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1.
《动物医学进展》2020,(7)
研究伊维菌素微乳剂在绵羊体内的药代动力学,对比高含量伊维菌素微乳剂与普通注射剂型的生物利用度差异。选取12只绵羊,分为2组,按照0.2 mg/kg体重分别皮下注射10 mg/mL伊维菌素注射液和30 mg/mL伊维菌素微乳剂。分别在给药前0.5 h,给药后2、4、6、8、10、12、16、20、24、36、48、96、144、192、240、336 h在颈静脉采集血液备用,用高效液相色谱荧光检测器对绵羊血浆中的伊维菌素进行检测,并利用内标法计算其含量。通过DAS2.1.1软件进行数据统计分析。结果显示,伊维菌素微乳剂组药时曲线下面积(AUC)为3 812.17 ng/mL·h,达峰浓度(C_(max))为97.71 ng/mL,达峰时间(T_(max))为12 h,消除半衰期(T_(1/2z))为43.46 h;伊维菌素注射液组AUC为2 501.25 ng/mL·h,C_(max)为48.15 ng/mL,T_(max)为24 h,T_(1/2z)为44.96 h。说明伊维菌素微乳剂吸收效果好,达峰时间短,达峰浓度高,生物利用度高。 相似文献
2.
为了探讨复方伊维菌素乳液在动物体内的药物代谢,为兽医临床提供用药参考。试验选取7只山羊,每只山羊按0.1 mL/kg (伊维菌素0.2 mg/kg, 阿苯达唑10 mg/kg)剂量口服,给药后0.5、1、2、3、4、6、8、12、16、24、36、48、60 h颈静脉采血5 mL,分离血清,-20 ℃保存,用高效液相色谱仪检测样品血药浓度。试验结果表明,①伊维菌素在山羊体内的代谢情况为：0.5 h,0.112151 μg/mL; 第1次达峰时间为4 h, 0.302702 μg/mL;第2次达峰时间为16 h,0.258284 μg/mL;60 h,0.011118 μg/mL。②阿苯达唑在山羊体内的代谢情况为：0.5 h, 0.049285 μg/mL;第1次达峰时间为8 h,4.95283 μg/mL ;第2次达峰时间为16 h,5.694551 μg/mL;60 h,0.06434 μg/mL。复方伊维菌素中的伊维菌素和阿苯达唑在山羊体内代谢时间短,第60小时已达到很低的血药浓度。 相似文献
3.
本文建立了用反相高效液相色谱法测定丙硫苯咪唑及其代谢物丙硫苯咪唑亚砜、丙硫苯咪唑砜的血药浓度的方法,并测定了6头健康猪口服丙硫苯咪唑(25mg/kg)后亚砜和砜的血药浓度及有关药代动力学参数。结果:给药后20min采血,6头猪血中,丙硫苯咪唑原形药均未检出,而以丙硫苯咪唑亚砜和丙硫苯咪唑砜的形式出现。以NaVa pack C18 4μm 0.39×15cm为固定相,紫外检测器波长为290nm,甲苯咪唑为内标物,测定丙硫苯咪唑亚砜和砜.本法测得血清中亚砜的最低含量为23.56ng/mL,砜为16.54ng/mL。亚砜平均回收率为93.73±6.75％,砜为90.044±5.33％,不同浓度水平测定结果的日内和日间变动系数均在10％以下。丙硫苯咪唑亚砜和砜的药代动力学符合有吸收因素二室模型,健康猪口服丙硫苯咪唑后,亚砜半衰期(t1/B)为12.6466±1.8491h;血浆清除率(CL_B)为0.1364±0.0921L/(kg·h);血药浓度达峰时间(Tmax)为10h,峰浓度(Cmax)为11.919±1.382μg/mL血清;药时曲线下面积(AUC)为1156.69±742.52μg/(mL·h)。 相似文献
4.
5.
