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1.
喹烯酮在猪体内的代谢物研究   总被引:5,自引:2,他引:5  
对5只猪按30 mg/kg单剂量口服给药,进行喹烯酮在猪体内侧链结构断开的代谢物研究。依据本试验建立的HPLC方法进行尿液代谢物含量测定。结果表明,喹烯酮以3-甲基-2-羧酸喹口恶啉的形式从尿中排出。  相似文献   

2.
本研究建立了鸡肉中卡巴氧、喹乙醇的代谢物残留的液相色谱-串联高分辨质谱测定方法。鸡肉样品经酸解后,固相萃取净化,液相色谱-串联四极杆静电场轨道阱高分辨质谱测定,稳定同位素内标定量。卡巴氧、喹乙醇的代谢物喹喔啉-2-羧酸、3-甲基-喹喔啉-2-羧酸在0.5μg/kg~10 g/kg范围内线性关系良好,最低定量限0.5μg/kg,检测限0.2μg/kg。高中低浓度精密度20%(RSD%),平均回收率70%~120%。经实际样品的测定,本方法简便、实用,适宜于大批量样品的测定。  相似文献   

3.
喹乙醇曾作为水产养殖动物饲料添加剂被广泛应用。随着人们对其毒性和危害的认识,对其使用也做出了新的规定。本文对喹乙醇的毒性及其与主要代谢物3-甲基-喹噁啉-2-羧酸(MQCA)的药代动力学、残留检测方法等做一简述。  相似文献   

4.
通过喹赛多(Cyadox,CYX)在大鼠体内消除规律研究,了解其对食品安全的影响,并为今后的药理学和毒理学研究提供较为详细的数据基础,研究建立了喹赛多及其两种主要代谢产物脱二氧喹赛多(BDCYX)和喹噁啉-2-羧酸(QCA)的提取和HPLC检测方法,并以大鼠作为研究载体,按推荐剂量连续混饲给药7 d后,研究喹赛多及其两种代谢物在血浆、肌肉、肝脏中消除规律;一次性灌胃给药后研究喹赛多及其两种代谢物在排泄物中的消除规律特点。结果表明,CYX和BDCYX在0~24 h和24~48 h时间段的粪便中可大量检出,在血浆、肌肉、肝脏和尿液中未检出;QCA在6 h的肌肉中有少量残留,在肝脏中一直到72 h还有一定量的残留,在血浆和粪便中未发现其存在。本研究结果为今后喹赛多在体内处置研究提供了可直接借鉴的技术手段和理论基础。  相似文献   

5.
鸡肉中喹乙醇、卡巴多及其代谢物的残留检测   总被引:3,自引:0,他引:3  
建立了测定鸡肉组织样品中喹乙醇、卡巴多以及喹噁啉-2-羧酸残留量的高效液相色谱法。鸡肉样品中的药物用乙腈与乙酸乙酯的混合液(1∶1,V/V)提取,经过浓缩、净化,用甲醇定容进行检测。色谱拄为Atlantis C18柱,流动相由甲醇、水和乙酸钠缓冲液(pH 4.6)组成,采用梯度洗脱程序;检测波长为320和380 nm。喹乙醇、卡巴多及噁喹啉-2-羧酸在0.05~1.0μg/mL浓度范围内,药物峰面积与浓度值呈良好的线性关系,其相关系数分别为0.997 5、0.997 9、0.998 2。空白鸡肉中添加药物浓度为0.05、0.1、0.2和0.5μg/?时,喹乙醇的回收率为(70.6±3.1)%~(87.5±3.6)%;卡巴多为(73.2±3.7)%~(91.5±2.7)%;喹噁啉-2-羧酸为(71.9±4.3)%~(86.6±3.5)%。喹乙醇、卡巴多和喹噁啉-2-羧酸的最低检测限分别为0.05、0.015、0.025μg/mL。  相似文献   

6.
近年来水产养殖中的常用药物恩诺沙星在鲫中的残留问题比较突出,但目前国家未对其在鲫中的休药期作出明确规定。为做到鲫养殖中科学合理使用恩诺沙星,在12~15℃水温条件下,以60 mg/kg.b.w.剂量,对体质量为(250±10)g的健康方正银鲫(Carassius auratus gibelio)灌服恩诺沙星;在灌服后0~120 d内不间断采样,用高效液相色谱-串联质谱仪检测,研究恩诺沙星及其代谢产物环丙沙星在方正银鲫鳃、血浆、肌肉、皮肤、肝脏和肾脏中的代谢及消除规律,从而为恩诺沙星在方正银鲫中的休药期制定提供参考。结果显示:灌药后,恩诺沙星在方正银鲫血浆、肌肉、肝脏、鳃、肾脏和皮肤中的达峰时间t_(max)分别为9、18、24、24、48和48 h,肾脏、肝脏、肌肉、血浆、鳃和皮肤中的达峰浓度c_(max)分别为30.490、21.372、18.715、16.636、15.157和11.663 mg/kg;皮肤中的消除半衰期t_(1/2β)最大,为338.2 h,血浆中最小,为93.303 h;代谢产物环丙沙星的代谢及消除趋势与恩诺沙星大致相同,血浆中达峰值产生最早,t_(max)为18 h,肾脏中的峰浓度最大,c_(max)为547.26μg/kg。结果表明,方正银鲫以单次口灌60 mg/kg.b.w.剂量恩诺沙星,皮肤和肌肉中的恩诺沙星和环丙沙星总量需要1 200度日才能满足限量要求。本研究为恩诺沙星在鲫鱼养殖中的科学使用提供了数据支撑。  相似文献   

