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1.
在水温(25±2)℃条件下,以15 mg/kg鱼体重的剂量给奥尼罗非鱼单次口灌盐酸土霉素,采用高效液相色谱法测定血浆和肌肉组织中的药物浓度,研究盐酸土霉素在奥尼罗非鱼体内的代谢及消除规律。结果显示:血药时间数据符合一级吸收二室开放模型,半衰期(T1/2Ka、T1/2α、T1/2β)分别为4.79、4.10、45.20 h,最大血药浓度为1.50μg/m L,达峰时间为7.30 h,药时曲线下面积(AUC)为42.35μg·h/m L。肌肉作为可食性组织,选取肌肉组织作为残留检测的靶组织,以0.1 mg/kg为最高残留限量,在本试验条件下,建议休药期不低于10 d。 相似文献
2.
Abstract. Oxytetracycline (OTC) was intraperitoneally injected into pike, Esox lucius L., to determine the validity of ages derived from cleithra and pelvic fin rays, to determine the rate of OTC incorporation into calcified structures, to decermine suitable marking dosages and to assess OTC-induced mortality.
The results showed that annuli were laid down on pike cleithra and pelvic fin rays. OTC was incorporated into most calcified structures as early as 6 h after injection and all structures were marked within 24 h. A dosage range of 25–50 mg OTC/kg fish was appropriate for marking pike. OTC-induced mortality was statistically insignificant. 相似文献
The results showed that annuli were laid down on pike cleithra and pelvic fin rays. OTC was incorporated into most calcified structures as early as 6 h after injection and all structures were marked within 24 h. A dosage range of 25–50 mg OTC/kg fish was appropriate for marking pike. OTC-induced mortality was statistically insignificant. 相似文献
3.
The present study examined the pharmacokinetics and bioavailability of oxytetracycline (OTC) in vannamei shrimp (Penaeus vannamei) after intra-sinus (10 mg/kg) and oral (10 and 50 mg/kg) administration and also investigated the net changes of OTC residues in the shrimp after the thermal, acid and alkaline processing methods. The hemolymph concentrations of OTC after intra-sinus dosing were best described by a two-compartment open model. The oral bioavailability was found to be 48.2 and 43.6% at doses of 10 and 50 mg OTC/kg, respectively. The peak hemolymph concentrations after 10 and 50 mg OTC/kg doses were 3.37 and 17.4 μg/ml; the times to peak hemolymph concentrations were 7 and 10 h. The elimination half-lives were found to be 15.0 and 11.5 h for the low and high dose, respectively. The residual OTC was rapidly eliminated from muscle with the elimination half-life value of 19.4 and 15.4 h, respectively, for the groups treated with doses of 10 and 50 mg/kg. The residual OTC levels in the muscle fell below the MRL (0.2 μg/g) at 72 and 96-h post-dosing at dose levels of 10 or 50 mg/kg, respectively. Residual OTC levels in muscle and shell were approximately 20–50% lower in the thermal treatment such as boiling, baking and frying. By the acid treatment, OTC residues were reduced to >80%, while those were reduced to around 30% by alkaline treatment. 相似文献
4.
