多拉菌素注射剂杀灭猪血虱试验

选购自然感染猪血虱的仔猪80头,根据猪血虱感染数量随机分为5组,分别肌肉注射多拉菌素400、300、200 μg/kg体重,皮下注射伊维菌素300 μg/kg体重,肌肉注射生理盐水0.5 mL/头.结果显示,各试验组药物对猪血虱都有明显的驱杀作用,其中多拉菌素高、中剂量组药物残效期达120 d以上.临床推荐剂量为300 μg/kg体重.     

Pharmacokinetics of subcutaneously administered doramectin in alpacas

The objective of this research was to evaluate comparative pharmacokinetics of doramectin in alpacas, after subcutaneous administration of 0.2 mg/kg dose. Six healthy adult alpacas, mean age of 5 years ± 1, (three female and three gelded males) of mean bodyweight of 62 kg ± 16 kg with an average body condition scored 2.8 ± 1 out of five, were used in this study. Serial blood samples were collected from the jugular vein before the administration until day 21 afterwards to establish the pharmacokinetics of doramectin after its subcutaneous administration at 0.2 mg/kg dose. The blood samples were analysed using high-performance liquid chromatography (HPLC), fluorescence detection method with precolumn derivatisation, validated for alpacas. The pharmacokinetic parameters were calculated using a noncompartmental model, and results showed Cmax (6.05 ± 5.34 ng/ml), Tmax (3.83 ± 2.48 days), AUC (62.12 ± 18.86 ng/ml × d), terminal half-life (6.2 ± 4.9 days) and MRT (11.56 ± 4.43 days). The results of this study showed that the Cmax and AUC were much lower than in cattle and sheep at the same dosage. Tmax remained similar to cattle and sheep. This study presents valuable information about pharmacokinetics of doramectin in alpacas, which can be utilised in its future efficacy studies.     

多拉菌素在猪体内的药代动力学

对多拉菌素在猪体内进行为期45d的药代动力学研究。长白×杜洛克杂交猪10头,临床健康,驱净寄生虫,体重36～50kg,以300μg/kg体重剂量分别通过静脉和肌肉注射给药。动物给药后在不同时间内分点经颈静脉采血。血浆样品用乙腈沉淀处理,上清液过C18富集柱,用甲醇提取多拉菌素并进行衍生化反应,以反向HPLC测定猪血清中的药物浓度。药代动力学参数用计算机程序MCPKP进行处理。结果表明,动物经静脉和肌肉注射给药后,血浆药物浓度分别可测至30d和25d,2种途径的药物浓度时间曲线均符合二室开放模型。主要药代动力学参数为:静脉注射T1/2α(1.092±0.66)d,T1/2β(6.11±2.73)d,AUC(274.19±119.89)μg/(L·d);肌肉注射T1/2α(0.056±0.022)d,T1/2β(3.20±1.34)d,AUC(223.51±65.20)μg/(L·d),CMAX(28.99±10.69)μg/L,Tp(1.24±0.87)d。多拉菌素肌肉注射的生物利用度为81.5%。结果显示多拉菌素在猪体内具有吸收分布较迅速、体内分布容积大、消除缓慢和生物利用度相对较高的特点,提示多拉菌素在猪体内作用的长效性主要由该化合物的自身特性所决定,而与给药途径和使用的溶剂关系不大,研究结果对指导临床正确用药具有重要意义。     

多拉菌素5%乳油防治甘蓝小菜蛾田间药效试验

多拉菌素5%乳油防治甘蓝小菜蛾,按推荐剂量5~15mL/667m2试验,结果表明,对1~3龄幼虫效果较明显,最佳施药时期为小菜蛾1~3龄期。防治效果最高可达95.22%。     

犬血浆中塞拉菌素含量的高效液相色谱-荧光检测方法的建立

本研究以多拉菌素为内标,建立了犬血浆中塞拉菌素的高效液相色谱-荧光检测方法.用乙腈作为血浆蛋白沉淀剂,用SampliQ C18型SPE固相萃取柱进行净化,用1-甲基咪唑和三氟乙酸酐衍生化处理.色谱条件为ODS-1色谱柱(250 mm×4.6 mm),流动相为甲醇∶乙腈∶1％1-庚烷磺酸∶0.4％乙酸=40.0∶57.6∶0.9 ∶ 1.5(v/v/v/v),流速1mL·min-,进样量20μL,激发波长355 nm,发射波长465 nm,柱温30℃.方法的检测限为0.25 ng·mL-1,线性范围0.5～50.0 ng·mL-,变异系数为1.47 ％～3.31％,方法的样品平均回收率为94.0％.结果表明,所建方法准确、灵敏度高和重复性好,可用于犬体内塞拉菌素血药含量的测定.     

多拉菌素的研究进展

作为新一代的优良抗寄生虫药,多拉菌素具有安全、广谱、高效、长效和奶中残留低等特点。文章阐述了多拉菌素的作用机制、药代动力学、抗虫谱与毒理学、药物制剂方面的研究进展。     

多拉菌素的研究进展及应用

多拉菌素是新一代大环内酯类抗寄生虫药,具有安全、广谱、高效、长效和奶中残留低等特点,文章从多拉菌素的药物制剂、药代动力学、药物残留检测、毒理学及其对机体免疫力的影响以及在临床兽医中的应用等几个方面进行了阐述,为临床合理用药提供可靠的指导。     

The effects of early-season treatments with doramectin on set-stocked calves naturally exposed to trichostrongyles

A study was carried out to evaluate the effects of strategic early-season treatments with doramectin on first-season grazing calves exposed to trichostronglylid infection on a naturally contaminated pasture. Two groups of cross-bred Limousine/Red Danish calves were turned out in early May on two plots that were similar with respect to size and herbage infectivity. They grazed separately until housing in early October. One of these groups was given doramectin at turnout and 10 weeks later, while the other group served as untreated controls. The results showed that the treatments significantly reduced trichostrongylid loads throughout the season, as evidenced by significant reductions in both their Ostertagia ostertagi burdens and serum pepsinogen levels compared with the controls. Furthermore, the results of herbage larval counts and post-mortem worm counts in tracer animals demonstrated that the treatment had successfully suppressed herbage infectivity on the treated plot.     

多拉菌素在犬体内药代动力学研究

 采用RP-HPLC法荧光监测器测定单剂量皮下注射多拉菌素［300μg/（kg BW）］）后，犬体内不同时间点的血浆药物浓度。血浆药物浓度-时间数据采用3P97药动软件分析。结果表明，本试验条件下血浆中药物添加浓度在0.1～100 ng/mL范围内与峰面积呈良好线性关系，检测限为0.5 ng/mL。不同浓度水平的日内日间变异系数分别小于3%和4%，各浓度的平均回收率均大于90%。给药后血药浓度－时间数据符合一级吸收一室开放模型，主要药物动力学参数为：t_1/2ka为（0.58±0.13）d，t_1/2β为（4.78±0.31）d，T_max为（2.00±0.29）d，C_max为（20.29±2.04）ng/mL，AUC为（187.43±24.99）（ng·d）/mL。提示多拉菌素在犬体内血药浓度维持的时间长，消除缓慢，且根据其半衰期判断，多拉菌素属于慢性消除药物。     

Sarcoptes scabiei infestation of a donkey in the UK

Sarcoptes scabiei infestation was identified as the cause of pruritic dermatitis in a donkey in the UK. Treatment with i.m. doramectin and topical selenium sulphide was successful in eliminating clinical signs. Foxes were identified as the possible source of infestation. Sarcoptic mange should be considered as a potential differential diagnosis for pruritic dermatitis in equids in the UK.