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1.
按 0 .2 m g/ kg单剂量对健康仔猪肌注亚硒酸钠溶液后 ,研究了其在血液中的药物代谢动力学。结果表明 :血液动力学特征符合一级吸收二室开放模型 ,其理论方程为 :C=0 .1773e- 0 .0 548t+0 .0 72 7e- 0 .0 0 2 6 t- 0 .2 5 0 0 e- 1 3.882 3t。主要动力学参数为 :吸收半衰期 (t1 /2 Ka)为 0 .0 4 99h;达峰时间 (tmax)为 0 .4 2 37h;消除半衰期 (t1 /2β)为 2 71.9311h;曲线下面积 (AU C)为 31.72 6 0 m g/ L·h;表观分布容积 (Vd)为 2 .4 72 1L/ kg。根据单剂量药动学参数 ,计算多剂量给药参数 ,为临床治疗制定给药方案。先导剂量 (D* )为 0 .5 0 89m g/ kg,维持剂量 (D0 )为 0 .2 mg/ kg,给药间隔 (τ)为 192 h,平均稳态血药浓度 (c)为 0 .16 5 2 mg/ L。  相似文献   

2.
本实验按 0 .6 mg/ kg BW单剂量对健康仔猪口服亚硒酸钠溶液后 ,首次系统地研究了其在血液中药物代谢动力学。实验结果表明 :血液动力学特征符合一级吸收二室开放模型 ,其理论方程为 :C=0 .0 82 0 e- 0 .0 4 2 1 t 0 .10 5 0 e- 0 .0 0 1 4t- 0 .1870 e- 2 .2 541 t。主要动力学参数为 :吸收半衰期 (t1 / 2 Ka)为 0 .30 75 h;达峰时间 (tmax)为 2 .15 17h;消除半衰期 (t1 / 2β)为 5 10 .2 70 6 h;曲线下面积 (AU C)为 75 .14 6 0 mg/ L· h;表观分布容积 (Vd)为 5 .5 74 2 L/ kg。根据单剂量药动学参数 ,计算多剂量给药参数 ,为临床治疗制订给药方案。先导剂量 (D* )为 1.2 2 6 2 mg/ kg BW,维持剂量(D0 )为 0 .6 m g/ kg BW,给药间隔 (τ)为 4 80 h,平均稳态血药浓度 (с)为 0 .15 6 6 μg/ m l  相似文献   

3.
恩诺沙星在眼斑拟石首鱼体内的药物代谢动力学   总被引：15，自引：0，他引：15  
应用反相高效液相色谱法 (RP- HPL C)研究了恩诺沙星在眼斑拟石首鱼 (Sciaenops ocellatus)体内的药物代谢动力学。实验数据经 DAS药代动力学分析软件分析后得出 :腹腔注射组血浆的药时数据符合一级吸收二室模型 ,动力学方程为 :C =4 .92 5 e- 1 .4 52 t +2 .730 e- 0 .0 75t ,其主要药代动力学参数 :AU C37.5 33mg· L- 1· h、Cmax 4 .74 7mg/ L、Tmax0 .75 0 h、t α0 .4 77h、t β9.2 92 h、Vd/ F 1 .6 76 L / kg、t Ka0 .1 70 h、Ka 4 .0 81 / h、K 6 .71 4 / h、K1 0 0 .1 91 / h、K1 2 0 .76 9/h、K2 1 0 .5 6 6 / h;灌服组血浆的药时数据符合一级吸收一室模型 ,动力学方程为 :C =6 .4 82 (e- 7.0 92 t- e- 1 0 .356 t) ,其主要药代动力学参数 :AU C1 5 .80 5 mg· L- 1 · h、Cmax2 .770 mg/ L、Tmax1 .5 0 0 h、t α4 .989h、Vd/ F2 .0 72 L/ kg、Ka7.0 92 /h、K 1 0 .35 6 / h。结果表明 ,腹腔注射给药比灌服给药吸收快 ,血药浓度达峰时间短于灌服给药 ,但血药浓度峰值明显高于灌服给药 (P<0 .0 5 ) ,血浆中恩诺沙星的回收率为 94 .5 79%。  相似文献   