《黑龙江畜牧兽医》2016,(24)
为了探讨小尾寒羊消化道线虫发病规律和药物防治效果,筛选驱虫效果最佳药物,试验随机选取小尾寒羊600只,分为芬苯达唑粉组、伊维菌素注射液组、阿苯达唑伊维菌素预混剂组、多拉菌素注射液组和生理盐水对照组,每组各120只。每组在试验前7天进行粪便虫卵检查,用药开始后,在每次用药的第7天分别进行粪便虫卵检查1次,在整个试验期间共检查4次。粪便虫卵检查采用饱和盐水漂浮法,计算粪便虫卵数、每克被检粪样中虫卵数量(EPG),比较每个试验组每个检查阶段的虫卵转阴率。结果表明:各组试验羊在用药7 d后虫卵转阴率由高到低依次为阿苯达唑伊维菌素预混剂组、伊维菌素注射液组、芬苯达唑粉组、多拉菌素注射液组,分别为92.5%、90.8%、90.0%和89.1%,阿苯达唑伊维菌素预混剂防治效果确实可靠,药效持续时间长,优于其他试验组。说明临床用药在防治小尾寒羊消化道线虫方面,阿苯达唑伊维菌素预混剂防治该病效果优于其他试验药物,值得推广应用。 相似文献
6.
《中国兽医杂志》2020,(6)
本文建立了同时检测猪血浆中芬苯达唑、奥芬达唑、芬苯达唑砜和伊维菌素的UPLC-MS/MS方法,该方法得到的芬苯达唑、奥芬达唑、芬苯达唑砜和伊维菌素的检测限分别为0.05μg/L、0.05μg/L、0.05μg/L和0.01μg/L,定量限分别为0.1μg/L、0.1μg/L、0.1μg/L和0.2μg/L。芬苯达唑、奥芬达唑、芬苯达唑砜和伊维菌素在猪血浆中3个不同添加浓度的回收率范围分别为89.42%～94.33%、79.05%～92.28%、86.19%～92.29%、82.09%～88.40%,线性方程分别为y=25 830.8x+18 629.1、y=11 299.7x+4 456.5、y=12 482.6x+2 319.5、y=421.76x-85.14,相关系数r都在0.999 2以上。动物试验结果显示,在给予复方芬苯达唑伊维菌素粉剂1 h后的血浆样品中检测到了4种药物。该方法符合血浆中药物的检测要求,能够用于快速测定血浆中这4种药物。 相似文献
7.
以阿苯达唑、伊维菌素为主原料，十二烷基硫酸钠为润湿剂，倍他环糊精、聚乙二醇6000为助溶剂，主原料与辅料经过混合、研磨粉碎制得阿苯达唑伊维菌素粉。配方组合为质量比M（阿苯达唑）:M（伊维菌素）:M（十二烷基硫酸钠）:M（倍他环糊精）:聚乙二醇6000=10:0.2:8:20:61.8。考察制得的阿苯达唑伊维菌素粉水中分散性良好，符合干混悬剂的沉降体积比要求，按阿苯达唑伊维菌素粉的质量标准检测为合格，低含量的伊维菌素含量均匀度符合要求，可以实现难溶性药物阿苯达唑的拌料和饮水给药。密闭保存，长期试验24个月，性状、外观几乎无改变；干燥失重由2.4%升高至2.6%；阿苯达唑含量由99.2%下降至97.3%；伊维菌素含量由100.2%下降至97.0%，含量下降不超过药物标示量百分含量的10%，符合规定。该阿苯达唑伊维菌素粉配方组成合理，工艺简单科学、操作简便，产品质量合格且稳定，有效期暂定为2年。 相似文献
8.