Pharmacokinetics and tissue distribution of oxytetracycline in carp, Cyprinus carpio L., following different routes of administration 总被引：4，自引：0，他引：4
J. L. GRONDEL J.F.M. NOUWS M. DE JONG A. R. SCHUTTE F. DRIESSENS 《Journal of fish diseases》1987,10(3):153-163
Abstract. The objective of this pharmacokinetic study was to investigate absorption, distribution, elimination and bioavailability of oxytetracycline (OTC) in carp, Cyprinus carpio L ., after different routes of administration, OTC was administered intravenously (i.v.), intramuscularly (i.m.) and orally at 60 mg/kg body weight. OTC levels were determined in plasma and several tissues. Analysis of the plasma drug concentration-time curves following i.v. OTC injection revealed three distinct phases. A three-compartment open model was used to derive pharmacokinetic parameters. Compared to mammals, a very extended final elimination half-life was observed (139.8±38.1 h). Following i.m. OTC administration, Cmax was 56.8±10.9μg OTC/ml at 14 h post-injection. The Vd area was 2.1 ± 0.66 1/kg. Extreme differences were observed with respect to bioavailability following i.m. and oral administration; approximately 80 and 0.6%, respectively. Following i.m. injection tissue OTC determinations revealed that the drug was accumulating in pronephros, bone tissue and scales. After 21 days the OTC concentrations were 2.9±0.8, 5.2±0.3 and 4.7±3.1 μg/ ml, respectively. In tissue samples from the dorsal region (muscle), including the injection site, OTC could not be demonstrated at that time. The pharmacokinetic data are discussed in relation to the susceptibility of the immune system of fish for modulation. 相似文献
5.
土霉素在锯缘青蟹体内的药物代谢和消除规律 总被引：1，自引：0，他引：1
采用高效液相色谱法检测土霉素,研究土霉素口灌给药途径下在锯缘青蟹体内的药代动力学。锯缘青蟹口灌给药土霉素50 mg/kg后,其血浆、肌肉和肝胰脏中的药峰浓度分别为16.78±1.98 mg/L、9.39±2.12μg/g和32.12±6.12μg/g,达峰时间分别为4 h、8 h和4 h。血浆中土霉素浓度-时间关系曲线符合一级吸收的二室开放动力学模型。土霉素在锯缘青蟹体内分布广泛,其表观分布容积(Vd)为2.129 L/kg;分布半衰期(t1/2α)和消除半衰期(t1/2β)分别为3.200 h和47.856 h,总体清除率(CLs)为0.063 mL/(kg.h)。肌肉和肝胰脏中土霉素浓度与时间关系的药动学参数采用统计矩原理分析,其消除半衰期(t1/2 z)分别为60.145 h和71.009 h,总体清除率(CLz)分别为0.054 g/(kg.h)和0.037 g/(kg.h)。土霉素在精巢和卵巢中达峰时间分别为8 h和12 h,峰浓度分别为9.83μg/g和10.26μg/g。给药后24 d时,血浆、肌肉、肝胰脏、精巢和卵巢中土霉素含量都已低于0.10μg/g。土霉素在锯缘青蟹体内消除比较缓慢。 相似文献
6.
(21±1)℃水温条件下,研究了三聚氰胺在斑点叉尾鮰(Ictalurus punctatus)体内的残留消除规律。结果显示:血浆中药时数据符合有吸收一室开放模型,动力学方程为:C=3.952660(e-0.027279t-e-0.127279t),吸收半衰期(T1/2kα)为5.4469 h,消除半衰期(T1/2ke)为25.4093 h,达峰时间(Tp)为15.4045 h,达峰浓度(Cmax)为20.3985 mg/L,表观分布容积(Vd)为2.5763(mg/kg)/(mg/L)。肌肉、肝、肾中吸收半衰期(T1/2kα)分别为3.5582、4.1884、5.4397 h,消除半衰期(T1/2ke)为50.8081、23.3504、23.7242 h,达峰时间(Tp)为14.6766、12.6524、14.9967 h,达峰浓度(Cmax)为7.6449、22.9249、40.6047 mg/L,表观分布容积(Vd)为8.5657、2.3970、1.2712(mg/kg)/(mg/L)。结果表明:药物在体内吸收迅速,药物浓度较高,分布广泛,消除较为缓慢。以80 mg/kg剂量混饲口灌3 d后,各组织中三聚氰胺含量总体呈现肾脏>肝脏>肌肉。停止灌药后第5天肌肉中及第7天肝脏和肾脏组织中三聚氰胺含量低于我国(2008)卫生部公布的乳制品及含乳食品中三聚氰胺临时管理限量值和欧盟对中国进口产品设定了三聚氰胺的最大残留限2.5 mg/kg。 相似文献
7.
