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71.
环丙沙星在鲤体内吸收、代谢和生物利用度   总被引:6,自引:1,他引:6       下载免费PDF全文
杨雨辉 《水产学报》2003,27(6):582-589
为评价环丙沙星在水生动物疾病防治上的应用,按10mg·kg~(-1)的剂量分别给鲤静注乳酸环丙沙星水溶液、口服乳酸环丙沙星水溶液、口服乳酸环丙沙星饲料糊。用高效液相色谱测定血浆中药物浓度,用MCPKP药代动力学程序处理药时数据,口服乳酸环丙沙星水溶液和口服乳酸环丙沙星饲料糊的生物利用度分别为10.25%和6.22%。静注给药的药时数据符合无吸收三室开放模型,主要药物代谢动力学的参数如下:t_(1/2α)=0.16h、t_(1/2)π=0.86h、t_(1/2β)=16.47h、V_1=0.10 L·kg~(-1)、Vb=3.03 L·kg~(-1)、Cl_B=0.12 L·kg~(-1)·h~(-1),环丙沙星在鲤体内分布广泛,排泄较慢;口服乳酸环丙沙星水溶液、口服乳酸环丙沙星饲料糊的药时数据均符合具有一个滞后时间的一级吸收二室开放模型;口服乳酸环丙沙星水溶液的主要药物代谢动力学的参数为:t_(1/2α)=0.31h、t_(1/2β)=6.47h、C_(max)=2.14μg·mL~(-1)、T_(max)=0.44h;口服乳酸环丙沙星饲料糊的主要药物代谢动力学的参数为:t_(1/2α)=0.53h、t_(1/2β)=14.47h、C_(max)=0.70μg·mL~(-1)、T_(max)=1.10h,说明鲤口服乳酸环丙沙星水溶液后吸收该药的速度比口服乳酸环丙沙星饲料糊快。从该药的生物利用度结果看,由于环丙沙星在鲤体内的吸收利用程度较低,所以应用该药治疗鲤  相似文献   
72.
The present study was designed to explore pharmacokinetics of enrofloxacin and its metabolite ciprofloxacin in healthy and Vibrio alginolyticus-infected large yellow croaker (Pseudosciaena crocea) after a single 10 mg/kg oral dose. Concentrations of enrofloxacin and ciprofloxacin in serum, liver, kidney, muscle and skin of fish were determined using high-performance liquid chromatography. Pharmacokinetic parameters were analysed based on classical compartmental model analysis. The overall changes in enrofloxacin concentration–time curves in serum and tissues of diseased fish were similar to those of healthy fish. However, the peak concentration and peak time of enrofloxacin in serum and tissues were different in healthy and diseased fish. A delay of enrofloxacin peak time in serum and all tissues appeared in the diseased fish. The peak concentrations in serum and tissues of the diseased fish were lower than those of healthy fish. In healthy fish, the area under the concentration–time curve (AUC) was in the order serum >liver > kidney >muscle > skin, while AUC was serum >live > muscle >kidney > skin in the diseased fish. The peak concentrations of ciprofloxacin in the liver, serum, kidney, muscle and skin of healthy fish were 0.93 μg/g, 0.55 μg/ml, 0.36 μg/g, 0.37 μg/g and 0.12 μg/g respectively. Tmax of ciprofloxacin in the corresponding tissues was 8, 24, 12, 12 and 16 h respectively. In the diseased fish, the peak concentrations of ciprofloxacin in the corresponding tissues were 0.52 μg/g, 0.52 μg/ml, 0.41 μg/g, 0.27 μg/g and 0.13 μg/g respectively. Tmax in the corresponding tissues were 0.5, 8, 12, 16 and 48 h respectively. These data indicate that the health status of fish affects drug absorption and metabolism.  相似文献   
73.