7.
通过贝鲁特反应和还原、脱羧反应在体外合成制备3-甲基喹噁啉-2-羧酸,并进行理化鉴定和抗菌活性测试;通过MTT方法研究3-甲基喹噁啉-2-羧酸对多种细胞的生长抑制作用,利用单细胞电泳研究其对细胞DNA的损伤作用,利用流式细胞术研究其对细胞周期的改变。结果显示,体外成功合成制备出3-甲基喹噁啉-2-羧酸,而3-甲基喹噁啉-2-羧酸几乎没有抗菌效果,对多种细胞的生长抑制作用较弱,在剂量检测范围内细胞抑制率不到30%,但在一定剂量下能导致细胞DNA损伤,主要表现为尾长和尾部DNA含量显著升高;并且3-甲基喹噁啉-2-羧酸也能改变Chang细胞的细胞周期,表现为S期阻滞。结果表明,3-甲基喹噁啉-2-羧酸具有一定的细胞毒性。  相似文献   

8.
建立了中兽药制剂中喹乙醇、乙酰甲喹、卡巴氧、喹烯酮等药物含量测定的高效液相色谱法。样品经三氯甲烷:甲醇(3:1)提取后,苯基柱分离,在360nm处检测。四种喹嗯啉类药物在0.2~100μg/mL浓度范围内呈线性相关。在空白样品中添加50~150mg/kg,回收率范围在87.90%~96.82%之间,批内变异系数为0.55%~4.65%。本方法的检测限为20mg/kg,定量限为50mg/kg。结果表明,本方法适合中兽药制剂中喹嗯啉类药物的测定。  相似文献   

9.
HPLC检测猪血浆和尿液中的喹烯酮及其主要代谢物   总被引:5,自引:3,他引:2  
本试验旨在建立猪血浆和猪尿液中喹烯酮及其主要代谢物3-甲基-喹噁啉-2-羧酸(MQCA)、脱一氧喹烯酮、脱二氧喹烯酮同时检测的高效液相色谱法。血浆样品用乙腈沉淀蛋白,经高速离心后直接检测。尿液样品用乙酸乙酯提取喹烯酮、脱一氧喹烯酮、脱二氧喹烯酮,用盐酸提取MQCA,再用乙酸乙酯萃取,50 ℃氮气吹干后过HLB固相萃取小柱。以0.1%甲酸水-乙腈为流动相梯度洗脱,314 nm波长下检测。喹烯酮及3种代谢物在血浆中的回收率在72.54%~104.2%之间,尿液中的回收率在63.20%~86.24%之间。4种目标化合物在血浆和尿液中定量限均为0.05 μg/mL。  相似文献   

10.
采用高效液相色谱法,对以80mg/kg b.W.单剂量口灌磺胺甲嗯唑的大菱鲆进行连续采样监测,研究大菱鲆口服磺胺甲嗯唑的药代动力学特征及残留消除规律。结果表明,磺胺甲嗯唑在大菱鲆血液、肌肉中药代动力学特征分别符合带时滞的一级吸收二室开放模型、一级吸收一室开放模型。磺胺甲嗯唑在大菱鲆体内消除速度较慢,16℃水温的实验条件下,在大菱鲆肌肉中的休药期为27天。  相似文献   

11.
采用高效液相色谱-质谱法,研究肌肉注射给药方式下,喹乙醇及其代谢物在罗非鱼(Tilapiafish)体内的药物代谢动力学.罗非鱼注射给药20 mg/kg后,其血浆、肌肉、肝脏中药物浓度-时间曲线关系符合一级吸收的二室开放动力学模型.喹乙醇在罗非鱼体内消除较快,在血液、肌肉、肝脏中的消除半衰期(t 1/2β)分别为5.2...  相似文献   

