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1.
恩诺沙星在奶牛血液和乳中药物浓度的监测   总被引：1，自引：1，他引：1  
对 5头患有子宫内膜炎的奶牛经子宫灌注含恩诺沙星的复方制剂 10 0mL ,并于给药 0 ,0 .5 ,1,2 ,4 ,8,12 ,2 4h后 ,用高效液相色谱法为定量手段 ,利用荧光检测器分别测定复方制剂中恩诺沙星及其代谢产物环丙沙星的血药、乳药浓度。结果表明 ,恩诺沙星给药后 2h左右在血中浓度达到最高值 ,然后逐渐下降。至 8h在血浆中的药物浓度为 (0 .6 4± 0 .16 ) μg/mL。 12h后检测不到恩诺沙星。而代谢产物环丙沙星于给药后 4h血药浓度可达最高峰 ,至 12h血药浓度为 (0 .0 5± 0 .0 1) μg/mL ,2 4h已检测不到。对于乳药浓度 ,恩诺沙星及其代谢产物环丙沙星皆于给药后 4h ,浓度达到最高峰 ,分别为 (1.6 9± 0 .30 ) μg/mL和 (0 .4 9± 0 .12 ) μg/mL。 12h后已经检测不到恩诺沙星和环丙沙星。从上述数值可见 ,恩诺沙星吸收较迅速 ,代谢较快、清除较快 ,表明恩诺沙星与环丙沙星在乳中不会形成残留。另外 ,在 8h内恩诺沙星、环丙沙星的血药、乳药浓度值均高于MIC值 ,所以仍具有抗菌作用。  相似文献   

2.
本研究以反相高效液相色谱为定量分析手段,采用5头患子宫内膜炎的奶牛,通过子宫内灌注盐酸环丙沙星（2.5g/头）,研究了盐酸环丙沙星在患子宫内膜炎奶牛体内的药代动力学规律。以二氟沙星为内标,血浆样品经甲醇沉淀蛋白,离心,经针头式过滤器处理,用反相高效液相法测定其中盐酸环丙沙星的浓度。色谱条件为：ODS-1C18柱;测定流动相为0.015mol/L四丁基溴化铵溶液-乙腈（92∶8,V/V）,pH为3.0;流速为1.0mL/min;荧光检测器,激发波长（λex）278nm,发射波长（λem）465nm。通过采用MCPKP房室分析程序,分析血中浓度-时间数据,发现有三头牛血样药时数据符合无吸收三室开放模型。其血样中主要药动学参数为：T1/2α为0.916h、T1/2β为49.20h、AUC高达7.6296mg/（L·h）、Clβ为1.582L/（kg·h）。有两头牛血样药时数据符合一级吸收二室开放模型。其主要药动学参数为：T1/2α为1.26h、T1/2β为10h、AUC高达28.336mg/（L·h）。试验结果表明,盐酸环丙沙星子宫给药吸收快,分布广泛,消除慢。  相似文献   

3.
本研究以反相高效液相色谱为定量分析手段，选用5头患子宫内膜炎的奶牛，通过子宫内灌注盐酸环丙沙星（2.5 g/头），研究了盐酸环丙沙星在患子宫内膜炎奶牛体内的药物动力学规律。以二氟沙星为内标，血浆样品经甲醇沉淀蛋白，离心，经针头式过滤器处理，用反相高效液相法测定其中盐酸环丙沙星的浓度。 色谱条件为：ODS-1C18柱；测定流动相为0.015 mol/L四丁基溴化铵溶液-乙腈（92∶8，V/V），pH为3.0；流速为1.0 ml/min；荧光检测器，激发波长（λex）278 nm，发射波长（λem）465 nm。通过采用MCPKP房室分析程序，分析血中浓度 时间数据，发现有3头奶牛血样药时数据符合无吸收三室开放模型。其血样中主要药动学参数为：T1/2α为0.916 h、T1/2β为49.20 h、AUC高达7.6296 mg/L·h、Clβ为1.582 L/kg·h，β为0.642 h-1。有2头奶牛血样药时数据符合一级吸收二室开放模型。其主要药动学参数为：T1/2α为1.26 h、T1/2β为9.2 h、AUC高达28.336 mg/L·h，β为0.3571 h-1。试验结果表明，盐酸环丙沙星子宫给药吸收快，分布广，消除慢。  相似文献   

