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Feray Altan Orhan Corum Ramazan Yildiz Hatice Eser Faki Merve Ider Mahmut Ok Kamil Uney 《Journal of veterinary pharmacology and therapeutics》2020,43(2):108-114
In this study, the pharmacokinetics of moxifloxacin (5 mg/kg) was determined following a single intravenous administration of moxifloxacin alone and co-administration with diclofenac (2.5 mg/kg) or flunixin meglumine (2.2 mg/kg) in sheep. Six healthy Akkaraman sheep (2 ± 0.3 years and 53.5 ± 5 kg of body weight) were used. A longitudinal design with a 15-day washout period was used in three periods. In the first period, moxifloxacin was administered by an intravenous (IV) injection. In the second and third periods, moxifloxacin was co-administered with IV administration of diclofenac and flunixin meglumine, respectively. The plasma concentration of moxifloxacin was assayed by high-performance liquid chromatography. The pharmacokinetic parameters were calculated using a two-compartment open pharmacokinetic model. Following IV administration of moxifloxacin alone, the mean elimination half-life (t1/2β), total body clearance (ClT), volume of distribution at steady state (Vdss) and area under the curve (AUC) of moxifloxacin were 2.27 hr, 0.56 L h−1 kg−1, 1.66 L/kg and 8.91 hr*µg/ml, respectively. While diclofenac and flunixin meglumine significantly increased the t1/2β and AUC of moxifloxacin, they significantly reduced the ClT and Vdss. These results suggest that anti-inflammatory drugs could increase the therapeutic efficacy of moxifloxacin by altering its pharmacokinetics. 相似文献
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The pharmacokinetics of amikacin (AMK) were investigated after intravenous (i.v.) and intramuscular (i.m.) administration of 7.5 mg/kg bw in 6 healthy lactating sheep. After i.v. AMK injection (as a bolus), the elimination half-life (t1/2beta), the volume of distribution (Vd,area), the total body clearance (ClB) and the area under the concentration-time curve (AUC) were 1.64 +/- 0.06 h, 0.19 +/- 0.02 L/kg, 1.36 +/- 0.1 ml/min per kg and 94.09 +/- 6.95 (microg.h)/ml, respectively. The maximum milk concentration of AMK (Cmax), the area under the milk concentration-time curve (AUCmilk) and the ratio AUCmilk/AUCserum were 1.18 +/- 0.22 microg/ml, 22.45 +/- 3.21 (micro.h)/ml and 0.24 +/- 0.02, respectively. After i.m. administration of AMK the t1/2beta, Cmax, time of Cmax (tmax) and absolute bioavailability (Fabs) were 1.29 +/- 0.1 h, 16.97 +/- 1.54 microg/ml, 1.0 +/- 0 h and 64.88% +/- 6.16%, respectively. The Cmax, AUCmilk and the ratio AUCmilk/AUCserum were 0.33 microg/ml, 1.67 (microg.h)/ml and 0.036, respectively. 相似文献
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二甲苯胺噻唑在绵羊脑脊液中的药物动力学研究 总被引：1，自引：0，他引：1
以内标气相色谱法为定量手段，研究二甲苯胺噻唑在绵羊脑脊液（ＣＳＦ）中的药动力学。实验结果表明，绵羊肌注二甲苯胺噻唑（２．５ｍｇ／ｍｌ）后，ＣＳＦ药物经时特征主要符合一级吸收单室开放模型，部分符合一级吸收双室开放模型，其主要药动学参数：吸收半衰期为３．８６８±１．４５２ｍｉｎ，消除半衰期为１４０．３３８±１１０．０３８ｍｉｎ，ＣＳＦ药浓度达峰时间为１７．６３７±５．８５０ｍｉｎ，ＣＳＦ药峰浓度为０． 相似文献
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替米考星在绵羊体内的药代动力学研究 总被引：1，自引：0，他引：1
5只健康小尾寒羊,采用静脉和皮下注射2种途径以替米考星10mg/kg体重剂量给药,进行体内药代动力学研究。动物给药后在96h内分点采血,血浆样品处理采用甲醇沉淀,离心去蛋白,调节pH值并用氯仿提取替米考星;样品测定采用苯基柱,以反向HPLC测定绵羊血清中的替米考星浓度。结果表明,绵羊静注和皮下注射替米考星的药时数据均符合二室开放模型,替米考星皮下注射和静脉给药在羊体内具有吸收和分布较迅速,消除缓慢,体内分布容积大,生物利用度较高的特点。结果对了解替米考星在绵羊体内的药动学特征以及指导临床正确用药具有重要意义。 相似文献