鸡血浆中环丙沙星的RP-HPLC法研究   总被引:2,自引:0,他引:2  
采用反相高效液相色谱(RP-HPLC)法,以氧氟沙星为内标物,测定鸡血浆中环丙沙星的含量。结果表明:环丙沙星回收率为88.20%~95.41%,日内、日间相对标准差分别为3.22%~7.04%、5.05%~9.00%(n=5),环丙沙星在0.05~7.50mg·L-1范围内呈显著线性相关(r为0.9993,n=9),最低检测限为0.015mg·L-1,可满足环丙沙星在肉仔鸡体内的药动学样品检测的要求。  相似文献   
74.
75.
Intorre, L., Mengozzi, G., Bertini, S., Bagliacca, M., Luchetti, E. and Soldani, G., 1997. The plasma kinetics and tissue distribution of enrofloxacin and its metabolite ciprofloxacin in the Muscovy duck. Veterinary Research Communications, 21 (2), 127-136The disposition and tissue distribution of enrofloxacin and of its main metabolite ciprofloxacin were investigated in ducks after oral or intramuscular administration of a single dose of 10 mg/kg enrofloxacin. Plasma and tissue concentrations were determined by a HPLC method. The peak concentrations of enrofloxacin after intramuscular administration (1.67 µg/ml at 0.9 h) were higher than after an oral dose (0.99 µg/ml at 1.38 h). The relative bioavailability of enrofloxacin after administration directly into the crop was 68%, while the metabolic conversion of enrofloxacin to ciprofloxacin was quite low (<10%) with both routes of administration. High tissue concentrations and high tissue:plasma concentration ratios were demonstrated for enrofloxacin and ciprofloxacin 24 h after treatment. It was concluded that a dose of 10 mg/kg per day provides serum and tissue concentrations sufficiently high to be effective in the control of many infectious diseases of ducks.  相似文献   
76.
环丙沙星(ciprofloxacin)在鸡蛋中残留的研究   总被引:2,自引:0,他引:2  
应用高效液相色谱法(HPLC)检测了鸡蛋中环丙沙星的残留。鸡蛋经乙腈溶液提取,提取液真空干燥后用流动相溶解。以0.015mol/L四丁基溴化铵/乙腈(94/6,V/V)作流动相,用SymmetryC18柱(5μm,3.9mm×150mm),在激发波长280nm、发射波长455nm处,用荧光检测器检测。将环丙沙星以0.05、0.50、1.00mg/kg分别添加到空白鸡蛋样品中,测得鸡蛋样品中环丙沙星的回收率分别为(82.2±6.8)%、(84.5±5.9)%、(87.9±4.7)%,相对标准差均低于8.3%。用该方法测定鸡蛋中环丙沙星的最低检测限为0.01mg/kg。各试验组产蛋鸡给药剂量分别按10.0、20.0mg/kg(体质量)内服环丙沙星水溶液,每天给药1次,连续5d。停药后鸡蛋中环丙沙星残留消除缓慢;休药8~9d时,鸡蛋中环丙沙星残留量低于0.03mg/kg;休药9~10d时,鸡蛋中环丙沙星残留量均低于最低检测限(0.01mg/kg);且随着环丙沙星给药剂量的增大,环丙沙星在鸡蛋中的残留量也相应增大。  相似文献   
77.
复方氨苄西林可溶性粉为氨苄西林与盐酸环丙沙星组成的复方制剂.为了验证临床疗效,以人工诱发鸡大肠杆菌病为模型,采用高、中、低三个治疗剂量与相应的氨苄西林和盐酸环丙沙星三个剂量的单方制剂进行了比较,结果:复方氨苄西林可溶性粉治疗组与阳性对照组比较差异极显著(P<0.01);复方氨苄西林高、中、低三个剂量组与氨苄西林高、中、低三个剂量组比较差异显著(P<0.05),与盐酸环丙沙星三个剂量组比较,死亡率均低于相同剂量的盐酸环丙沙星对照组,但差异不显著(P>0.05).在增重效果上,复方氨苄西林治疗组平均增重高于阳性对照组,其中高、中剂量组明显高于氨苄西林和盐酸环丙沙星对照组.结果表明:复方氨苄西林可溶性粉对鸡大肠杆菌病的疗效好于氨苄西林和盐酸环丙沙星的单方制剂,两药配伍有一定的增效作用.  相似文献   
78.