12.
为检测猪、鸡可食性组织中喹噁啉类兽药残留标示物喹噁啉-2-羧酸(QCA)和3-甲基喹噁啉-2-羧酸(MQ-CA),建立了同时检测这2种残留标示物的高效液相色谱-串联质谱法.将样品碱水解,乙酸乙酯等液-液萃取,65℃氮气吹干,甲醇:0.5%甲酸水溶液(30:70)溶解,0.45μm微孔滤膜过滤后,采用高效液相色谱-串联质谱分析.结果显示,猪、鸡可食性组织中喹噁啉类兽药残留标示物MQCA和QCA检测限为0.2~0034μg/kg和0.5~0.9μg/kg,定量限为0.5~0.61μg/kg和0.77~1.31μg/kg.相对回收率在90.07%~106.8%范围内,日内变异系数≤13.69%.日间变异系数≤15.43%.MQCA和QCA在2~100μg/kg范围内具有较好的线性关系(r~2>0.99).结果表明,本方法简单、灵敏度高.适用于猪、鸡可食性组织中喹噁啉类兽药残留标示物的定量检测.  相似文献   

13.
试验采用高效液相色谱分析法,对饲喂含有不同浓度喹乙醇饲料(75mg/kg、100mg/kg、125mg/kg)的猪体组织(肝脏、肾脏、肌肉)和血浆中喹乙醇含量进行检测,分析喹乙醇在猪体内的残留分布,探讨喹乙醇在血浆中的含量与猪体内组织的残留含量的相关性。结果表明:饲料中喹乙醇添加量与组织和血浆中残留量均呈线性相关关系;同一浓度的喹乙醇添加量在猪组织和血浆中的残留量分布:肝脏>肾脏>肌肉>血浆;建立的血浆与组织间残留量的回归方程具有较高的可靠性。  相似文献   

14.
The pharmacokinetics of amoxicillin (Amx) were determined in pigs following intravenous (IV) administration of a single dose of 15 mg/kg and a single dose of 15 mg/kg of a new oral formulation (Amx-FP containing 10% amoxicillin). Residue studies were performed to determine residues in edible tissues of healthy pigs after chronic oral administration of Amx-FP at a daily dose of 15 mg/kg for five consecutive days. After IV administration, the plasma concentration was characteristic of a two-compartment open model. The main pharmacokinetic variables were: t(1/2lambda(n)), MRT=90.1 min, V(darea)=0.81 L/kg and Cl(b)=3.9 mL/kg/min. After single oral administration the main pharmacokinetic variables were: C(max)=758 mug/L, t(max)=347 min and Cl(b/f)=3.7 mL/kg/min for Amx-FP. The oral bioavailability (F) was calculated at 11% for Amx-FP. Based on maximum residue levels (MRL) for AMX in pigs established at 50 microg/kg for all tissues, the withdrawal times of AMX in muscle and skin plus fat were estimated (95% tolerance limit and 95% confidence) to fall below the MRL after a withdrawal period of seven days. Levels of AMX in the liver and kidneys were estimated to fall below the MRL after a withdrawal period of four days.  相似文献   

15.
To estimate the consumer exposure to olaquindox (OLA) residues in porcine edible tissues, a physiologically based pharmacokinetic (PBPK) model for methyl‐3‐quinoxaline‐2‐carboxylic acid (MQCA), the marker residue of OLA, was developed in pigs based on the assumptions of the flow‐limited distribution, hepatic metabolism, and renal excretion. The model included separate compartments corresponding to blood, muscle, liver, kidney, adipose, and an extra compartment representing the remaining carcass. Physiological parameters were determined from literatures. Plasma protein binding, partition coefficients, and renal clearance for MQCA were determined in in vitro and in vivo studies. The metabolic conversion of OLA to MQCA was assumed as a simple, one‐step process, and an apparent first‐order rate constant (k) was employed to describe this metabolic process. The PBPK model was optimized and validated with plasma and tissue data from literatures and our study. Sensitivity analysis and Monte Carlo simulation were also implemented to estimate the influence of model parameters on the goodness of fit. When compared with the observed data, the PBPK model underestimated the MQCA level in all compartments at the early time points, whereas gave excellent predictions of MQCA concentration in porcine edible tissues at later time points. The correlation coefficients between the predicted and observed values were over 0.88. The consistency between the model predictions and the real residues of OLA in pigs proved the good applicability of our model in food safety risk assessment.  相似文献   

16.
喹乙醇是饲料中常见的促生长剂,适量使用有利于鱼类的生长,但过量喹乙醇会对鲤鱼鳃、肾脏、肝脏等组织产生一系列的毒害作用。因此在水产养殖中应该对喹乙醇的使用量加以控制。本文从组织受损、营养代谢和生理生化功能等方面综述了喹乙醇对鲤鱼的毒性及作用机理。  相似文献   