4.
为探讨利福昔明悬乳剂灌注泌乳期奶牛乳房后在奶牛乳区的分布情况,进行了奶牛牛乳和血液中药物的药代动力学研究。试验选取6头荷斯坦奶牛,每头奶牛随机选择2个乳区,以每个乳区200 mg的剂量进行单次乳房灌注利福昔明悬乳剂,利用高效液相色谱法检测牛乳与血液中利福昔明的含量。结果表明:利福昔明悬乳剂采用单次乳房灌注给药后,给药乳区36 h内乳头中利福昔明的浓度都在2μg/mL以上,且血液中未检出利福昔明。说明药物主要集中在给药乳区,进入体循环的量极少,并且能在较长时间内具有抑菌作用。  相似文献   

5.
随机收集了8头处于泌乳期的中国荷斯坦奶牛24h内乳样,对乳中尿素氮浓度的昼夜变化情况进行研究。结果发现,同一奶牛个体在不同的时间点乳尿素氮浓度差异较大。因此,单个时间点的乳液尿素氮浓度代表性较差,有必要收集全天乳样。  相似文献   

6.
《中国兽医学报》2019,(11):2233-2237
子宫内膜炎是影响奶牛生产的重要疾病之一,该病的有效防控至关重要。本试验探讨了约氏乳杆菌对LPS诱导的奶牛子宫内膜上皮细胞炎症反应的预防作用。约氏乳杆菌悬浮至10~4,10~5,10~6 CFU/mL后,与奶牛子宫内膜上皮细胞共同培养3 h,添加1 mg/L LPS处理3 h,检测趋化因子IL-8和促炎因子TNF-αmRNA、蛋白分泌量和NF-κB信号通路关键蛋白表达量。结果表明,LPS处理奶牛子宫内膜上皮细胞3 h后,IL-8和TNF-αmRNA和蛋白分泌量均显著上升(P0.05), 10~4 CFU/mL约氏乳杆菌预处理后IL-8、TNF-α表达和NF-κB信号通路关键蛋白均显著降低(P0.05),而10~5或10~6 CFU/mL约氏乳杆菌预处理并未影响IL-8和TNF-α表达。结果提示,约氏乳杆菌具有预防奶牛子宫内膜炎的作用,且10~4 CFU/mL表现出良好的抗炎效用。  相似文献   

7.
目的:探究"产后宫乳康"在治疗奶牛子宫内膜炎的运用效果。方法选取患有子宫内膜炎症的奶牛20头,按照治疗方法的不同分成4组,每组5头,进行治疗效果比较分析。结果:采用"产后宫乳康"治疗奶牛子宫内膜炎,具有高治愈率、低复发率。结论:"产后宫乳康"对奶牛子宫内膜炎具有很好的治疗效果。  相似文献   

8.
用TTC法检测44例经过抗菌药物治疗的患子宫内膜炎荷斯坦奶牛。其中，41例采用子宫内灌注药物治疗，主要药物有土霉素、金霉素和庆大霉素；每个病例治疗1～5次不等，3例采用静脉注射，主要药物有磺胺嘧啶钠和头孢噻啶。结果表明，31例经土霉素子宫内灌注的奶牛，停药后第24h所采的奶样均可检出抗生素；其中6头奶牛在第6d仍然抗生素阳性，残留时间最长的可达8d。8例用金霉素子宫灌注治疗的奶牛，停药后第48h所采的奶样，抗生素检出率100％，其在牛奶中的残留时间为2～5d不等。2例经庆大霉素子宫灌注治疗的患病牛，药残时间分别为1～2d。3头经静脉滴注治疗的病牛，牛奶中的药残时间约达到9d以上。此外，从3头用金霉素子宫内灌注的奶牛采集牛奶用于乳酸菌发酵试验。结果表明，牛奶TTC阳性时，发酵产酸较低。在治疗后6h采集的牛奶都不能正常发酵产酸、凝固。3例试验牛牛奶发酵产生的酸度分别于治疗后第13、24和48h恢复到治疗前的水平。  相似文献   

9.
为研究宫溯康对奶牛产后子宫内膜炎的临床预防效果,本试验选择分娩后胎衣自下的奶牛,试验分为预防组和对照组。预防组奶牛从分娩后24～36h通过消毒过的专用投药器投入3粒宫溯康至奶牛子宫孕角深部;对照组产后子宫不做任何处理。结果表明,试验组奶牛急性子宫内膜炎的发病率为5.3%,而对照组急性子宫内膜炎的发病发病率为24.3%,其发病率显著高于试验组(P<0.05)。宫溯康能显著降低产后奶牛子宫内膜炎的发病率,具有很好的临床应用前景。  相似文献   