4.
应用新银盐法研究三氧化二砷在雏鸡体内的药物代谢动力学特征。数据经MCPKP药代动力学软件分析得出:腹腔注射三氧化二砷的药时数据符合一级吸收二室模型,动力学方程为:C=1.62916 e-0.22733t+0.15327 e-0.02024t-1.78243 e-1.36943t,其主要药代动力学参数:AUC0.13459 mg.L-1.h、Cmax 1.08215 mg.L-1、Tpeak 1.64099 h、T1/2Ka0.50605 h、T1/2α3.04841 h、T1/2β34.23920 h、Ka 1.36943 h、K120.09436 h、K210.04101 h、Kel0.11220 h。  相似文献   

5.
酒石酸乙酰异戊酰泰乐菌素在猪体内的药代动力学研究   总被引：2，自引：0，他引：2  
健康猪口服酒石酸乙酰异戊酰泰乐菌素(AIV),不同时间点采血,高效液相色谱法测定血药浓度,残数法拟合药时曲线,计算药动学参数.结果表明,6头猪口服AIV(20mg/kg体重)后,其药动学表现有吸收因素二室模型特征.最佳药时曲线方程为:C=0.654·e-2.0593·t+0.981 3·e-3.0973·t-1.635 3·e-63.3197·t;吸收半衰期(t1/2Ka)为0.014 9±0.012 7 d,消除半衰期(t1/2ke)为0.1138±0.055 5 d,药时曲线下面积(AUC)为0.604 5±0.068 3(μg/mL)·d.表明酒石酸乙酰异戊酰泰乐菌素在猪体内吸收迅速,消除相对较慢.  相似文献   

6.
18头健康杜洛克×长白×大白杂交猪,分3组,每组6头,通过气管内接种含有猪肺炎支原体的病肺悬液复制疾病模型后,以5.0mg/kg静注、肌注及内服给药进行环丙沙星药物动力学研究.高效液相色谱法测定血浆中药物浓度.MCPKP药物动力学程序处理药时数据.结果显示感染猪静注给药的药时数据适合二室开放模型,t1/2α为0.59 h,t1/2β为3.52 h,Vd(area)为3.21 L/kg,ClB为0.645 L/(ks·h).感染猪肌注和内服给药后的药时数据则适合一级吸收一室模型,t1/2ka分别为0.09、0.31 h;tmax分别为0.46、1.41 h;Cmax分别为1.67、0.35 mg/L;F分别为97.30%、34.66%.上述结果表明,支原体性肺炎对环丙沙星静注给药在猪体内的分布有一定影响,但对其消除过程的影响不大;与健康猪比较,感染猪肌注给药的峰浓度、药时曲线下面积及生物利用度均显著提高,而内服给药的峰浓度、药时曲线下面积及生物利用度均显著降低.  相似文献   

7.
复方黄柏颗粒剂在小鼠体内的药代动力学   总被引：1，自引：0，他引：1  
为探讨复方黄柏颗粒剂有效成分-盐酸小檗碱在小鼠体内的药动学特征,按25 g/kg(相当于盐酸小檗碱10.95 mg/kg)的剂量经口给予小鼠复方黄柏颗粒剂,用高效液相色谱法检测用药后不同时间血浆中盐酸小檗碱的质量浓度,研究在小白鼠体内的药物动力学。结果表明口服复方黄柏颗粒的有效成分-盐酸小檗碱在小鼠体内的药时数据符合开放性二室模型,动力学方程为C=17.8e-0.859 81t 14.51e-0.636 1t。主要药代动力学参数:t1/2α为(0.81±0.07)h,t1/2β为(5.25±2.96)h,t1/2Ka为(0.76±0.05)h,AUC0→∞为(3.389 3±0.437 4)mg.L-1.h,CL/F为(3.281 8±0.446 3)L/h,Vd/F为(13.65±22.38)L/kg,Tpeak为(1.617 19±0.056 50)h,Cmax为(1.149 98±0.056 04)μg/mL。  相似文献   

