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1.
联合应用阿苯达唑和伊维菌素在线虫感染鄂尔多斯细毛羊体内的药动学研究 总被引：1，自引：0，他引：1
为阐明联合应用阿苯达唑(ABZ)和伊维菌素(IVM)在胃肠道线虫感染鄂尔多斯细毛羊体内的药动学互作关系,以感染胃肠道线虫的鄂尔多斯细毛羊为研究对象,比较研究了单独或联合应用阿苯达唑和伊维菌素后的药物动力学特征。通过粪便虫卵检查法,选取感染胃肠道线虫的鄂尔多斯细毛羊15只,随机分成3组,每组5只。第1组口服给予阿苯达唑(15mg/kg),第2组皮下注射伊维菌素(0.2mg/kg),第3组皮下注射伊维菌素(0.2mg/kg)的同时口服阿苯达唑(15mg/kg)。于给药后不同时间,由颈静脉采集血样,分离血浆,并用高效液相色谱法测定各时间点血浆阿苯达唑、阿苯达唑亚砜、阿苯达唑砜和伊维菌素浓度,并用PK Solution 2.0药物动力学软件计算出各药动学参数。结果表明,联合用药组绵羊血浆伊维菌素峰浓度(Cmax)、药时曲线下面积(AUC)和平均滞留时间(MRT)分别为44.80ng/mL±6.12ng/mL、5 007.46ng.h/mL±1 301.42ng.h/mL和85.47h±5.03h,均显著(P<0.05)小于单独用药组的对应参数值67.62ng/mL±9.06ng/mL、7 125.08ng.h/mL±908.52ng.h/mL和113.39h±9.00h。口服阿苯达唑组绵羊血浆中仅检测到了阿苯达唑砜和阿苯达唑亚砜,而未检测到阿苯达唑母药。联合用药后,除阿苯达唑砜的达峰时间(T max)显著推迟外,阿苯达唑砜和阿苯达唑亚砜的其他各参数之间均无显著性差异。因此,联合应用IVM和ABZ可影响它们在胃肠道线虫感染鄂尔多斯细毛羊体内的药动学特征,且对伊维菌素药动学特征的影响尤为明显,在临床联合用药过程中应予以重视。 相似文献
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《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
3.
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
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为比较研究制备的伊维菌素长效透皮制剂与普通伊维菌素注射剂药物代谢及药效时间,本研究制备伊维菌素含量分别为0.5%、1.0%和1.5%的长效透皮制剂,采用高效液相色谱法检测不同药量相同体积伊维菌素长效透皮制剂和普通伊维菌素注射剂（1.0%）在家兔体内的药代动力学,并通过PKSolver药代动力学处理软件对数据进行分析。结果显示,0.5%、1.0%、1.5%伊维菌素长效透皮剂和1.0%普通注射剂吸收半衰期分别为0.81、0.52、1.02和0.12 d;达峰时间为1.55、0.97、1.62和0.42 d;峰浓度为47.36、72.02、115.30和99.53 ng/mL;消除半衰期为3.61、5.92、5.59和1.79 d;平均滞留时间为5.27、7.37、5.13和2.16 d;药时曲线面积为1 488.70、3 081.98、3 161.20和480.00 ng·d/mL,伊维菌素长效透皮剂体内维持有效药物浓度的时间长达35 d,普通注射剂仅为9 d。结果表明,伊维菌素长效透皮剂效果稳定,可进行更深入的研究。 相似文献
6.