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The resulting serum concentrations were measured in six ewes after intramuscular administration of 10 mg/kg of gentamicin. The model providing the best fit for the experimental data was determined both by linear regression analysis between the experimental and theoretical values and by means of the Minimum Akaike Information Criterion Estimation (MAICE) test.Linear regression analysis showed certain differences favouring the monocompartmental model although the advantage was not conclusive. The MAICE test, however, permitted a clear discrimination in favour of the same model. When linear regression analysis is not conclusive, the MAICE test represents a good alternative. 相似文献
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国产表阿佛菌素在绵羊体内的药代动力学研究 总被引：1，自引：0，他引：1
用反相高效液相色谱结合荧光检测法,对试验绵羊经静脉、皮下单剂量注射0 2 mg/kg表阿佛菌素的药代动力学进行了研究。血样提取物通过C18小柱富集、洗脱,甲醇洗提部分经加入1 甲基咪唑和三氟乙酸酐的乙腈液衍生化后进行色谱分析。血药浓度在 2. 5 ~ 200 ng/mL 范围呈良好线性关系(R= 0 996 8),方法平均回收率96 65%±3.84%,血药最低检测限 2.5 ng/mL,日内、日间变异系数分别小于 10%、12%。2 种途径给药后体内药物运转分别符合二室和一室开放模型。主要药代参数如下,静脉注射:消除半衰期(T1/2β)12.66±2.05 h,药时曲线下面积(AUC0~74)1.02±0 30 (mg/L)·h,fc=0 13±0 05; 皮下注射:吸收半衰期(T1/2ka )4.42±1.04 h,峰浓度(Cmax)0 02±0 01 μg/mL,峰时(Tmax ) 15. 36±2. 91 h,消除半衰期(t1/2k ) 26. 22±9. 04 h,药时曲线下面积(AUC0~122)1.19±0 37 (mg/L)·h。上述结果表明,绵羊静脉注射表阿佛菌素后体内药物分布广泛,消除较慢。皮下注射吸收好,消除比静脉注射更为缓慢,体内药物平均滞留时间长。 相似文献
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研究了克洛素隆注射剂在绵羊体内的药物动力学过程。以邻甲苯磺酰胺为内标,建立应用RP-HPLC检测绵羊血浆中克洛素隆含量的方法,血浆浓度在0.01μg/mL~1.0μg/mL及1.0μg/mL~20.0μg/mL范围呈良好线性关系,方法回收率和精密度均能满足药物动力学分析的要求。结果表明,绵羊按4mg/kg单剂量皮下注射克洛素隆,体内药物运转符合二室开放模型。主要药物动力学参数分别为:t1/2Ka=1.355h±0.746h,t1/2β=17.924h±9.186h,tmax=3.181h±1.046h,Cmax=5.121μg/mL±0.997μg/mL,AUC=56.730(mg/L)·h±5.248(mg/L)·h。克洛素隆注射剂皮下注射吸收快,消除较慢,适于绵羊临床寄生虫病的防治。 相似文献
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为研究阿莫西林在藏系羊体内的药物动力学特征,了解阿莫西林在藏系羊体内的吸收、分布、转化及排泄规律,以期为牧区兽医临床用药提供依据。本试验选取8只成年藏系羊,阿莫西林口灌给药,不同时间点采集藏系羊血液,利用高效液相色谱法测定血浆中药物浓度。结果表明,阿莫西林经藏系羊口灌给药(15 mg/kg.B.W)后,其主要药动学参数为:t_(1/2α)为(0.773±0.097)h,t1/2ka为(0.156±0.021)h,t_(1/2β)为(3.787±0.973)h,AUC为(8.249±1.023)μg·h/m L,T_(max)为(0.497±0.036)h,C_(max)为(2.667±0.198)μg/m L。表明阿莫西林口灌给药后,在成年藏系羊体内吸收迅速,消除较快。 相似文献
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Sara Locke Vinny Naidoo Ibrahim Hassan Neil Duncan 《The Onderstepoort journal of veterinary research》2022,89(1)
Diclofenac was responsible for the decimation of Gyps vulture species on the Indian subcontinent during the 1980s and 1990s. Gyps vultures are extremely sensitive (the lethal dose 50 [LD50] ~ 0.1 mg/kg – 0.2 mg/kg), with toxicity appearing to be linked to metabolic deficiency, demonstrated by the long T1/2 (~12 h – 17 h). This is in striking comparison to the domestic chicken (Gallus gallus domesticus), in which the LD50 is ~10 mg/kg and the T1/2 is ~1 h. The phase 1 cytochrome P450 (CYP) 2C subfamily has been cited as a possible reason for metabolic deficiency. The aim of this study was to determine if CYP2C9 homolog pharmacogenomic differences amongst avian species is driving diclofenac toxicity in Gyps vultures. We exposed each of 10 CYP-inhibited test group chickens to a unique dose of diclofenac (as per the Organisation for Economic Co-operation and Development [OECD] toxicity testing