, norfloxacin was absorbed rapidly, with a t max of 1.46 ± 0.06 h. The elimination half-life ( t 1/2β) and the mean residence time of norfloxacin in plasma were 4.99 ± 0.28 and 6.05 ± 0.22 h, respectively, after i.m. administration and 3.65 ± 0.16 and 3.34 ± 0.16 h, respectively, after i.v. administration. Intramuscular bioavailability was found to be 53.7 ± 4.4%. Plasma concentrations greater than 0.2 μg/mL were achieved at 20 min and persisted up to 8 h post-administration. Maximal plasma concentration was 1.11 ± 0.03 μg/mL. Statistically significant differences between the two routes of administration were found for the half-lives of both distribution and elimination phases ( t 1/2α, t 1/2β) and apparent volume of distribution (Vd(area)). In pigs, norfloxacin was mainly converted to desethylenenorfloxacln and oxonorfloxacin. Considerable tissue concentrations of norfloxacin, desethylenenorfloxacin, and oxonorfloxacin were found when norfloxacin was administered intramuscularly (8 mg/kg on 4 consecutive days). The concentration of the parent fluoroquinolone in liver and kidney ranged between 0.015 and 0.017 μg/g on day 12 after the end of dosing.  相似文献   

15.
Bioavailability and pharmacokinetics of metoclopramide in cattle   总被引：1，自引：0，他引：1  
The bioavailability of metoclopramide was investigated in three steers following administration of 8 mg/kg by the oral, abomasal (cannula), and intravenous routes, using a Latin square design. The mean (± SD) oral and abomasal bioavailabilitles were 51.3 ± 30.7% and 76.2 ± 15.5%, respectively. The mean value for clearance ( C1 ) was 20.1 ± 5.9 ml/min and the volume of distribution ( V d) was 0.51 ± 0.19 1/kg. Additionalpharmacokmetic parameters for metoclopramide were determined following intravenous administration to seven cows. A predominate two-compartment model of distribution was found in six cows with a t 1/2α harmonic mean of 24.2 min and a range of 11.2–72.4 min, a t 1/2β harmonic mean of 53.1 min and a range of 31.1–134.1 min, a Cl of 42.2 ± 8.7 ml/min, and a V d of 2.1 ± 0.8 1/kg. To better define the relationship between metoclopramide concentration and release of prolactin, a treatment-by-subjects infusion study was conducted in which four different loading doses followed by constant infusion were used. A steady-state metoclopramide concentration ( MCP ss) of 8.8 ± 2.6 ng/ml was associated with a three-fold elevation of prolactin to a mean value of 12.1 ± 3.1 ng/ml in six yearling steers. Steady state serum prolactin concentrations ( PRL ss) did not rise significantly above 23.3 ± 6.9 ng/ml, even when MCP ss reached a concentration of 518.5 ±151.2 ng/ml. The short half-life, moderate V d, low minimum pharmacologically effective concentration, and rapid C1 found for metoclopramide in cattle in this study, suggest that a continuous release device could potentially be useful in the application of this drug in the prevention and treatment of fescue toxicosis.  相似文献   

16.
Phenylbutazone was administered intravenously (i.v.) to a group of four lactating cows at a dosage of 6 mg/kg body weight. Whole plasma, protein-free plasma and milk were analysed for phenylbutazone residues. Pharmacokinetic parameters of total and free phenylbutazone in plasma were calculated using a non compartmental method. In regards to whole plasma data, the mean volume of distribution at steady state ( V ss), was 147 mL/kg body weight, with a mean (± SEM) terminal elimination half-life ( t 1/2) of 40 ± 6 h. The mean clearance ( Cl ) was 3 mL/h/kg body weight. The V ss as determined from the protein-free plasma fraction was 50 021 mL/kg body weight. This larger V ss of free phenylbutazone compared to total plasma phenylbutazone was attributed to a high degree of plasma protein binding, as well as the greater penetration of free phenylbutazone into tissues. The mean t 1/2 of free phenylbutazone was 39 ± 5 h. This similarity to the t 1/2 estimated from total plasma phenylbutazone data is attributed to an equilibrium between free and plasma phenylbutazone during the terminal elimination phase. Mean t 1/2 as determined from milk, applying a urinary excretion rate model, was 47 ± 4 h. Milk clearance of phenylbutazone was 0.009 mL/h/kg body weight, or about 0.34% of total body clearance. Furthermore, evidence suggests that phenylbutazone either binds to milk proteins, or is actively transported into milk, as its concentration in milk was greater than that predicted due to a simple partitioning from plasma into milk.  相似文献   