《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
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《中国畜牧兽医》2020,(1)
为比较研究制备的伊维菌素长效透皮制剂与普通伊维菌素注射剂药物代谢及药效时间,本研究制备伊维菌素含量分别为0.5%、1.0%和1.5%的长效透皮制剂,采用高效液相色谱法检测不同药量相同体积伊维菌素长效透皮制剂和普通伊维菌素注射剂(1.0%)在家兔体内的药代动力学,并通过PKSolver药代动力学处理软件对数据进行分析。结果显示,0.5%、1.0%、1.5%伊维菌素长效透皮剂和1.0%普通注射剂吸收半衰期分别为0.81、0.52、1.02和0.12 d;达峰时间为1.55、0.97、1.62和0.42 d;峰浓度为47.36、72.02、115.30和99.53 ng/mL;消除半衰期为3.61、5.92、5.59和1.79 d;平均滞留时间为5.27、7.37、5.13和2.16 d;药时曲线面积为1 488.70、3 081.98、3 161.20和480.00 ng·d/mL,伊维菌素长效透皮剂体内维持有效药物浓度的时间长达35 d,普通注射剂仅为9 d。结果表明,伊维菌素长效透皮剂效果稳定,可进行更深入的研究。 相似文献
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《中国畜牧兽医文摘》2016,(7)
为了研究几种药物的驱虫效果以及药物对山羊生产的影响,分别对阿苯达唑50mg/kg;依维菌素注射液0.2 mg/kg;吡喹酮片50 mg/kg;以上三种药物进行驱虫试验。实验结果表明:驱虫羊的增重速度显著高于不驱虫羊;从增重效果来看,以阿苯达为最佳,驱虫效果最佳的是伊维菌素,因此,建议龙里县选择阿苯达+伊维菌素驱虫药物组合进行大面积推广。 相似文献
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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
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Doré E Angelos JA Rowe JD Carlson JL Wetzlich SE Kieu HT Tell LA 《Journal of veterinary pharmacology and therapeutics》2011,34(1):25-30
Doré, E., Angelos, J. A., Rowe, J. D., Carlson, J. L., Wetzlich, S. E., Kieu, H. T., Tell, L. A. Pharmacokinetics of ceftiofur crystalline free acid after single subcutaneous administration in lactating and nonlactating domestic goats (Capra aegagrus hircus). J. vet. Pharmacol. Therap. 34 , 25–30. Six nonlactating and six lactating adult female goats received a single subcutaneous injection of ceftiofur crystalline free acid (CCFA) at a dosage of 6.6 mg/kg. Blood samples were collected from the jugular vein before and at multiple time points after CCFA administration. Milk samples were collected twice daily. Concentrations of ceftiofur and desfuroylceftiofur‐related metabolites were measured using high‐performance liquid chromatography. Data were analyzed using compartmental and noncompartmental approaches. The pharmacokinetics of CCFA in the domestic goat was best described by a one compartment model. Mean (±SD) pharmacokinetic parameters were as follows for the nonlactating goats: area under the concentration time curve0–∞ (159 h·μg/mL ± 19), maximum observed serum concentration (2.3 μg/mL ± 1.1), time of maximal observed serum concentration (26.7 h ± 16.5) and terminal elimination half life (36.9 h; harmonic). For the lactating goats, the pharmacokinetic parameters were as follows: area under the concentration time curve0–∞ (156 h·μg/mL ± 14), maximum observed serum concentration (1.5 μg/mL ± 0.4), time of maximal observed serum concentration (46 h ± 15.9) and terminal elimination half life (37.3 h; harmonic). Ceftiofur and desfuroylceftiofur‐related metabolites were only detectable in one milk sample at 36 h following treatment. There were no significant differences in the pharmacokinetic parameter between the nonlactating and lactating goats. 相似文献
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This case report describes the treatment of demodicosis (Demodex caprae) in 2 goats. The entire body surface of both goats was scattered with lens-large nodes from which pasty secretion emptied itself during palpation. One goat was administered 0.67 mg/kg Ivermectin orally once weekly for 12 weeks, the other goat was treated with 0.5 mg/kg Eprinomectin pour-on. The treatment led to an entire healing without any scar formation or depigmentations of the skin. 相似文献
13.
本试验旨在探讨加丽素红中角黄素在鸡体内的药代动力学特征.选取19周龄的海兰蛋鸡12只,单次灌胃口服加丽素红9.6 mg/kg BW,在72 h内不同时间段分10次采集静脉血,用高效液相色谱法测定鸡血清中角黄素的质量浓度,并利用3P97药代动力学程序软件处理血药浓度-时间数据.结果如下:加丽素红经口服给药后,角黄素在鸡体内的血药浓度-时间数据符合一级吸收一室模型,其理论方程为C=0.471(e-0.036-e-0.190),主要药代动力学参数为:吸收半衰期t1/2(Ka)=(3.643±0.205)h,消除半衰期t1/2(Ke)=(19.263±1.312)h,达峰时间Tmax=(10.795±1.007)h,达峰浓度Cmax=(0.259±0.048)μg/mL,血药浓度-时间曲线下面积AUC=(10.607±1.029)μg/(mL·h),总体清除率CLB=(0.905±0.076)L/(kg·h),表观分布容积Vd=(2.515±0.133)L/kg.上述结果表明,角黄素在鸡体内血药浓度的变化表征了加丽素红在鸡体内代谢的变化规律,具有吸收分布较迅速、达峰快、体内分布广泛、消除速度较慢等特点. 相似文献
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Olsén L Ingvast-Larsson C Bondesson U Broström H Tjälve H Larsson P 《Journal of veterinary pharmacology and therapeutics》2007,30(3):194-200