8.
在(14±1)℃水温条件下,对黑鲪单次口灌100 mg/kg体重的磺胺二甲嘧啶,进行药物代谢动力学研究。在(20±2)℃水温条件下,按照《中华人民共和国水产行业标准磺胺类药物水产养殖使用规范》推荐剂量对黑鮶连续5天口灌给予磺胺二甲嘧啶,研究其在黑鮶体内的残留消除规律。血浆、肌肉和肝脏样品采用高效液相色谱检测,DAS2.0药物代谢动力学软件对数据进行处理分析。结果表明磺胺二甲嘧啶在黑鲪血浆、肌肉和肝脏中均符合一室模型,肝脏、血液和肌肉中药物达峰时间分别为6 h,8 h和10 h;峰值浓度分别为26.45μg/g、25.57μg/g和31.15μg/g;连续多次给药后,黑鮶血液、肌肉、肝脏中药物浓度分别在给药后12d、14d、15d后小于最大残留限量要求(0.1mg/kg)。  相似文献   

9.
桔梗的“引经”作用对氟苯尼考药动学的影响   总被引：3，自引：0，他引：3  
20只新西兰白兔随机均分成2组(A、B组),A组单剂量1次灌胃内服氟苯尼考30 mg/kg;B组氟苯尼考30mg/kg与桔梗煎液2 g/kg单荆量1次同时灌胃内服给药;采用高效液相色谱法测定血药浓度,血药浓度最低检测限为0.05 mg/L,以3p97药代动力学程序和SPSSl2.0统计分析软件对所得数据进行分析.结果,药-时数据均符合一级吸收一室开放模型(W=1/C2),主要药代动力学参数及拟合方程如下.A组:T1/2ka(0.461±0.066)h,T1/2kc(2.013±0.195)h,Tpeak(1.180±0.123)h,Cmax(7.332±1.000)mg/L,AUC(31.445±3.566)mg·h-1·L-1,V/F(2.995±0.330)L/kg,拟合方程为:C=19.833(e-0.396t-e-2.387t);B组;T1/2ka(0.550±0.112)h,T1/2ke(3.308±0.270)h,Tpeak(1.414±0.183)h,Cmax(4.737±0.360)mg·L-1,AUC(23.128±2.096)mg·h-1·L-1,V/F(1.400±0.127)L/kg,拟合方程为:C-11.021(e-0.342t-e-10860t).结果表明,桔梗与氟苯尼考同时灌胃内服后,桔梗的"引经"对氟苯尼考在家兔体内药物代谢有较大影响.  相似文献   

10.
氧氟沙星(Ofloxacin)在鲤鱼体内的药代动力学   总被引：3，自引：0，他引：3  
应用 HPL C法测定了单次混饲口服氧氟沙星 (10 mg/ kg)后 ,鲤鱼体内不同时间的血浆药物浓度。利用 MCPKP药代动力学软件分析数据 ,其药代动力学特征符合一级吸收一室开放模型 ,动力学方程为 C=3.2 94 31(e- 0 .0 4 34 1 t-e- 1 .1 1 474 t )。主要药代动力学参数 :吸收半衰期 (T1 /2 ka) 0 .6 2 16 7h,半衰期 (T1 /2 k) 15 .96 4 0 5 h,最高血药浓度 (Cmax)2 .775 89mg/ L ,出现最高血药浓度时间 (TPP,血药浓度时间曲线下面积 (AUC) 72 .934mg/ L· h,血浆治疗浓度维持时间 TCP(ther) 5 .4 4 10 h。结果表明 ,氧氟沙星在鲤鱼体内吸收较迅速 ,达峰时间较短 ,血药峰浓度高 ,消除缓慢 ,保持有效杀菌浓度时间长 ,适用于鱼类细菌性疾病的预防和治疗  相似文献   

11.
Enrofloxacin pharmacokinetics were studied in European cuttlefish, Sepia officinalis, after a single 5 mg/kg i.v. injection or a 2.5 mg/L 5 h bath. A pilot study with two animals was also performed following a 10 mg/kg p.o. administration. The concentration of enrofloxacin in hemolymph was assayed using high-performance liquid chromatography (HPLC) and pharmacokinetic parameters were derived from compartmental methods. In the i.v. study, the terminal half-life (t(1/2)), apparent volume of distribution, and systemic clearance were respectively 1.81 h, 385 mL/kg, and 4.71 mL/min/kg. Following bath administration the t(1/2), peak hemolymph concentration (C(max)), and area under the curve to infinity (AUC(0-infinity)) were 1.01 h, 0.5 +/- 0.12 mug/mL, and 0.98 microg.h/mL, respectively. After oral administration, the t(1/2), C(max), and AUC(0-infinity) were 1.01 h, 10.95 microg/mL, 26.71 mug.h/mL, respectively. The active metabolite of enrofloxacin, ciprofloxacin, was not detected in any samples tested. The hemolymph concentration was still above minimum inhibitory concentration (MIC) values for shrimp and fish bacterial isolates at 6 h after i.v. administration, therefore, a dose of 5 mg/kg i.v. every 8-12 h is suggested for additional studies of efficacy. The C(max) value for the water bath was lower than for the i.v. study, but a bath of 2.5 mg/L for 5 h once to twice daily is suggested for additional studies to test efficacy against highly susceptible organisms. Although only two animals were used for the oral study, a dose of 10 mg/kg produced hemolymph concentrations of enrofloxacin that were in a range consistent with therapeutic efficacy in other species.  相似文献   