在14±2℃水温条件下,连续5d对红鳍东方鲍口灌剂量为100mg／kg的土霉素,采用高效液相色谱法测定了停药后血清、肌肉、肝脏组织中的药物含量、消除速率常数和消除半衰期,提出了该温度下的休药期。研究表明,在停药2d后红鳍东方鲍血清和肌肉中的药物浓度达到峰值,分别为1．092μg／ml和0．806μg／g;停药3d后肝脏内土霉素浓度达到峰值1．229μg／g,土霉素在血清、肌肉和肝脏中的消除半衰期分别为23．8、22．4和26．8d;土霉素在红鳍东方纯肌肉组织中降到0．1μg／g残留限量的时间为58d,降到0．05μg／g残留限量的时间为81d。 相似文献
8.
Abstract. The present study was performed to obtain further details on the immuno-modulating effects of oxytetracycline (OTC) in carp, Cyprinus carpio L. The immuno-logical study was extended by investigating the pharmacokinetic behaviour of OTC. Oxytetracycline, at a dosage of 60 mg/kg, was administered five times intra-peritoneally at 3-day intervals; the first injection was given 1 day before immunization. The kinetics of the primary anti-sheep red blood cell (SRBC) response, during a short-term OTC treatment revealed that the kinetics of the plaque-forming cell (PFC) response was not significantly affected by OTC nor its solvent. In contrast, the number of plaque-forming cells was significantly decreased. The anti-SRBC antibody production was delayed by 2–4 days in both experimental groups (OTC and solvent). However, within 12–14 days post-immunization, the same antibody levels were detected as in the control group. High OTC plasma levels (>50 μg/ml) were detected about 10 h after a single i. p. injection. A mean plasma elimination half-life (T1 /2 ) of 34·5 h was calculated. 相似文献
9.
10.
土霉素在黑鲷体内的药物代谢动力学研究 总被引：10，自引：0，他引：10
首次报道了黑鲷口服土霉素的药物代谢动力学特征，用高效液相色谱法测定组织中的药物含量，药物在肌肉，血液，肝脏中的平均回归率分别为８５.61%,85.38%,82.005,该方法的检测限可达0.01μg/g，黑鲷１次口服剂量为７５mg/kg的土壤素后，其血液药物浓度－时间数据符合一室开放动力学模型，吸收速率常数（ka)为０.296/h，达峰时间（Ｔamx)为１０.635h,峰浓度（Ｃmax)为１.398μg/ml, 分布半衰期（Ｔ１／２a）为２.339h ,消除半衰期(T1/20β）为46.663h，药时曲线下面积（ＡＵＣ）为１１0.25mg/L.h，黑绸口服药物０.5h后在血液，肥肉，肝脏，肾脏４种组织中就可以检测到药物的存在，药物在１６h的采样点浓度达最高，分别为1.68μg/ml,1.68,2.52,6.77μg/g。 相似文献
11.
George Rigos Maria Alexis Argyro Andriopoulou Ioannis Nengas 《Aquaculture (Amsterdam, Netherlands)》2002,210(1-4):59-67
A pharmacokinetic study of oxytetracycline (OTC) following an intravascular administration (40 mg/kg) was carried out in sea bass, Dicentrarchus labrax (110 g), at 13.5 and 22 °C water temperature. Blood, muscle and liver samples were taken at 1, 2, 4, 8, 16, 32, 64 and 128 h post-injection. The plasma data were conformed to a two-compartment model. The kinetic profile of the drug was found to be temperature dependent. The absorption half-life (t1/2) of OTC was 0.98 and 0.192 h at 13.5 and 22 °C, respectively, whereas the elimination half-time (t1/2β) of the drug was 69 h at 13.5 °C and 9.65 h at 22 °C. The apparent volume of distribution of the drug at steady state [Vd(ss)] was 5.62 l/kg at 13.5 °C and 2.59 l/kg at 22 °C. The mean residence time (MRT) of OTC was found to be 37.7 h at 22 °C and 71 h at 13.5 °C. The total clearance of the drug (CLT) was calculated to be 73.5 and 68.7 ml/kg/h at 13.5 and 22 °C, respectively.