guidelines) and compared the toxicity and pharmacokinetic results to control group birds that received no CYP inhibitor. Although no differences were noted in the LD50 values for each group (11.92 mg/kg in the CYP-inhibited test group and 11.58 mg/kg in the control group), the pharmacokinetic profile of the test group was suggestive of partial inhibition of CYP metabolism. Evaluation of the metabolite peaks produced also suggested partial metabolic inhibition in test group birds, as they produced lower amounts of metabolites for one of the three peaks demonstrated and had higher diclofenac exposure. This pilot study supports the hypothesis that CYP metabolism is varied amongst bird species and may explain the higher resilience to diclofenac in the chicken versus vultures. 相似文献
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Batzias GC Delis GA Koutsoviti-Papadopoulou M 《Veterinary research communications》2005,29(8):699-712
The combination of sulphadiazine and trimethoprim is extensively used in farm animal species; however, there are no data concerning
its pharmacokinetics after intramuscular administration in sheep. Twelve rams of the Chios breed were used to study the disposition
of sulphadiazine, its metabolite N4-acetylsulphadiazine and trimethoprim after intravenous (i.v.) and intramuscular (i.m.) administration of a sulphadiazine/trimethoprim
(5:1) combination in sheep. Sulphadiazine bioavailability (±SD) was 69.00%±10.51%. The half-life of the terminal phase (4.10±0.58
h afteri. v., and 4.03±0.31 h after i.m. administration) was significantly higher than the respective value for trimethoprim
(0.59±0.19 h) afteri.v. administration. The maintenance of a constant plasma concentration ratio after i.v. administration
was therefore impossible. The acetylation capacity in sheep, determined by the AUC ratio between N4-acetylsulphadiazine and the parent compound, sulphadiazine, was very low (less than 4%). The most remarkable finding of this
study was that trimethoprim was not detected in sheep plasma after i.m. injection. In conclusion, according to the findings
of the present study, following i.v. administration of the sulphadiazine/trimethoprim combination, trimethoprim can be considered
as the limiting factor for any possible synergistic effect, and the i.m. route cannot be recommended in sheep. 相似文献
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Lifschitz A. Virkel G. Mastromarino M. Lanusse C. 《Veterinary research communications》1997,21(3):201-211
Lifschitz, A., Virkel G., Mastromarino, M. and Lanusse C., 1997. Enhanced plasma availability of the metabolites of albendazole in fasted adult sheep. Veterinary Research Communications, 21 (3), 201-211The influence of fasting prior to treatment and of dosing rate on the plasma availability and disposition kinetics of albendazole (ABZ) and its sulphoxide (ABZSO) and sulphone (ABZSO2) metabolites was studied in adult sheep grazing on pasture. A micronized suspension of ABZ was administered orally at either 7.5 mg/kg (group A) or 11.3 mg/kg (group C) to sheep fed ad libitum, and at 7.5 mg/kg to sheep subjected to a 24 h fasting period prior to treatment (group B). Blood samples were taken serially over 96 h after treatment, and the plasma was analysed for ABZ and its metabolites