10.
试验随机收集了8头处于泌乳期的中国荷斯坦奶牛24h内的尿样和乳样,对我国奶牛尿液中尿素氮浓度的昼夜变化情况以及与乳中尿素氮浓度的相关性进行研究。结果表明:同一奶牛个体在不同时间点的尿中尿素氮浓度差异较大,尿素氮浓度较高的奶牛这种差异更明显,单个时间点的尿中尿素氮浓度代表性较差,有必要收集全天尿液;全天平均乳尿素氮浓度与平均尿液中尿素氮浓度(R2=0.99)和尿液中尿素氮日排泄量(R2=0.97)密切相关(P<0.001),证明了尿素在体液中的扩散理论以及乳尿素氮估测尿氮观点的科学性。  相似文献   

11.
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.  相似文献   

12.
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13.
The single-dose disposition kinetics of danofloxacin were determined in clinically normal lactating cows after intravenous (i.v.) and intramuscular (i.m.) administration of the drug at 1.25 mg/kg. The drug concentrations in blood serum and milk were determined by microbiological assay methods and the data were subjected to kinetic analysis. The mean i.v. and i.m. elimination half-lives ( t ½el) in serum were 54.9 and 135.7 min, respectively. The steady-state volume of distribution ( V ss) was 2.04 L/kg. The drug was quickly absorbed after i.m. injection but a 'flip flop' effect was clearly evident and bioavailability was > 100%. Penetration of danofloxacin from blood into milk was rapid and extensive with drug concentrations in milk exceeding those in serum beginning 90–120 min after i.v. and i.m. administration and onwards. Milk danofloxacin concentrations equal to or higher than the minimal inhibitory concentrations (MIC) for pathogenic Gram-negative bacteria and Mycoplasma species were maintained over ≈ 24 h.
  Concentrations greater than the MIC for Staphylococcus aureus were maintained in the milk for 12 h.  相似文献   

14.
Five Ayrshire cows were given enrofloxacin (5 mg/kg body weight) intravenously (i.v.), intramuscularly (i.m.) and subcutaneously (s.c). The antimicrobial activity was measured in milk and serum samples using the agar-diffusion technique. High-performance liquid chromatography (HPLC) assay was used to study the extent of metabolism of enrofloxacin to dprofloxacin. Analysis of the serum concentration-time data was based on statistical moment theory. Mean t 1/2β of antimicrobial activity in serum was 1.7, 5.9 and 5.6 h after i.v., i.m. and s.c. administration, respectively. Both i.m. and s.c. routes were associated with a marked flip-flop phenomenon. Based on HPLC analysis of serum samples, the half-lives of enrofloxacin and ciprofloxacin were approximately the same. A marked proportion of enrofloxacin was metabolized to ciprofloxacin. The enrofloxacin fraction bound in vitro to serum proteins was 36–45%. About 0.2% of the total enrofloxacin dose was found in milk during the first 24h and the amount transferred did not depend on the route of administration. Based on the HPLC data, enrofloxacin concentration in milk was parallel to that in serum, while ciprofloxacin was concentrated in milk. After i.v. injection, the peak concentration of enrofloxacin in milk was reached between 0.7 and 1.3 h but occurred much later for ciprofloxacin ( t max 5–8 h). After i.m. and s.c. administration the concentration-time curves for both enrofloxacin and ciprofloxacin in milk were shallow and there were no obvious peaks.  相似文献   

15.
The pharmacokinetic properties of ciprofloxacin and its metabolites were determined in healthy chickens after single i.v. and oral dosage of 8 mg ciprofloxacin kg(-1) bodyweight. After i.v. and oral administration, the plasma concentration-time graph was characteristic of a two-compartment open model. Mean (SD) elimination half-life and mean residence time of ciprofloxacin in plasma were 8.84 (2.13) and 8.54 (1.64) hours, respectively, after i.v. administration and 11.89 (1.95) and 13.32 (2.65) hours, respectively, after oral administration. Mean maximal plasma concentration of ciprofloxacin was 2.63 (0.20) microg ml(-1), and the interval from oral administration until maximum concentration was 0.36 (0.07) hours. The mean oral bioavailability of ciprofloxacin was found to be 69.12 (6.95) per cent. Ciprofloxacin was mainly converted to oxociprofloxacin and desethyleneciprofloxacin. Considerable kidney, liver, muscle and skin + fat tissue concentrations of ciprofloxacin and its metabolites oxociprofloxacin and desethyleneciprofloxacin were found when ciprofloxacin was administered orally (8 mg kg(-1) on 3 successive days). It was estimated that mean tissue concentrations of ciprofloxacin and its metabolites ranging between 0.011 to 0.75 microg g(-1) persisted for 5 days.  相似文献   