Liver levels indicated higher OTC values than respective muscle levels at all time points and for both temperatures. The elimination of OTC from tissues tested was faster at the high temperature, whereas the drug was eliminated faster from liver compared to muscle when comparisons are made at the same temperature. 相似文献
12.
Chloramphenicol (CAP) is a banned substance in fish farming; yet, residues are sometimes detected in farmed fish products. Therefore, it is important that tissue distribution and elimination rates of CAP are measured to allow monitoring of fish farms. The tissue distribution and residue of CAP in carp (Cyprinus carpio L.) after muscle injection was investigated. Chloramphenicol concentrations were determined using high‐performance liquid chromatography. Pharmacokinetics were used for the studies of CAP residue and the results showed that the CAP was easily assimilated in the liver, serum and gill, with the absorption rates of 6383, 3.02 and 1.39 h?1, respectively, following a single‐dose injection of 80 mg kg bw?1. The elimination half‐lives (t1/2) were 22.28, 15.47, 14.87, 9.28 and 5.32 h for the liver, serum, gill, muscle and kidney respectively. The t1/2 after 5 days of multi‐doses of repeated CAP injection with 40 mg kg bw?1 was 1.09, 0.887, 0.872, 0.476 and 0.617 days for the five tissues respectively. The results validated that CAP in the liver, serum and gill could be markers for CAP residue analysis. 相似文献
13.
Although tricaine methanesulfonate (MS-222) is often used to tranquilize fish, the guidelines for its use in sea bass, a brackish species, have not been established. The aim of the study reported here was to establish the tranquilizing concentration of MS-222, based on the time required for MS-222 residue elimination and withdrawal. Thirty-six fish (6/group) were immersed in different concentrations of MS-222 (0, 30, 50, 60, 70 and 90 mg/l) to evaluate the fish physiological behavior. After 200 fish were anesthetized at 90 mg/l, the fish achieved a healthy recovery within 72 h after the administration of saline. The 10 fish in the control group were subject to the same treatment without anesthesia, 3 out of 10 died. After 108 fish (54/group) were immersed in 30 or 60 mg/l of MS-222, the sedated fish were healthy during and after the 8 h of transport. However, all the 10 fish in the control group died within 3 days. By high-performance liquid chromatography, the residue of MS-222 was assessed. In the skinned muscle and liver, the elimination half-life was 5.54 and 5.27 h (30 mg/l) and 8.72 and 7.15 (60 mg/l), respectively, and the withdrawal time was at least 4.5 days at 30 mg/l and 7.5 days at 60 mg/l. 相似文献
14.
《Aquaculture (Amsterdam, Netherlands)》1996,143(1):33-42
The pharmacokinetics and bioavailability of oxytetracycline (OTC) were examined in healthy and vibriosis-infected ayu (Plecoglossus altivelis). Water temperature was maintained at 18.0 ± 0.3 °C in all experiments. Serum concentrations of OTC in healthy fish after intravascular administration (25 mg kg−1 body weight) were best described by a two-compartment model, whereas serum concentration-time curves after oral administration (100 mg kg−1 body weight) in healthy and infected ayu could not be fitted by the nonlinear least squares method using one- and two-compartment models with first-order absorption. The estimated bioavailability after oral administration was 9.3% for healthy fish and 3.8% for infected fish. The elimination half-lives of serum, muscle, liver and kidney were 53.1 h, 106 h, 125 h and 117 h for healthy fish, and 63.2 h, 92.9 h, 107 h and 123 h for infected fish, respectively. A significant difference in bioavailability was revealed between healthy fish and infected fish, whereas elimination was similar in both fish. Serum protein binding in vivo of OTC was 68.0 ± 2.8% for healthy fish and 69.9 ± 4.4% for infected fish. 相似文献
15.