by high-performance liquid chromatography. ABZSO and ABZSO2 were recovered from the plasma. Fasting induced marked modifications in the pharmacokinetic behaviour of the ABZ metabolites in sheep. An extended absorption process, with a delayed peak concentration in the plasma, was observed for both metabolites in the fasted sheep. Significantly higher area under the curve (AUC) and peak plasma concentration (Cmax) values were obtained for both metabolites in the fasted animals compared to those fed ad libitum. Delayed elimination with prolonged detection in plasma was also observed in the fasted sheep. Treatment with ABZ at 7.5 mg/kg in the starved animals resulted in bioequivalence to the administration of the compound at a 50% higher dose rate (11.3 mg/kg) in the fed animals. It is suggested that fasting enhances ABZ dissolution and absorption by delaying its passage down the digestive tract. 相似文献
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Giulia Maria De Benedictis Mario Giorgi Alice Depase Virginia De Vito Giorgia della Rocca Luca Bellini 《Veterinary anaesthesia and analgesia》2017,44(5):1245-1252
Objective
To evaluate the pharmacokinetics of two doses of tramadol during isoflurane anaesthesia in sheep and their ability to prevent the cardiovascular response induced by surgical stimulation.Study design
Prospective randomized controlled study.Animals
A total of 12 healthy sheep (mean weight, 47.5 ± 7.9 kg) undergoing lumbar transpedicular intervertebral disk nucleotomy.Methods
Sheep were sedated with medetomidine, anaesthesia was induced with propofol and maintained with isoflurane at 1.5 vol.%. Baseline heart rate and blood pressure were measured and sheep were randomly assigned an intravenous injection of tramadol (4 or 6 mg kg?1). Fentanyl was injected as rescue analgesic if cardiovascular parameters were increased more than 20% compared to baseline. If those variables were below 20% of baseline, the concentration of isoflurane was gradually decreased until parameters returned to the original value. Blood collections were performed at pre-assigned times, and concentrations of tramadol and O-desmethyltramadol (M1) assessed by high-performance liquid chromatography.Results
Time from premedication to anaesthesia induction, anaesthesia time, propofol dose and intraoperative body temperature were similar between doses. Cardiovascular variables remained between ±20% of baseline value, and no statistical difference was observed between treatments. Regardless of the dose of tramadol administered, arterial blood pressure was statistically higher than baseline 10 minutes after tramadol administration, but it gradually returned to previous values. A two-compartment model and a non-compartment model described the pharmacokinetics of tramadol and M1, respectively. Plasma concentrations of tramadol rapidly decreased in the first 2 hours for both doses with an elimination half-life of more than 40 minutes. The M1 maximum concentration was similar for both doses, and it was detected in plasma after 35 minutes.Conclusions and clinical relevance
Both doses of tramadol provided adequate cardiovascular stability during spinal surgery in sheep. The pharmacokinetic variables may be used to plan the dosage regime during general anaesthesia. 相似文献16.