复方伊维菌素片含量测定方法的探讨 总被引：1，自引：1，他引：0
采用HPLC法及紫外-可见分光光度法分别测定复方伊维菌素片中伊维菌素及阿苯达唑的含量，以控制该制剂的质量。用十八烷基键合硅胶柱分离伊维菌素，以甲醇-水(85：15)为流动相，检测波长245nm；用紫外-可见分光光度法在295nm波长处测定阿苯达唑的含量。结果表明，用HPLC法测定本品中伊维菌素的含量时，伊维菌素能与阿苯达唑完全分离，平均回收率为99．56％，RSD=1．27(n=5)；用紫外-可见分光光度法测定本品中阿苯达唑的含量，伊维菌素对测定无干扰，平均回收率为99．14％，RSD=0．48(n：4)。本法简便、快速，可用于该产品的质量控制。 相似文献
9.
10.
为了建立阿苯达唑亚砜盐酸盐中有关物质的检测方法,本文采用高效液相色谱(HPLC)方法,通过系统适用性、专属性、检测限等试验,确定了阿苯达唑亚砜盐酸盐中有关物质的HPLC检测方法。色谱条件:采用C18色谱柱,流动相为乙腈-蒸馏水(40∶60),检测波长为230nm。结果显示:阿苯达唑亚砜盐酸盐在1.25～40.0μg/mL浓度范围内线性关系良好,检测限为0.032μg/mL。在此条件下阿苯达唑亚砜盐酸盐与其合成原料阿苯达唑、合成中可能产生的阿苯达唑砜、降解产物分离情况良好。 相似文献
11.
Alvarez L Lifschitz A Entrocasso C Manazza J Mottier L Borda B Virkel G Lanusse C 《Journal of veterinary pharmacology and therapeutics》2008,31(3):230-239
Mixtures of drugs from different chemical families have been proposed as a valid strategy to delay the development of anthelmintic resistance. The current work summarizes the outcome of the evaluation of the plasma disposition kinetics of albendazole (ABZ) and ivermectin (IVM) administered either alone or co-administered to lambs infected with gastrointestinal (GI) nematodes resistant to both anthelmintic molecules. Thirty six (36) Corriedale lambs naturally infected with multiple resistant GI nematodes were allocated into six treatment groups: (a) ABZ intravenous (ABZ(IV)); (b) IVM(IV); (c) ABZ(IV) + IVM(IV); (d) ABZ intraruminal (IR); (e) IVM subcutaneous (SC) and (f) ABZ(IR) + IVM(SC). Plasma samples were collected over 15 days post-treatment and analysed by HPLC. The estimated pharmacokinetic (PK) parameters were statistically compared using parametric and non-parametric statistical tests. The presence of IVM did not affect the plasma disposition kinetics of ABZ and its metabolites after the i.v. administration. However, the ABZ sulphoxide (ABZSO) area under the concentration vs. time curve (AUC) was significantly lower (P < 0.01) after the intraruminal (i.r.) administration of ABZ alone compared to that obtained for the combined treatment with IVM [subcutaneous (s.c.) injection]. The IVM plasma AUC obtained after its i.v. co-administration with ABZ was 88% higher (P < 0.05) compared to the treatment with IVM alone. Any marked difference on IVM PK parameters was observed between the treatments ABZ + IVM and IVM alone injected subcutaneously. The data obtained here indicate that the co-administration of ABZ and IVM does not induce an adverse kinetic interaction. This type of pharmacology-based evaluation of drug interactions is becoming highly relevant as drug combinations are now widely used as an alternative to control resistant helminth parasites in livestock. 相似文献
12.
Enhanced Plasma Availability of the Metabolites of Albendazole in Fasted Adult Sheep 总被引：2，自引：0，他引：2
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
13.