在水温(22±2)℃条件下,将平均体质量约为100 g的健康草鱼、花鲈、鲫鱼在50 mg/L的间氨基苯甲酸乙酯甲磺酸盐(MS-222)药液中浸泡,分别于药浴0.5、1、2、3、7 h和10 h时取样测定肌肉、肝(胰)脏、血液中MS-222的残留量,10 h后将试验鱼置于清洁水中,分别于0.5、1、2、4、6、8、16、32、96、120、192、264、336、432、528、624、720 h时再测定肌肉、肝(胰)脏、血液中MS-222的残留量。结果显示,MS-222在草鱼、花鲈、鲫鱼的血液、肌肉、肝(胰)脏中残留分别在3、3、7 h达到峰值,随后略下降;MS-222在草鱼血液、肌肉、肝胰脏组织中的消除半衰期分别为5.4、6.7、7.9 h;在花鲈血液、肌肉、肝脏组织中的消除半衰期分别为3.9、5.1、5.7 h;在鲫鱼血液、肌肉、肝胰脏组织中的消除半衰期分别为 4.8 、6.3、8.4 h。MS-222在3种鱼类肝(胰)脏、肌肉、血液中的消除速率均为 V肝(胰)脏相似文献
16.
Pharmacokinetics and bioavailability of flumequine and oxolinic acid after various routes of administration to Atlantic salmon in seawater 总被引：2，自引：0，他引：2
Astri Rogstad Odd F. Ellingsen Christian Syvertsen 《Aquaculture (Amsterdam, Netherlands)》1993,110(3-4):207-220
The present preclinical study was performed to investigate the pharmacokinetics of flumequine in Atlantic salmon (Salmo salar L.) in seawater after administration of different doses and dosage formulations. Flumequine was administered intravenously (dose 4.9 mg/kg fish) and orally from the drug delivery system Aqualets as Apoquin 5 g/kg (dose 25 mg/kg) and 10 g/kg (dose 50 mg/kg), respectively. Experiments were carried out with oxolinic acid administered in the same way for the purpose of comparing the two compounds. The seawater temperature was 5±0.2°C in all experiments.
The pharmacokinetic calculations showed that the distribution half-life for flumequine was and for oxolinic acid . The drugs were absorbed rapidly, and flumequine reached a plasma concentration of Cmax = 2.26 μg/ml after a single oral dose of 25 mg/kg, whereas oxolinic acid reached Cmax = 0.99 μg/ml. The apparent bioavailability of flumequine was found to be 40–45%, whereas the apparent bioavailability of oxolinic acid varied from 25% at a dose of 50 mg to 40% at a dose of 25 mg/kg body weight of fish. The distribution profile of flumequine in the various compartment of fish appeared to be different from that of oxolinic acid. After a single oral dose (25 mg/kg) the areas under the concentration-time curves showed that flumequine was 2.3 times more concentrated in plasma and 2.6 times more concentrated in liver compared to oxolinic acid. In muscle the difference was less pronounced, flumequine being 1.4 times more concentrated than oxolinic acid. 相似文献
17.
Tissue depletion studies of antibacterials are an important part of data packages required to obtain a label from the U.S. Food and Drug Administration (FDA) in the United States for use of therapeutants in food fishes. Currently, withdrawal tima are set based on results of such studies obtained from healthy animals. Bacterial infection can lead to dramatic physiological changes in affected fish. In this investigation, the impact of bacterial infection on depletion kinetics of oxytetracycline (OTC) was examined in tilapia Oreochromis niloticus challenged with Streptococcus iniae (a model Gram positive bacterium) or Vibrio vulnificus (a model Gram negative bacterium). An additional group of fish injected with Brain Heart Infusion (BHI) broth was included as a non-infectious stimulus. Although some differences in elimination kinetics of OTC were observed between treated fish and non-treated controls, OTC was rapidly eliminated from tilapia in all groups. In all cases, mean concentration of OTC was below the current 2.0 ppm (μg/g) FDA tolerance for OTC in the edible portion (muscle plus skin) after day 3 postdosing. 相似文献
18.