Orhan Corum Duygu Durna Corum Ayse Er Kamil Uney 《Journal of veterinary pharmacology and therapeutics》2019,42(6):647-653
The purpose of this study was to determine the pharmacokinetics of cefquinome (CFQ) following single and repeated subcutaneous (SC) administrations in sheep. Six clinically healthy, 1.5 ± 0.2 years sheep were used for the study. In pharmacokinetic study, the crossover design in three periods was performed. The withdrawal interval between the study periods was 15 days. In first period, CFQ (Cobactan, 2.5%) was administered by an intravenous (IV) bolus (3 sheep) and SC (3 sheep) injections at 2.5 mg/kg dose. In second period, the treatment administration was repeated via the opposite administration route. In third period, CFQ was administrated subcutaneously to each sheep (n = 6) at a dose of 2.5 mg/kg q. 24 hr for 5 days. Plasma concentrations of CFQ were measured using the HPLC‐UV method. Pharmacokinetic parameters were calculated using non‐compartmental methods. The elimination half‐life and mean residence time of CFQ after the single SC administration were longer than IV administration (p < 0.05). Bioavailability (F%) of CFQ following the single SC administration was 123.51 ± 11.54%. The area under the curve (AUC0‐∞) and peak concentration following repeated doses (last dose) were higher than those observed after the first dose (p < 0.05). CFQ accumulated after repeated SC doses. CFQ can be given via SC at a dose of 2.5 mg/kg every 24 hr for the treatment of infections caused by susceptible pathogens, which minimum inhibitory concentration is ≤1.0 μg/ml in sheep. 相似文献
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Huseyin Gungor;Orhan Corum;Duygu Durna Corum;Alper Serhat Kumru;Gökhan Yilmaz;Devran Coskun;Alparslan Coskun;Kamil Uney; 《Journal of veterinary pharmacology and therapeutics》2024,47(3):202-207
The aim of this study is to determine the pharmacokinetic change after intravenous administration of meloxicam at doses of 0.5, 1 and 2 mg/kg to sheep. The study was carried out on six Akkaraman sheep. Meloxicam was administered intravenously to each sheep at 0.5, 1, and 2 mg/kg doses in a longitudinal pharmacokinetic design with a 15-day washout period. Plasma concentrations of meloxicam were determined using the high performance liquid chromatography-ultraviolet, and pharmacokinetic parameters were evaluated by non-compartmental analysis. Meloxicam was detected up to 48 h in the 0.5 mg/kg dose and up to 96 h in the 1 and 2 mg/kg doses. As the dose increased from 0.5 to 2 mg/kg, terminal elimination half-life, and dose normalized area under the concentration versus time curve increased and total clearance decreased. Compared to the 1 mg/kg dose, it was determined that Vdss decreased and C0.083h increased in the 2 mg/kg dose. Meloxicam provided the therapeutic concentration of >0.39 μg/mL reported in other species for 12, 48 and 96 h at 0.5, 1 and 2 mg/kg doses, respectively. These results show that meloxicam exhibits non-linear pharmacokinetics and will achieve unpredictable plasma concentrations when administered IV for a rapid effect at dose of ≥1 mg/kg in sheep. 相似文献
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Evelyn E. MacKay Kevin E. Washburn Ashley L. Padgett Virginia R. Fajt Chih‐Ping Lo Travis P. Mays Shannon E. Washburn 《Journal of veterinary pharmacology and therapeutics》2019,42(4):373-379