17.
喹烯酮在鸡体内的代谢及药物动力学研究   总被引:2,自引:0,他引:2  
以HPLC-MS/MS为定量手段,研究了喹烯酮经静脉注射(2.5 mg/kg)、口服(30 mg/kg)两种给药途径在鸡体内的代谢及药物动力学特征.鸡静脉注射喹烯酮后,血浆中检测到喹烯酮原药和1-脱氧喹烯酮;口服灌注喹烯酮后,血浆中检测到喹烯酮原药和3-甲基喹噁啉-2-羧酸(MQCA).喹烯酮在鸡体内的药动学数据采用统...  相似文献   

18.
鲤鱼急性喹乙醇中毒的病理学研究   总被引:15,自引:0,他引:15  
试验对鲤鱼进行了喹乙醇急性中毒的病理学研究。喹乙醇对鲤鱼 (60± 5g)口服给药的LD50 为 :32 4 9 4mg/kg体重。中毒鱼表现出特征性的“应激性出血症” ,鳍条基部、嘴部和腹部充血、出血发红 ,肠道排出白色半透明粘液便 ,临死前出现明显的神经症状。病理组织学上 ,肝脂肪变性或水泡变性及凝固性坏死 ,肾上腺空泡变性 ,肠呈卡他性肠炎 ,肾小管上皮细胞、心肌纤维空泡变性 ;鳃小片水肿 ,上皮增生、变性、坏死和脱落。超微结构上 ,心肌、肝和肾小管上皮细胞的线粒体肿胀 ,嵴断裂、溶解 ,肝细胞内糖原颗粒减少。中毒早期肠上皮微绒毛断裂 ,脱落 ,随着病程的发展肠上皮细胞变性、坏死、脱落。  相似文献   

19.
AIMS: To determine the plasma disposition and concentrations of ivermectin (IVM) in eggs produced by laying hens following S/C, oral and I/V administration.

METHODS: Twenty-four laying hens, aged 37 weeks and weighing 1.73 (SD 0.12) kg were allocated to three groups of eight birds. The injectable formulation of IVM was administered either orally, S/C, or I/V, at a dose of 0.2?mg/kg liveweight, following dilution (1:5, v/v) with propylene glycol. Heparinised blood samples were collected at various times between 0.25 hours and 20 days after drug administration. Eggs produced by hens were also collected daily throughout the study period. Samples of plasma and homogenised egg were analysed using HPLC.

RESULTS: Maximum concentrations of IVM in plasma and mean residence time of IVM were lower after oral (10.2 (SD 7.2) ng/mL and 0.38 (SD 0.14) days, respectively) than after S/C (82.9 (SD 12.4) ng/mL and 1.05 (SD 0.24) days, respectively) administration (p<0.01). The time to maximum concentration and elimination half-life were shorter following oral (0.14 (SD 0.04) and 0.23 (SD 0.11) days, respectively) than S/C (0.25 (SD 0.00) and 1.45 (SD 0.45) days, respectively) administration (p<0.01). IVM was first detected in eggs 2 days after treatment in all groups and was detected until 8 days after oral and I/V administration, and until 15 days after S/C administration. Peak concentrations of IVM were 15.7, 23.3 and 1.9?µg/kg, observed 2, 5 and 4 days after I/V, S/C and oral administration, respectively.

CONCLUSIONS AND CLINICAL RELEVANCE: The low plasma bioavailability of IVM observed after oral administration in laying hens could result in lower efficacy or subtherapeutic plasma concentrations, which may promote the development of parasitic drug resistance. Due to high IVM residues in eggs compared to the maximum residue limits for other food-producing animal species, a withdrawal period should be necessary for eggs after IVM treatment in laying hens.  相似文献   

20.
Six pigs were used in a two-period crossover study to investigate the pharmacokinetics of amoxycillin after single intravenous and oral doses of 20 mg/kg bodyweight. Twelve pigs were used to study the residues of the drug in muscle, kidney, liver and fat after they had received daily oral doses of 20 mg/kg amoxycillin for five days. The mean (sd) elimination half life (t1/2beta) and mean residence time of amoxycillin in plasma were 3.38 (0.30) and 3.54 (0.43) hours, respectively, after intravenous administration and 4.13 (0.50) and 4.47 (0.30) hours, respectively, after oral administration. After oral administration, the maximum plasma concentration (Cmax) was 7.37 (0.42) microg/ml and it was reached after 0.97 (0.29) hours. Six days after the last oral dose, the mean concentration of amoxycillin in the pigs' kidneys was 21.38 ng/g and in the liver it was 12.32 ng/g, but no amoxycillin could be detected in fat or muscle; the concentrations of amoxycillin in edible tissues were less than the European Union maximal residue limit of 50 microg/kg.  相似文献   

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