Uptake of albendazole and albendazole sulphoxide by Haemonchus contortus and Fasciola hepatica in sheep 总被引：1，自引：0，他引：1
The pattern of in vivo uptake of albendazole (ABZ) and its major metabolite, ABZ-sulphoxide (ABZSO), by Haemonchus contortus and Fasciola hepatica recovered from ABZ-treated sheep, was investigated. Concentration profiles of both compounds were simultaneously measured in target tissues/fluids from the same infected sheep. In addition, the proportion of the (+) and (-) ABZSO enantiomers was determined in plasma, bile and F. hepatica recovered from treated sheep. Sheep naturally infected with H. contortus were intraruminally (i.r.) treated with ABZ (micronized suspension, 7. 5mg/kg) and the plasma concentrations of ABZSO and ABZ-sulphone (ABZSO(2)) determined in addition to the concentration of ABZ and ABZSO in H. contortus, abomasal mucosa and fluid content samples. In addition, F. hepatica artificially infected sheep were treated i.r. with the same ABZ suspension (7.5mg/kg), and samples of blood, bile, liver tissue and adult flukes were collected and analysed by HPLC to determine the concentrations of ABZ and both enantiomers of ABZSO. ABZSO and ABZSO(2) were the analytes recovered in plasma with ABZ and ABZSO present in H. contortus. ABZ was the analyte recovered at the highest concentration in H. contortus and abomasal mucosa, whereas higher concentrations of ABZSO were measured in abomasal fluid content. Only low concentrations of ABZ were detected in F. hepatica and bile, but markedly higher concentrations of ABZ were measured in liver tissue. ABZSO was the main molecule recovered in F. hepatica, plasma and bile samples collected from ABZ-treated sheep. The (+) enantiomer of ABZSO was recovered at a higher proportion in plasma (75%), bile (78%) and F. hepatica (74%) after ABZ administration to infected sheep. 相似文献
14.
C. E. LANUSSE R. K. PRICHARD 《Journal of veterinary pharmacology and therapeutics》1990,13(2):170-178
The pharmacokinetics and the profile of urine excretion of netobimin (NTB) and its metabolites were investigated after its intraruminal (i.r.) and subcutaneous (s.c.) administration to sheep at 20 mg/kg. Plasma and urine concentrations of NTB, albendazole (ABZ), albendazole sulphoxide (ABZSO) and albendazole sulphone (ABZSO2) were measured serially over a 120-h period by HPLC. NTB showed a similar pharmacokinetic profile in both treatments, being detected between 0.5 and 12 h post-treatment, but the tmax was achieved significantly earlier (P less than 0.05) after s.c. treatment. ABZ was detected in plasma only after i.r. treatment, resulting in a low area under the curve (AUC). The peak plasma concentration (Cmax) and AUC for ABZSO and ABZSO2 were significantly higher after i.r. administration of NTB. In both treatments, the ABZSO Cmax was reached earlier than the ABZSO2 Cmax. The ratio of AUC ABZSO2:ABZSO was higher following s.c. administration (1.33) than following i.r. administration (0.35). The percentages of total dose excreted in the urine as NTB, ABZ, ABZSO and ABZSO2 were 17.05 (i.r.) and 8.16 (s.c.). There was a less efficient conversion of NTB into ABZ metabolites after s.c. administration. The detection of ABZ in plasma and the high ABZSO AUC obtained after i.r. treatment may be of major importance for anthelmintic efficacy. 相似文献
15.
Virkel G Lifschitz A Sallovitz J Inza G Lanusse C 《Veterinary journal (London, England : 1997)》2004,167(3):265-271
The benzimidazole (BZD) anthelmintics, netobimin (NTB) pro-drug and albendazole sulphoxide (ABZSO) are reduced to albendazole (ABZ) by ruminal microflora. The aim of the current work was to evaluate the influence of the ionophore monensin (MON) on the in vitro biotransformation of NTB and ABZSO by sheep ruminal fluid. Ruminal fluid, collected from Corriedale sheep, was preincubated (24 h) either without (control) or with known MON concentrations (0.5, 1.5 and 3.0 microg/mL) at 38 degrees C under a CO2 atmosphere. Afterwards, aliquots from both MON-pretreated and control ruminal fluid samples were incubated (30 and 60 min) with 2 microg/mL of either NTB or ABZSO. Incubated samples were chemically extracted and analysed by High Performance Liquid Chromatography to quantify the metabolites formed. The rate of ABZ production after 30 min of NTB incubation with control ruminal fluid was 0.023 microg/min. Conversely, the rates of ABZ formation were significantly (P<0.05) lower (0.009, 0.011 and 0.013 microg/min) when NTB was incubated with ruminal fluid pretreated with MON (at 0.5, 1.5 and 3.0 microg/mL, respectively). After both incubation periods, the reduction of ABZSO to ABZ was 22 to 70% lower when the ruminal fluid was preincubated with the different MON concentrations. The lower ABZ production observed in the presence of MON may result in a modified availability of this molecule in the gastrointestinal (GI) tract and hence, on its anthelmintic efficacy against GI nematodes. 相似文献
16.