Macrolides are important antimicrobials frequently used in human and veterinary medicine in the treatment of pregnant women and pregnant livestock. They may be useful for the control of infectious ovine abortion, which has economic, animal health, and human health impacts. In this study, catheters were surgically placed in the fetal vasculature and amnion of pregnant ewes at 115 (±2) days of gestation. Ewes were given a single dose of 2.5 mg/kg tulathromycin subcutaneously, and drug concentrations were determined in fetal plasma, maternal plasma, and amniotic fluid at 4, 8, 12, 24, 36, 48, 72, 144, and 288 hr after drug administration. Pharmacokinetic parameters in maternal plasma were estimated using noncompartmental analysis and were similar to those previously reported in nonpregnant ewes. Tulathromycin was present in fetal plasma and amniotic fluid, indicating therapeutic potential for use against organisms in these compartments, though concentrations were lower than those in maternal plasma. Time‐course of drug concentrations in the fetus was quite different than that in the ewe, with plasma concentrations reaching a plateau at 4 hr and remaining at this concentration for the remainder of the sampling period (288 hr), raising questions about how tulathromycin may be transported into or metabolized and eliminated by the fetus. 相似文献
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Devran Coskun Orhan Corum Enver Yazar 《Journal of veterinary pharmacology and therapeutics》2020,43(3):288-296
The purpose of this study was to determine the influences of supportive therapy (ST) on the pharmacokinetics (PK) of marbofloxacin in lipopolysaccharide (LPS)-induced endotoxemic sheep. Furthermore, minimum inhibitory concentration (MIC) of marbofloxacin against Escherichia coli, Mannheimia haemolytica, Pasteurella multocida, Klebsiella pneumoniae, Salmonella spp., and Staphylococcus aureus was determined. The study was performed using a three-period cross PK design following a 15-day washout period. In the first period, marbofloxacin (10 mg/kg) was administered by an intravenous (IV) injection. In the second and third periods, marbofloxacin was co-administered with ST (lactated ringer + 5% dextrose + 0.45% sodium chloride, IV, 20 ml/kg, dexamethasone 0.5 mg/kg, SC) and ST + LPS (E. coli O55:B5, 10 µg/kg), respectively. Plasma marbofloxacin concentration was measured using HPLC-UV. Following IV administration of marbofloxacin alone, the , AUC0–∞, ClT, and Vdss were 2.87 hr, 34.73 hr × µg/ml, 0.29 L hr−1 kg−1, and 0.87 L/kg, respectively. While no change was found in the MBX + ST group in terms of the PK parameters of marbofloxacin, it was determined that the ClT of marbofloxacin decreased, AUC0–∞ increased, and and MRT prolonged in the MBX + ST + LPS group. MIC values of marbofloxacin were 0.031 to >16 µg/ml for E. coli, 0.016 to >16 µg/ml for M. haemolytica, 0.016–1 µg/ml for P. multocida, 0.016–0.25 µg/ml for K. pneumoniae, 0.031–0.063 µg/ml for Salmonella spp., and 0.031–1 µg/ml for S. aureus. The study results show the necessity to make a dose adjustment of marbofloxacin following concomitant administration of ST in endotoxemic sheep. Also, the PK and pharmacodynamic effect of marbofloxacin needs to be determined in naturally infected septicemic sheep following concomitant administration of single and ST. 相似文献
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替米考星静脉及皮下注射后在绵羊体内的药代动力学研究 总被引：1，自引：0，他引：1
健康成年杂交绵羊静脉和皮下注射替米考星注射液后,用反相高效液相色谱法测定不同时间点血清中的药物浓度。采用3p97药代动力学程序软件处理数据,替米考星两种给药途径的药 时数据均符合二室开放模型静脉注射给药(5 mg/kg bw)的主要药代动力学参数: t1/2a 为 0. 611±0. 017 h、t1/2β为 23. 215±0. 459 h、AUC为11 815±0.396(μg/mL)·h、CL(s)为 0.424±0.014 L/(kg·h)。替米考星皮下注射主要药代动力学参数: 1mg/kg bw剂量组 t1/2a 为 1 751±0 557 h、t1/2β为 22 896±2 747 h、t1/2Ka 为 0. 100±0. 025 h、AUC 为 25. 828±1 479 (μg/mL)·h、CL(s)为0.393±0.017 L/(kg·h),Tmax为0.500±0.065 h,Cmax为1.424±0.156μg/mL、F为109.28%±6.25%。30 mg/kg bw剂量组 t1/2a为1.342±0.244 h、t1/2β为 20.052±1.236 h、t1/2Ka为 0.086±0.015h、AUC为57 575±6.760 (μg/mL)·h、CL(s)为0.527±0.068 L/(kg·h)、Tmax为0.437±0.039 h、Cmax为 3.343±0 512μg/mL、F为81.22%±9.54%。结果表明,绵羊静脉和皮下注射替米考星体内分布广,消除缓慢;皮下注射后在体内吸收迅速,达峰快,生物利用度高。 相似文献