The uptake and elimination profile of oxytetracycline (OTC) following a prolong bath treatment in gilthhead sea bream (Sparus aurata) were investigated in this study. The bath experiment was carried out using a OTC concentration of 50 μg/ml for 24 h at 17-18 °C water temperature. Plasma and muscle fish samples were analysed at 1, 3, 6 and 24 h during and at 1, 2, 3, 4 and 6 d following the bath. Detectable OTC levels were revealed only at the end of bath treatment (24 h) in examined tissues of gilthead sea bream, where drug concentration was measured to be as low as 0.096 and 0.047 μg/g or ml in muscle plus skin and plasma, respectively. The findings of the present study indicate that OTC bath treatment under this dosage schedule is unlikely to confront systemic bacterial infections. 相似文献
19.
以80 mg/kg鱼体重对牙鲆单次口灌给药恩诺沙星,给药后在不同的时间点取样,用高效液相色谱荧光检测器检测,研究恩诺沙星及其主要代谢产物环丙沙星在牙鲆体内的代谢消除规律。研究表明,停药后0.25 h,肌肉中恩诺沙星残留量最低。各组织的消除半衰期依次为腮肝脏血液肾脏肌肉,其中肌肉中恩诺沙星消除半衰期最低为67.759 h,消除最快,停药后12 d检测不到恩诺沙星。停药后0.25 h,在牙鲆血液、肝脏、肾脏中均有环丙沙星残留,残留量依次为肝脏肾脏血液,肌肉和鳃中未检出环丙沙星。停药后22 d在血液、肝脏和肾脏3个组织中仍然能够检测出恩诺沙星,但是停药7 d后这3个组织中均检测不出环丙沙星。结果显示,恩诺沙星在牙鲆体内代谢速度较慢,而且只是在一段时间内有脱乙基代谢为环丙沙星的反应发生,但并不是在恩诺沙星消除的全过程都发生,而且代谢物环丙沙星在牙鲆体内的消除速度要比恩诺沙星快。 相似文献
20.
土霉素在奥尼罗非鱼体内的药动学研究 总被引：2，自引：0，他引：2
在(21±1)℃的水温条件下,以50 mg/kg的单剂量,分别给奥尼罗非鱼(Oreochromis aureus×O.niloticus)水剂口灌和混饲口灌土霉素,用高效液相色谱法(HPLC)检测给药后各个时间点的血药浓度。结果显示:最低检测限为0.005μg/mL,线性范围为0.005~4μg/mL。水剂口灌组和混饲口灌组的药时数据均符合具时滞的二室开放动力学模型,水剂口灌组的动力学方程为:Ct=0.231e-0.028(t-0.010)+0.353e-0.011(t-0.010)-0.584e-0.468(t-0.010),混饲口灌组动力学方程:Ct=0.839e-0.057(t-0.459)+0.442e-0.013(t-0.459)-1.281e-0.282(t-0.459)。水剂口灌组及混饲口灌组主要药动学参数分别为:吸收半衰期(t1/2ka)为1.481 h,2.458 h;分布半衰期(t1/2α)为24.834 h,12.193 h;消除半衰期(t1/2β)为60.312 h,51.533 h;达峰时间(Tmax)为7.230 h,8.221 h;最大血药浓度(Cmax)为0.494μg/mL,0.796μg/mL;血药浓度-时间曲线下面积(AUC)=37.74μg.h/mL,43.075μg.h/mL。这些参数表明,水剂口灌比混饲口灌吸收快,分布和消除慢,在血液中达到峰浓度的时间更短,但峰浓度值比混饲口灌低。 相似文献