Kjos SA Snowden KF Craig TM Lewis B Ronald N Olson JK 《Veterinary parasitology》2008,155(3-4):249-256
Combination of anthelmintic drugs from different chemical groups has been proposed as alternative parasite control strategies where failure of individual drugs is documented. The main goal of the current trial was to compare the clinical anthelmintic efficacy of albendazole (ABZ) and ivermectin (IVM) given either separately or co-administered to lambs naturally infected with gastrointestinal nematodes resistant to both molecules. Seventy (70) Corriedale lambs naturally infected with multiple resistant gastrointestinal nematodes were involved in the efficacy trial: the animals were allocated into 7 experimental groups (n=10) and treated with either ABZ intravenously (iv) (ABZ(IV)), IVM(IV), ABZ(IV)+IVM(IV), ABZ intraruminally (ir) (ABZ(IR)), IVM subcutaneously (sc) (IVM(SC)) and ABZ(IR)+IVM(SC) or kept as untreated controls. The indirect estimation of the efficacy of the different treatments was performed by the faecal egg count reduction test (FECRT). Additionally, four animals randomly chosen from the untreated control and ABZ(IV,) IVM(IV) and ABZ(IV)+IVM(IV) experimental groups were sacrificed 15 days post-treatment to evaluate the efficacy against different adult resistant nematode parasites. The results were statistically compared by a non-parametric ANOVA (Kruskal-Wallis test). The following egg output reduction values were obtained: 73.4% (ABZ(IV)), 79.0% (IVM(IV)), 91.9% (ABZ(IV)+IVM(IV)), 43.5% (ABZ(IR)), 79.8% (IVM(SC)) and 70.8% (ABZ(IR)+IVM(SC)). The efficacy against Haemonchus spp. was 95.1 (ABZ(IV)), 99.3 (IVM(IV)) and 99.9% (ABZ(IV)+IVM(IV)), while the efficacy against Trichostrongylus colubriformis for the same treatment groups was 79.6, 100 and 99.9%. The data obtained on the assessment of the ABZ-IVM combination indicates that no potentiation synergism is observed. This work is complementary to a parallel study that demonstrated the lack of negative pharmacokinetic interactions between the two anthelmintics acting by different mode of action. Thus, an additive effect may be achieved against nematodes resistant to both compounds. Further work is required to understand the implications of potential pharmacokinetic/pharmacodynamic interactions between anthelmintics before drug combined formulations are developed to be introduced into the pharmaceutical market. 相似文献
17.