12.
The pharmacokinetic properties of ciprofloxacin, a second-generation fluoroquinolone, were investigated in six cats after single intravenous and repeat oral administration at a dosage of 10 mg/kg b.i.d. Ciprofloxacin serum concentration was analyzed by microbiological assay using Klebsiella pneumoniae ATCC 10031 as microorganism test. Serum ciprofloxacin disposition was best fitted to a bicompartmental and a monocompartmental open models with first-order elimination after intravenous and oral dosing respectively. After intravenous administration, distribution was rapid (t(1/2(d)), 0.22 +/- 0.23 h) and wide as reflected by the steady-state volume of distribution of 3.85 +/- 1.34 L/kg. Furthermore, elimination was rapid with a plasma clearance of 0.64 +/- 0.28 L/h.kg and a t(1/2(el)) of 4.53 +/- 0.74 h. After repeat oral administration, absorption was rapid with a half-life of 0.23 +/- 0.22 h and T(max) of 1.30 +/- 0.67 h. However bioavailability was low (33 +/- 12%), the peak plasma concentration at steady-state was 1.26 +/- 0.67 microg/mL. Drug accumulation was not significant after seven oral administrations. When efficacy predictors were estimated ciprofloxacin showed a good profile against gram-negative bacteria when administered either intravenously or orally, although its efficacy against gram-positive microorganisms is lower.  相似文献   

13.
OBJECTIVE: To determine the pharmacokinetics of enrofloxacin administered IV and orally to foals. ANIMALS: 5 clinically normal foals. PROCEDURE: A 2-dose cross-over trial with IV and oral administration was performed. Enrofloxacin was administered once IV (5 mg/kg of body weight) to 1-week-old foals, followed by 1 oral administration (10 mg/kg) after a 7-day washout period. Blood samples were collected for 48 hours after the single dose IV and oral administrations and analyzed for plasma enrofloxacin and ciprofloxacin concentrations by use of high-performance liquid chromatography. RESULTS: For IV administration, mean +/- SD total area under the curve (AUC0-infinity) was 48.54 +/- 10.46 microg x h/ml, clearance was 103.72 +/- 0.06 ml/kg/h, half-life (t1/2beta) was 17.10 +/- 0.09 hours, and apparent volume of distribution was 2.49 +/- 0.43 L/kg. For oral administration, AUC0-infinity was 58.47 +/- 16.37 microg x h/ml, t1/2beta was 18.39 +/- 0.06 hours, maximum concentration (Cmax) was 2.12 +/- 00.51 microg/ml, time to Cmax was 2.20 +/- 2.17 hours, mean absorption time was 2.09 +/- 0.51 hours, and bioavailability was 42 +/- 0.42%. CONCLUSIONS AND CLINICAL RELEVANCE: Compared with adult horses given 5 mg of enrofloxacin/kg IV, foals have higher AUC0-infinity, longer t1/2beta, and lower clearance. Concentration of ciprofloxacin was negligible. Using a target Cmax to minimum inhibitory concentration ratio of 1:8 to 1:10, computer modeling suggests that 2.5 to 10 mg of enrofloxacin/kg administered every 24 hours would be effective in foals, depending on minimum inhibitory concentration of the pathogen.  相似文献   