17.
Medetomidine, an α2-adrenoceptor agonist, is a potent sedative and analgesic agent in the dog. When necessary, its action can be effectively antagonized by atipamezole. The present work was designed to study the effects of these drugs on each others' pharmacokinetics when a single intramuscular dose of medetomidine (50 μg kg-1) was followed by a dose of atipamezole (250 μg kg-1). Three different treatments were used: medetomidine alone, atipamezole alone, and atipamezole after medetomidine. Drug concentrations in plasma were measured by GC-MS. Statistical analysis of the results (anova) revealed significant differences between treatments in the kinetic parameters of medetomidine. Atipamezole decreased the AUC of medetomidine from 41.3 to 28.6 ng h ml"1(P = 0.005), t1/4 from 1.44 to 0.87 h ( P = 0.015), and increased Cl from 21 to 31 ml min-1kg-1(P = 0.017). Differences in V2 did not reach statistical significance. The only statistically significant effects of medetomidine on the pharmacokinetics of atipamezole in this study were the slight decrease of Cl and C max as well as the increase of AUC . It is suggested that the large dose of medetomidine used caused haemodynamic changes, resulting in decreased hepatic circulation and slower drug metabolism. Antagonism by atipamezole restored the hepatic blood flow and, consequently, increased the elimination of medetomidine by biotransformation.  相似文献   

18.
The pharmacokinetics of kanamycin were studied in beagle dogs. A parenteral preparation of kanamycin sulphate (5% aqueous solution), which was given at a dosage level of 10 mg/kg of body weight, was the drug product used. The disposition curve which resulted from the intravenous administration of a single bolus dose of the drug was completely described by the biexponential equation:
C p= 50e-0.1977 t + 36.3e-0.0128 t where C p represents concentration of the drug in the serum at time t (in minutes) and the experimental constants are mean values. Pseudo-distribution equilibrium was rapidly attained and the apparent volumes of the central and peripheral compartments of the two-compartment open model were the same ( ca 125 ml/kg). Body clearance (mean ± S.D., n = 6) of kanamycin was 3.21 ±0.72 ml/kg/min. The half-life of the drug was short (58.18 ± 18.43 min) and independent of the route of parenteral (intravenous and intramuscular) administration. Absorption of kanamycin from the intramuscular site was rapid, with a half-time of 9.08 ± 1.10 min. A systemic availability of 89.1 ± 15.8% was obtained. Based on the bioavailability and disposition kinetics a dosage regimen consisting of the intramuscular injection of the dose (10 mg/kg) at 6 h intervals is proposed. An intravenous infusion rate of 48 μg/kgymin is predicted to establish a steady state serum concentration of 15 μg/ml, which is a therapeutic level of the antibiotic for susceptible micro-organisms.  相似文献   

19.
The pharmacokinetic properties of pradofloxacin and doxycycline were investigated in serum, saliva, and tear fluid of cats. In a crossover study design, six cats were treated orally with a single dose of pradofloxacin (Veraflox® Oral Suspension 2.5%) and doxycycline (Ronaxan® 100 mg) at 5 mg/kg body weight. Following administration, samples of serum, saliva, and tear fluid were taken in regular intervals over a period of 24 h and analysed by turbulent flow chromatography/tandem mass spectrometry. All values are given as mean ± SD. Pradofloxacin reached a mean maximum serum concentration ( C max) of 1.1 ± 0.5 μg/mL after 1.8 ± 1.3 h ( t max). In saliva and tear fluid, mean C max was 6.3 ± 7.0 and 13.4 ± 20.9 μg/mL, respectively, and mean t max was 0.5 ± 0 and 0.8 ± 0.3 h, respectively. Doxycycline reached a mean C max in serum of 4.0 ± 0.8 μg/mL after 4.3 ± 3.2 h. Whilst only at two time-points doxycycline concentrations close to the limit of quantification were determined in tear fluid, no detectable levels were found in saliva. The high concentrations of pradofloxacin in saliva and tear fluid are promising to apply pradofloxacin for the treatment of conjunctivitis and upper respiratory tract infections in cats. As doxycycline is barely secreted into these fluids after oral application the mechanisms of its clinical efficacy remain unclear.  相似文献   

20.
The pharmacokinetics of thiamphenicol were investigated in 10 calves and six lactating cows. It was found that this drug is rapidly absorbed (1 5 min) following intramuscular injection with an absorption rate constant and a bioavailability of 8.7 h-1 and 84%, respectively. The drug appears to be widely distributed into various body fluids, yielding a volume of distribution (Vd(area)) of approximately 0.9 l/kg. The micro-rate constants indicated that the antibiotic rapidly diffuses into the peripheral compartment (k12 > k21). Elimination from plasma is relatively rapid, with a biological half-life of about 1.75 h. Thiamphenicol appears shortly in milk (15 min) after its intravenous administration, and gives milk to plasma concentration ratios greater than one between 4 and 12 h.  相似文献   

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