Alvarez L Suárez G Ceballos L Moreno L Lanusse C 《Journal of veterinary pharmacology and therapeutics》2012,35(4):365-372
The gastrointestinal absorption of most drugs follows a first-order kinetics, whereby a constant fraction of the total drug is absorbed in each equal time interval. Although this related absorption principle is applicable to the most of the therapeutically used drugs, it remains unclear for poorly water-soluble compounds such as the benzimidazole anthelmintics in ruminants. The goal of the current work was to characterize the albendazole (ABZ) metabolites plasma disposition kinetics after ABZ administration at different dosages to nematode-infected lambs. Eighteen Corriedale lambs artificially infected with a resistant Haemonchus contortus strain were allocated into three groups and intraruminally treated with ABZ at either 5 (ABZ(5)), 15 (ABZ(15)) or 45 (ABZ(45)) mg/kg. Blood samples were collected up to 120 h post-treatment, and the collected plasma was analysed by high-performance liquid chromatography. The estimated pharmacokinetic parameters were statistically compared using parametric and nonparametric tests. None of the animals involved in the current trial showed any adverse events during the study. While ABZ parent drug was not recovered in the bloodstream, the area under the concentration vs time curve (AUC) of the active ABZ-sulphoxide (ABZSO) metabolite increased significantly (P<0.05) from 21.0 (ABZ(5)) up to 158.6 (ABZ(15)) and 389.7 μg·h/mL (ABZ(45)), which indicates some type of nonproportionality in the relationship between dose level and drug systemic exposure. The overall kinetic disposition of the inactive sulphone metabolite did not change after treatment at threefold the therapeutic ABZ dosage. However, significantly (P<0.05) higher AUC, C(max) and mean residence time values were observed after the administration of the highest dosage level. The higher dosages accounted for a significantly (P<0.05) enhancement of the ABZSO peak plasma concentration, which were obtained at delayed times post-treatment. High correlations between AUC(0-LOQ) and C(max) and nematode counts were observed, with Spearman's coefficients of -0.83 and -0.84, respectively. The results obtained in the current experiment show that increasing the dose of ABZ in sheep is clearly associated with enhanced plasma ABZ metabolites exposure. The data showed a nonproportionality on the gastrointestinal absorption of ABZ in nematode-infected lambs. 相似文献
18.
Pharmacokinetics of ivermectin in sheep following pretreatment with Escherichia coli endotoxin 
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下载免费PDF全文 J. Riquelme V. Cazanga J. Jeldres R. Pérez 《Journal of veterinary pharmacology and therapeutics》2018,41(5):755-759
The comparative pharmacokinetics of ivermectin (IVM), between healthy and in Escherichia coli lipopolysaccharides (LPS) injected sheep, was investigated after an intravenous (IV) administration of a single dose of 0.2 mg/kg. Ten Suffolk Down sheep, 55 ± 3.3 kg, were distributed in two experimental groups: Group 1 (LPS): treated with three doses of 1 μg LPS/kg bw at ?24, ?16, and ?0.75 hr before IVM; group 2 (Control): treated with saline solution (SS). An IV dose of 0.2 mg IVM/kg was administered 45 min after the last injection of LPS or SS. Plasma concentrations of IVM were determined by liquid chromatography. Pharmacokinetic parameters were calculated based on non‐compartmental modeling. In healthy sheep, the values of the pharmacokinetic parameters were as follows: elimination half‐life (2.85 days), mean residence time (MRT) (2.27 days), area under the plasma concentration curve over time (AUC, 117.4 ng day?1 ml?1), volume of distribution (875.6 ml/kg), and clearance (187.1 ml/day). No statistically significant differences were observed when compared with the results obtained from the group of sheep treated with LPS. It is concluded that the acute inflammatory response (AIR) induced by the intravenous administration of E. coli LPS in adult sheep produced no changes in plasma concentrations or in the pharmacokinetic behavior of IVM, when it is administered intravenously at therapeutic doses. 相似文献
19.