14.
The pharmacokinetic behaviour of enrofloxacin (ENR) and its active metabolite ciprofloxacin (CIP) were determined in six greater rheas following a single intravenous (i.v.) dose of 15 mg/kg bw. Plasma concentrations of ENR and CIP were simultaneously determined by a HPLC/u.v. method. Following i.v. administration, the plasma drug concentrations were best fitted by an open two-compartment model with a rapid distribution phase. The high volume of distribution (V(ss)=5.01 L/Kg) suggests good tissue penetration. ENR presents a high clearance (3.95 L/kg h) explaining the low AUC values (3.57 mg h/L) and a short permanence (t(1/2beta)=2.66 h and MRT=1.23 h). Ciprofloxacin comprised 14% of the total fluoroquinolone (ENR+CIP).  相似文献   

15.
Plasma, urine, and skin drug concentrations were determined for dogs (n=12) given five daily oral doses of marbofloxacin (MAR) (2.75 mg/kg), enrofloxacin (ENR) (5.0 mg/kg) or difloxacin (DIF) (5.0 mg/kg). Concentrations of the active metabolite of ENR, ciprofloxacin (CIP), were also determined. The three-period, three-treatment crossover experimental design included a 21-day washout period between treatments. Area under the plasma drug concentration vs. time curve (AUC0-last, microg/mLxh of MAR was greater than for ENR, CIP, ENR/CIP combined, and DIF. Maximum concentration (Cmax) of MAR was greater than ENR, CIP, and DIF. Time of maximum plasma concentration (Tmax) was similar for MAR and DIF; Tmax occurred earlier for ENR and later for CIP. Plasma half-life (t1/2) of MAR was longer than for ENR, CIP, and DIF. Urine concentrations of DIF were less than MAR or ENR/CIP combined, but urine concentrations of MAR and ENR/CIP combined did not differ. DIF skin concentrations were less than the concentrations of MAR or ENR/CIP combined 2 h after dosing, but skin concentrations of MAR and ENR/CIP combined did not differ.  相似文献   

16.
The comparative pharmacokinetics of enrofloxacin (ENR) and its metabolite ciprofloxacin (CIP) were investigated in healthy and Aeromonas hydrophila‐infected crucian carp after a single oral (p.o.) administration at a dose of 10 mg/kg at 25 °C. The plasma concentrations of ENR and of CIP were determined by HPLC. Pharmacokinetic parameters were calculated based on mean ENR concentrations by noncompartmental modeling. In healthy fish, the elimination half‐life (T1/2λz), maximum plasma concentration (Cmax), time to peak (Tmax), and area under the concentration–time curve (AUC) values were 64.66 h, 3.55 μg/mL, 0.5 h, and 163.04 μg·h/mL, respectively. In infected carp, by contrast, the corresponding values were 73.70 h, 2.66 μg/mL, 0.75 h, and 137.43 μg·h/mL, and the absorption and elimination of ENR were slower following oral administration. Very low levels of CIP were detected, which indicates a low extent of deethylation of ENR in crucian carp.  相似文献   

17.
实验研究了30日龄肉鸡单次肌注(0.6mg/Kg)亚硒酸钠注射液后不同时间采血,用流动注射氢化物发生原子吸收光谱法测定血硒浓度,经微机处理得出血硒浓度及药动学参数,血硒浓度-时间曲线符合一级吸收一室开放模型,最佳药时方程:C=100.2001(e-0.0197t-e-1.6428t)。主要药动学参数:t1/2Ka为0.421 9h,t1/2Ke为35.121 5h,tp为3.312 4h,Cmax为93.986 5μg/L,AUC为5 025.314 9(μg/L).h。根据单剂量给药参数,计算出多剂量给药参数。  相似文献   

18.
以血清一氧化氮（NO）变化为药理效应指标,用药理效应法研究了中药复方制剂禽病康在免疫抑制雏鸡体内的药代动力学特征,并探讨了其扶正固本、增强机体免疫功能的作用机制。结果表明,免疫抑制雏鸡单剂量口服禽病康的效应动力学参数为：最低起效剂量Xmin=2.61 g/kg,效应呈现半衰期t1/2ka（E）=0.61 h,效应达峰时间tp（E）=1.82 h,效应消除半衰期t1/2b（E）=3.25 h;以时间-体存量进行数学模型拟合,符合一级吸收二室模型,其数学表达式为C=24.221e-0.931t＋3.485e-0.012t＋27.705e-1.166t。禽病康药代动力学结果表明其口服后吸收较快,分布也快,而消除较慢,体内存留时间长,药效维持时间长。  相似文献   

19.
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   

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