The pharmacokinetics of the histamine H(1)-antagonist cetirizine and the effects of pretreatment with the antiparasitic macrocyclic lactone ivermectin on the pharmacokinetics of cetirizine were studied in horses. After oral administration of cetirizine at 0.2 mg/kg bw, the mean terminal half-life was 3.4 h (range 2.9-3.7 h) and the maximal plasma concentration 132 ng/mL (101-196 ng/mL). The time to reach maximal plasma concentration was 0.7 h (0.5-0.8 h). Ivermectin (0.2 mg/kg bw) given orally 1.5 h before cetirizine did not affect its pharmacokinetics. However, ivermectin pretreatment 12 h before cetirizine increased the area under the plasma concentration-time curve by 60%. The maximal plasma concentration, terminal half-life and mean residence time also increased significantly following the 12 h pretreatment. Ivermectin is an inhibitor of P-glycoprotein, which is a major drug efflux transporter in cellular membranes at various sites. The elevated plasma levels of cetirizine following the pretreatment with ivermectin may mainly be due to decreased renal secretion, related to inhibition of the P-glycoprotein in the proximal tubular cells of the kidney. The pharmacokinetic properties of cetirizine have characteristics which are suitable for an antihistamine, and this substance may be a useful drug in horses. 相似文献
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Rao GS Ramesh S Ahmad AH Tripathi HC Sharma LD Malik JK 《Journal of veterinary pharmacology and therapeutics》2000,23(6):365-372
Pharmacokinetics of enrofloxacin and its active metabolite ciprofloxacin were investigated in normal, febrile and probenecid‐treated adult goats after single intravenous (i.v.) administration of enrofloxacin (5 mg/kg). Pharmacokinetic evaluation of the plasma concentration–time data of enrofloxacin and ciprofloxacin was performed using two‐ and one‐compartment open models, respectively. Plasma enrofloxacin concentrations were significantly higher in febrile (0.75–7 h) and probenecid‐treated (5–7 h) goats than in normal goats. The sum of enrofloxacin and ciprofloxacin concentrations in plasma ≥0.1 μg/mL was maintained up to 7 and 8 h in normal and febrile or probenecid‐treated goats, respectively. The t1/2β, AUC, MRT and ClB of enrofloxacin in normal animals were determined to be 1.14 h, 6.71 μg.h/mL, 1.5 h and 807 mL/h/kg, respectively. The fraction of enrofloxacin metabolized to ciprofloxacin was 28.8%. The Cmax., t1/2β, AUC and MRT of ciprofloxacin in normal goats were 0.45 μg/mL, 1.79 h, 1.84 μg.h/mL and 3.34 h, respectively. As compared with normal goats, the values of t1/2β (1.83 h), AUC (11.68 μg ? h/mL) and MRT (2.13 h) of enrofloxacin were significantly higher, whereas its ClB (430 mL/h/kg) and metabolite conversion to ciprofloxacin (8.5%) were lower in febrile goats. The Cmax. (0.18 μg/mL) and AUC (0.99 μg.h/mL) of ciprofloxacin were significantly decreased, whereas its t1/2β (2.75 h) and MRT (4.58 h) were prolonged in febrile than in normal goats. Concomitant administration of probenecid (40 mg/kg, i.v.) with enrofloxacin did not significantly alter any of the pharmacokinetic variables of either enrofloxacin or ciprofloxacin in goats. 相似文献
16.
González A Sahagun AM Diez MJ Fernandez N Sierra M Garcia JJ 《American journal of veterinary research》2006,67(2):323-328
OBJECTIVE: To evaluate the pharmacokinetics of a novel commercial formulation of ivermectin after administration to goats. ANIMALS: 6 healthy adult goats. PROCEDURE: Ivermectin (200 microg/kg) was initially administered IV to each goat, and plasma samples were obtained for 36 days. After a washout period of 3 weeks, each goat received a novel commercial formulation of ivermectin (200 microg/kg) by SC injection. Plasma samples were then obtained for 42 days. Drug concentrations were quantified by use of high-performance liquid chromatography with fluorescence detection. RESULTS: Pharmacokinetics of ivermectin after IV administration were best described by a 2-compartment open model; values for main compartmental variables included volume of distribution at a steady state (9.94 L/kg), clearance (1.54 L/kg/d), and area under the plasma concentration-time curve (AUC; 143 [ng x d]/mL). Values for the noncompartmental variables included mean residence time (7.37 days), AUC (153 [ng x d]/mL), and clearance (1.43 L/kg/d). After SC administration, noncompartmental pharmacokinetic analysis was conducted. Values of the variables calculated by use of this method included maximum plasma concentration (Cmax; 21.8 ng/mL), time to reach Cmax (3 days), and bioavailability (F; 91.8%). CONCLUSIONS AND CLINICAL RELEVANCE: The commercial formulation used in this study is a good option to consider when administering ivermectin to goats because of the high absorption, which is characterized by high values of F. In addition, the values of Cmax and time to reach Cmax are higher than those reported by other investigators who used other routes of administration. 相似文献
17.