The pharmacokinetics of enrofloxacin (ENR) was studied in crucian carp (Carassius auratus gibelio) after single administration by intramuscular (IM) injection and oral gavage (PO) at a dose of 10 mg/kg body weight and by 5 mg/L bath for 5 hr at 25°C. The plasma concentrations of ENR and ciprofloxacin (CIP) were determined by HPLC. Pharmacokinetic parameters were calculated based on mean ENR or CIP concentrations using WinNonlin 6.1 software. After IM, PO and bath administration, the maximum plasma concentration (Cmax) of 2.29, 3.24 and 0.36 μg/ml was obtained at 4.08, 0.68 and 0 hr, respectively; the elimination half‐life (T1/2β) was 80.95, 62.17 and 61.15 hr, respectively; the area under the concentration–time curve (AUC) values were 223.46, 162.72 and 14.91 μg hr/ml, respectively. CIP, an active metabolite of enrofloxacin, was detected and measured after all methods of drug administration except bath. It is possible and practical to obtain therapeutic blood concentrations of enrofloxacin in the crucian carp using IM, PO and bath immersion administration.  相似文献   
79.
Antimicrobial susceptibility was determined for 805 domestic Campylobacter jejuni isolates obtained from broilers (= 459), bovines (= 120), human patients (= 95), natural waters (= 80), wild birds (= 35) and zoo animals/enclosures (= 16) with known multilocus sequence types (MLST) for 450 isolates. The minimum inhibitory concentration (MIC) values for erythromycin, tetracycline, streptomycin, gentamicin and the quinolones ciprofloxacin and nalidixic acid were determined with the VetMIC method. MICs were compared with MLST types to find possible associations between sequence type and resistance. The proportions of resistant isolates were 5% (broilers), 6.3% (natural waters), 11.4% (wild birds), 11.6% (human patients), 16.7% (bovines) and 31.3% (zoo). The most common resistance among the human and bovine isolates was quinolone resistance alone while resistance to streptomycin alone was most often detected among the broiler isolates and tetracycline resistance was most commonly observed in the wild bird, water and zoo isolates. No or negligible resistance to erythromycin or gentamicin was detected. In all data, 12/26 of the tetracycline‐resistant isolates were also resistant to streptomycin (< 0.001) and the clonal complex (CC) ST‐1034 CC showed a high proportion of 75% (9/12) of tetracycline‐resistant isolates, most originating from the zoo and broilers with closely associated MLST types from these sources. No association between quinolone resistance and MLST type was seen. The low percentage of resistant isolates among the domestic Campylobacter infections is most probably due to the long‐term controlled use of antimicrobials. However, the higher percentage of tetracycline resistance observed among the zoo isolates could present a risk for zoo visitors of acquisition of resistant C. jejuni. The resistance pattern of tetracycline and streptomycin most often found in ST‐1034 CC could indicate a common resistance acquisition mechanism commonly present in this CC. Overall, MLST typing was found to be a useful method in recognition of potential genetic lineages associated with resistance.  相似文献   
80.
为查明环丙沙星高、低累积菜心根际消除环丙沙星(CIP)高低差异的微生物学机理,通过室内土壤盆栽实验,研究了这两种菜心根际土壤中酶活性和微生物学特征差异。结果表明:种植高、低累积菜心均促进土壤CIP的消除,在高污染水平时,高累积菜心对土壤CIP的消除效果显著高于低累积菜心,其降解率分别为48.7%和39.4%(P0.05);高累积菜心根际土壤的可培养细菌数量和细菌群落结构多样性与丰富度(尤其含CIP特异降解菌Beta proteobacteria的相对丰度),以及过氧化氢酶和脲酶活性均显著高于低累积菜心。研究结果初步揭示了高累积菜心根际去除CIP能力更强且体内吸收累积CIP更多这一初步机理。  相似文献   
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