伊维菌素微球在家兔体内的药动学

皮下注射伊维菌素 (IVM )微球悬液 (5 0mg/kg及 10 0mg/kg)和害获灭 (1%伊维菌素 ,0 5mg/kg) ,RP HPLC UV法定量 ,研究了IVM在家兔体内的药物动力学。害获灭皮下注射给药 ,药 时数据符合一级吸收一室开放模型 ,主要动力学参数为 :t1/2ka=7 2 4± 2 96h ;t1/2ke=36 38± 8 6 6h ;tmax=2 1 4 6± 4 82h ;Cmax=2 2 53± 2 32ng/ml;AUC =174 9± 318ng/1.h ,其动力学参数表现比较明显的个体差异 ,且与其它动物有明显差别。微球皮下注射一周后 ,血药浓度呈较稳定状态 ,到第 4 2天 (高剂量组 )和第 32天 (低剂量组 ) ,血浆中测不出H2 B1a(低于 2 5ng/ml)。以房室模型拟合 ,微球高低剂量组均符合有吸收二室开放模型 ,主要药动学参数均表现显著的个体差异。  

伊维菌素浇泼剂对牦牛皮蝇蛆病的防治效果及安全性试验

应用0.5％伊维菌素浇泼剂，10月中下旬每头牛100kg体重分别按1ml、2ml用量，沿背中线皮肤一次浇泼给药，翌年3月、5月份检查防治效果。结果：感染率、感染强度由对照组牛的86．2％和5．24(0—24)个虫体(瘤疱)，均下降为0，有效率达100％；按0．1ml/kg bw、0．15ml/kg bw、0．2ml/kg bw剂量给药牦牛均可耐受。试验证明：伊维菌素浇泼剂防治牦牛皮蝇蛆病效果好，用量小，给药方便，毒副作用小，安全范围大，适宜各地推广。  

牛肝中阿维菌素类药物残留的高效液相色谱荧光检测方法的研究

采用高效液相色谱分离,荧光检测器检测,建立了固相萃取分析牛组织中埃普利诺菌素、阿维菌素、多拉菌素和伊维菌素残留的方法.样品用乙腈提取,碱性氧化铝和C18SPE柱净化,用乙酸酐和1-甲基咪唑的乙腈溶液作衍生化试剂,在96℃条件下,完全衍生化需要100min.4种药物的平均回收率为70.02%～88.75%,日内变异系数小于8.52%,日间变异系数小于7.13%.埃普利诺菌素、阿维菌素、多拉菌素和伊维菌素的检出限为0.4～0.5μg/kg,定量限为2ug/kg.该方法可靠、灵敏,可用于常规残留分析.  

家畜伊维菌素中毒的研究

作者综述了伊维菌素的杀虫及中毒机理，临床应用的安全性及犬、猫、羊、兔、牛的中毒剂量、临床症状、病理变化、预防、治疗措施，并说明了阿维菌素、伊维菌素和多拉菌素的应用。认为家畜中毒的原因是超量使用该药物；除敏感犬种外，伊维菌素是当前防治畜禽寄生虫病的最佳药物之一，同时指出对发生中毒和过敏的动物，早期发现，治疗得当，则治愈率高。  

高效液相色谱法测定伊维菌素脂质体药物的含量及包封率

本试验旨在建立伊维菌素脂质体载体药物含量及包封率测定的高效液相色谱法。Waters surfire C18柱(150 mm×2.1 mm，5 μm)，流动相为乙腈—甲醇—水(62∶30∶8)，流速1 mL/min，检测波长245 nm，进样量10 μL，柱温30 ℃。采用凝胶过滤法、透析法、冷冻超速离心法、超滤离心法4种方法对脂质体与药物进行分离。结果表明，在优化色谱条件下伊维菌素与辅料及溶剂峰均得到良好分离，伊维菌素在1～50 μg/mL浓度范围内线性关系良好(r=0.9998，n=5)，最终采用超速冷冻离心法可将脂质体与药物很好的分离，伊维菌素脂质载体的包封率可达98.54%±1.6%。该方法准确可靠、简单快速，可用于伊维菌素脂质体载体药物含量及包封率的测定。  

HPLC法测定微乳中伊维菌素的含量

建立了HPLC测定伊维菌素微乳中伊维菌素含量的方法。色谱柱为ZirchromC18(4.6mm×250 mm,5μm),流动相为甲醇∶水(85∶15),测定波长为245 nm,流速为1.0 mL/min,柱温为40℃。伊维菌素与辅料及溶剂峰分离良好,在2.22~111.0μg/mL时线性关系良好(R2=0.999 9)。HPLC测定伊维菌素方法便捷、准确、重复性好,可用于伊维菌素微乳含量的测定。  

Treatment protocols for demodicosis: an evidence-based review

Publications discussing the treatment of demodicosis in the dog and cat are reviewed. Based on the evidence in the literature, amitraz rinses at 0.025-0.06% every 7-14 days, and oral daily ivermectin at 300 micro g kg(-1), milbemycin at 2 mg kg(-1) and moxidectin at 400 micro g kg(-1), respectively, can all be recommended for the treatment of generalized canine demodicosis. Ivermectin and moxidectin should be initiated at lower doses and patients monitored for possible adverse effects during therapy. In cats, 2% lime sulfur dips and amitraz rinses at 0.0125-0.025% have been used successfully.  

伊维菌素脂质体的制备及质量控制研究

为研究伊维菌素脂质体 ,以卵磷脂和胆固醇为载体 ,采用注入法制备了伊维菌素脂质体 ,并应用紫外倍率系数法测定脂质体中伊维菌素的含量 ,采用高速离心法测定其包封率。结果表明 ,采用注入法制备的伊维菌素脂质体稳定性好 ,大小均匀 ,包封率效果良好 (77.42 %以上 ) ,紫外倍率系数法能消除辅料干扰 ,可作为伊维菌素脂质体质量控制的有效方法  

伊维菌素驱除香猪体内外寄生虫的试验

应用进口伊维菌素对刚从贵州引进的20头香猪进行了驱虫试验,以400μgkg体重剂量皮下注射,两周后重复一次,驱虫后8天粪中线虫虫卵转阴率为94.74%,虫卵减少率为100%;驱虫后4周体表血虱及其虫卵全部转阴。  

The distribution and some pharmacokinetic parameters of ivermectin in pigs

Ivermectin was injected subcutaneously into five pigs at the usual dose rate of 300 µg/kg and found to distribute well to all tissues and body fluids which were sampled 24 h post-injection. Ivermectin was detected in the contents and mucus at all levels of the gastrointestinal tract. The drug was excreted in bile, with high concentrations of the drug in the intestines and faeces. High concentrations of ivermectin were measured in skin, ears and ear wax, suggesting that the drug should be effective in the treatment of ectoparasitic infestations, particularly ear mites. The high lipid solubility of the drug may explain the high concentrations found in ear wax and skin. Ivermectin was also detected in the body fluids and tissues of an untreated pig penned with the treated animals. Direct contact appeared to be necessary for transfer of ivermectin from the treated to the untreated pig but coprophagia or urine drinking is a possible explanation.The pharmacokinetics of ivermectin administered subcutaneously at a dose rate of 300 µg/kg to six pigs were studied. There was marked individual variation in the pharmacokinetics of ivermectin. In one pig the area under the plasma concentration-time curve was particularly high. This may reflect individual variation in uptake and excretion of the drug. The mean elimination half-life of the drug was 35.2 h, suggesting that the drug is cleared slowly from pigs with drug detectable in plasma for 6–10 days. This persistence should allow a short period of protection before re-infection with parasites.