Bauer C 《DTW. Deutsche tier?rztliche Wochenschrift》2001,108(2):49-50
Anthelmintic resistance of nematodes to benzimidazoles and ivermectin was suspected from field observations in an Angora goat herd in northern Hesse. Larvae of the caprine trichostrongyle isolate were used for artificial infections of helminth-naive sheep. Groups of the lambs were treated with albendazole (3.8 mg/kg p.o.) or ivermectin (0.2 mg/kg s.c.) four weeks after infection or remained untreated as controls and were necropsied one week later. Albendazole reduced the mean faecal egg counts by 82% and the mean worm counts of Haemonchus contortus by 22%, Ostertagia circumcincta by 10% and Trichostrongylus colubriformis by 41% as compared with the controls. Ivermectin was 100% effective. This is the first report from Germany of multispecific resistance to benzimidazoles in a trichostrongyle population of goats. 相似文献
18.
The disposition of spiramycin and lincomycin was measured after intravenous (i.v.) and oral (p.o.) administration to pigs. Twelve healthy pigs (six for each compound) weighing 16–43 kg received a dose of 10 mg/kg intravenously, and 55 mg/kg (spiramycin) or 33 mg/kg (lincomycin) orally in both a fasted and a fed condition in a three-way cross-over design. Spiramycin was detectable in plasma up to 30 h after intravenous and oral administration to both fasted and fed pigs, whereas lincomycin was detected for only 12 h after intravenous administration and up to 15 h after oral administration. The volume of distribution was 5.6 ± 1.5 and 1.1 ± 0.2 L/kg body weight for spiramycin and lincomycin, respectively. For both compounds the bioavailability was strongly dependent on the presence of food in the gastrointestinal tract. For spiramycin the bioavailability was determined to be 60% and 24% in fasted and fed pigs, respectively, whereas the corresponding figures for lincomycin were 73% and 41%. The maximum plasma concentration of spiramycin (Cmax) was estimated to be 5 μg/mL in fasted pigs and 1 μg/mL only in fed pigs. It is concluded that an oral dose of 55 mg/kg body weight is not enough to give a therapeutically effective plasma concentration of spiramycin against species of Mycoplasma, Streptoccocus, Staphylococcus and Pasteurella multocida. The maximum plasma concentration of lincomycin was estimated to be 8 μg/mL in fasted pigs and 5 μg/mL in fed pigs, but as the minimum inhibitory concentration for lincomycin against Actinobacillus pleuropneumoniae and P. multocida is higher than 32 μg/mL a therapeutically effective plasma concentration could not be obtained following oral administration of the drug. For Mycoplasma the MIC90 is below 1 μg/mL and a therapeutically effective plasma concentration of lincomycin was thus obtained after oral administration to both fed and fasted pigs. 相似文献
19.
The tissue concentration and efficacy of ivermectin after per os and subcutaneous administration were compared in goats experimentally infected with Trichostrongylus colubriformis (ivermectin-susceptible strain, INRA). Infected goats (n = 24) were treated per os (n = 9) or subcutaneously (n = 9) with ivermectin, 0.2 mg/kg, or kept as not treated controls. The faecal egg counts and small intestine worm counts were determined. Ivermectin concentration was measured in the plasma, gastrointestinal tract, lung, skin or hair, liver and adipose tissues at 0, 2, 7 and 17 days post-treatment. The efficacy of ivermectin against T. colubriformis infection in goat was 98.7 and 99.9% for subcutaneous and oral administration, respectively. Ivermectin concentration declined with time and only residual concentration was measured at 17 days post-treatment in plasma and gastrointestinal tract. Ivermectin concentration was higher after subcutaneous compared to per os injection in most of the tissue examined. In skin, hair and subcutaneous adipose tissue ivermectin persisted at significant concentrations 17 days post-treatment for both routes of administration. In our experimental conditions, ivermectin provides similar efficacy against T. colubriformis after subcutaneous or per os administration in goat. However, the lower ivermectin levels in tissues after per os administration suggest that the lasting of efficacy may be shortened after per os compared to subcutaneous administration especially in animals with poor body condition in pasture where re-infection occurs quickly after anthelmintic treatment. 相似文献
20.
四川凉山州羊寄生虫调查及防治研究 总被引：3，自引：0，他引：3
作者用完全蠕虫解剖法检查绵羊 5 2只 ,山羊 92只 ,收集虫体 1 2 8万多条 ,虫体经分类鉴定共 92种 ,隶属 7纲、31科、48属 ;优势虫种 1 6个 ;一只羊最多混合感染 38种寄生虫 ,最大荷虫量 1 4 2 76 8条。经防治试验认为 ,用啤酒瓶稀释 ,按每千克体重一次口服丙咪唑 (Albcndazole) 5毫克对羊寄生蠕虫有良好驱治作用 ,用螨净 (Neocidol)按 1∶1 0 0 0浓度药浴 ,对驱治羊体表寄生虫也有很好疗效 相似文献