16.
The excretion of selenium in milk was investigated in twelve ewes. Four of these were injected 12–29 days before, and four immediately after delivery, with Se75-sodium selenite. One month after delivery two ewes were injected with Se75-selenomethionine, and two with Se75-sodium selenite. The Se75-concentration was measured in the milk and its various fractions as well as in the plasma, whole blood and organs of three lambs.The excretion of Se75 into the milk was markedly higher when Se75-selenomethionine was administered than when Se75-sodium selenite was given. The amount of Se75 in the various milk fractions was, to a great extent, proportional to the amount of protein in the fractions; this applied to the administration of organic as well as inorganic selenium. The highest Se75-concentration in the milk was obtained already within 24 hours after injection. Selenium administered before delivery gave the highest concentration in samples taken less than six hours after delivery. The lambs which received Se75 via the milk had a higher content of Se75 than those who received it during the fetal period.  相似文献   

17.
Disposition kinetics of danofloxacin and ciprofloxacin in broiler chickens.   总被引：3，自引：0，他引：3  
Disposition kinetics of danofloxacin and ciprofloxacin were studied in broiler chickens following intravenous, intramuscular and oral administration in a single dose of 5 and 10 mg/kg-1 body weight respectively. In addition, tissue distribution and residual pattern of both drugs were determined. The maximum serum concentration (Cmax) after intramuscular and oral administration were 1.03 and 0.55 mu/ml for danofloxacin and 2.92 and 1.24 mu/ml for ciprofloxacin attained at 0.8 and 2.43 and 0.55 and 1.27 hours for danofloxacin and ciprofloxacin respectively. The volume of distribution and systemic bioavailability were higher for danofloxacin (Vdss 2.21 L/kg and F% 96.56 and 81.4%) as compared with ciprofloxacin (Vdss 1.41 L/kg and F% 75.5 and 29.4%). Data relating to intravenous injection for both drugs were analyzed using a two compartment open model curve fit. Danofloxacin and ciprofloxacin were not detected in the serum of broilers at the 5th and 3rd day respectively following the drugs withdrawal while were detected in liver, kidneys, spleen and lungs. Danofloxacin completely disappeared from all tissues at the 13th day after stopping of the drug medication but ciprofloxacin disappeared after 5 days only.  相似文献   

18.
The purpose of this study was to establish the pharmacokinetics of enrofloxacin and its metabolite ciprofloxacin in the plasma and interstitial fluid (ISF) following subcutaneous (s.c.) administration of enrofloxacin. Ultrafiltration probes were placed in the s.c. tissue, gluteal musculature, and pleural space of five calves. Each calf received 12.5 mg/kg of enrofloxacin. Plasma and ISF samples were collected for 48 h after drug administration and analyzed by high pressure liquid chromatography. Plasma protein binding of enrofloxacin and ciprofloxacin was measured using a microcentrifugation system. Tissue probes were well tolerated and reliably produced fluid from each site. The mean +/- SD plasma half-life was 6.8 +/- 1.2 and 7.3 +/- 1 h for enrofloxacin and ciprofloxacin, respectively. The combined (ciprofloxacin + enrofloxacin) peak plasma concentration (Cmax) was 1.52 microg/mL, and the combined area under the curve (AUC) was 25.33 microg/mL. The plasma free drug concentrations were 54% and 81% for enrofloxacin and ciprofloxacin, respectively, and free drug concentration in the tissue fluid was higher than in plasma. We concluded that Cmax/MIC and AUC/MIC ratios for free drug concentrations in plasma and ISF would meet suggested ratios for a targeted MIC of 0.06 microg/mL.  相似文献   

19.
Josamycin is a macrolide antibiotic which is produced by fermentation of cultures of Streptomyces narbonensis. It was once administrated (18 mg/kg b. wt.) in fowls via intravenous, oral and intramuscular routes for determination of blood concentration, kinetic behaviour and bioavailability. Following a single intravenous injection, the blood concentration-time-curve indicated a two compartments open model with an elimination half life value (t1/2 beta) of 1.83 +/- 0.06 hours. Both oral and intramuscular routes showed higher values, i.e. 2.33 +/- 0.13 and 2.85 +/- 0.17 hours. The lower apparent volume of distribution of Josamycin in fowls than one liter/kg elucidate higher distribution in blood than in tissues. Systemic bioavailability after both oral and intramuscular administration, i.e. 33.88 +/- 2.4 and 27.28 +/- 1.46% respectively, showed lower absorption from site of i.m. application. Josamycin was administered (18 mg/kg b. wt.) intramuscularly and orally once daily for 5 consecutive days. The drug peaked in serum 1 hour (intramuscular) and 2 hours (orally) after each dose. The recorded results revealed that serum level of Josamycin was higher after oral application (29.98 +/- 1.92 micrograms/ml) than after i.m. application. The drug persisted in the lung tissues and fat for 72 hours after administration and disappeared from all body tissues 96 hours after the last dose of repeated administration.  相似文献   

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