Pharmacokinetics of albendazole sulfoxide enantiomers administered in racemic form and separately in rats 总被引：1，自引：1，他引：0
Capece BP Castells G Godoy C Arboix M Cristòfol C 《Veterinary journal (London, England : 1997)》2008,177(2):297-299
The pharmacokinetic behaviour of albendazole sulfoxide (ABZSO) enantiomers was studied in rats after the oral administration of 10 mg/kg of rac-ABZSO, 5 mg/kg of (-)-ABZSO or 5 mg/kg of (+)-ABZSO. The disposition profiles of ABZSO enantiomers were similar in all treatments, but the calculated area under the curve for the (-)-ABZSO was higher in all cases compared with (+)-ABZSO. The results suggest that there is no chiral inversion of ABZSO enantiomers. After the administration of rac-ABZSO, 17.2% of the total dose was recovered in urine as albendazole ABZ (0.1%), albendazole sulfone ABZSO(2) (0.3%), albendazole 2-aminosulfone (ABZ-SO(2)NH(2)) (3.1%) and ABZSO (13.7%). The ratio (+) to (-) was similar in urine (1.6) and blood (1.7). 相似文献
20.
M. BISTOLETTI L. ALVAREZ C. LANUSSE L. MORENO 《Journal of veterinary pharmacology and therapeutics》2013,36(2):161-168
Bistoletti, M., Alvarez, L., Lanusse, C., Moreno, L. Disposition kinetics of albendazole and metabolites in laying hens. J. vet. Pharmacol. Therap. 36 , 161–168. An increasing prevalence of roundworm parasites in poultry, particularly in litter‐based housing systems, has been reported. However, few anthelmintic drugs are commercially available for use in avian production systems. The anthelmintic efficacy of albendazole (ABZ) in poultry has been demonstrated well. The goal of this work was to characterize the ABZ and metabolites plasma disposition kinetics after treatment with different administration routes in laying hens. Twenty‐four laying hens Plymouth Rock Barrada were distributed into three groups and treated with ABZ as follows: intravenously at 10 mg/kg (ABZ i.v.); orally at the same dose (ABZ oral); and in medicated feed at 10 mg/kg·day for 7 days (ABZ feed). Blood samples were taken up to 48 h posttreatment (ABZ i.v. and ABZ oral) and up to 10 days poststart feed medication (ABZ feed). The collected plasma samples were analyzed using high‐performance liquid chromatography. ABZ and its albendazole sulphoxide (ABZSO) and ABZSO2 metabolites were recovered in plasma after ABZ i.v. administration. ABZ parent compound showed an initial concentration of 16.4 ± 2.0 μg/mL, being rapidly metabolized into the ABZSO and ABZSO2 metabolites. The ABZSO maximum concentration (Cmax) (3.10 ± 0.78 μg/mL) was higher than that of ABZSO2Cmax (0.34 ± 0.05 μg/mL). The area under the concentration vs time curve (AUC) for ABZSO (21.9 ± 3.6 μg·h/mL) was higher than that observed for ABZSO2 and ABZ (7.80 ± 1.02 and 12.0 ± 1.6 μg·h/mL, respectively). The ABZ body clearance (Cl) was 0.88 ± 0.11 L·h/kg with an elimination half‐life (T1/2el) of 3.47 ± 0.73 h. The T1/2el for ABZSO and ABZSO2 were 6.36 ± 1.50 and 5.40 ± 1.90 h, respectively. After ABZ oral administration, low ABZ plasma concentrations were measured between 0.5 and 3 h posttreatment. ABZ was rapidly metabolized to ABZSO (Cmax, 1.71 ± 0.62 μg/mL) and ABZSO2 (Cmax, 0.43 ± 0.04 μg/mL). The metabolite systemic exposure (AUC) values were 18.6 ± 2.0 and 10.6 ± 0.9 μg·h/mL for ABZSO and ABZSO2, respectively. The half‐life values after ABZ oral were similar (5.91 ± 0.60 and 5.57 ± 1.19 h for ABZSO and ABZSO2, respectively) to those obtained after ABZ i.v. administration. ABZ was not recovered from the bloodstream after ABZ feed administration. AUC values of ABZSO and ABZSO2 were 61.9 and 92.4 μg·h/mL, respectively. The work reported here provides useful information on the pharmacokinetic behavior of ABZ after both i.v. and oral administrations in hens, which is a useful first step to evaluate its potential as an anthelmintic tool for use in poultry. 相似文献