碘醚柳胺对大鼠胚胎毒性和致畸性

以23．0,51.8,116.4mg/kg碘醚柳胺在Wistar大鼠妊娠后7－15d口服，各剂量组吸收胎和死胎率增加，活胎率减少，但对胎鼠外观，骨骼和内脏无致畸性，高剂量组对胎鼠生长发育和孕体重增长有明显的负影响，表明碘西边柳胺对大鼠有胚胎毒性，无致畸作用，提出，在临床上怀孕动物应慎用。     

Research on Anthelmintic Effects of Rafoxanide on Six Months Old Yili Horses

This test was aimed to research the role of rafoxanide on anthelmintic effects in six months old Yili horses.Ten Yili male horses with same date of birth,body weight（117.60±15.84)kg and the horses of six months old were randomly divided into 2 groups,each group of 5 horses,control and trial groups,respectively.The horses in two groups were fed with the same nutritional levels of roughage and concentrate supplement.Horses of trial group were expelled passasite by rafoxanide,but control group had not treatment.After expelling passasite,and a 18-day feeding trials,the number of worm eggs output and species in each horses were calculated,and anthelmintic effects were evaluated.The results showed that we identified 9 species worm eggs,included Parascaris SP,Capillaria equouum,Cyathostomes,Triodontophorus tenuicollis,G. acgyptiacus,Strongyloides westeri,Dictyocaulus arnfieldi,Oxyuris equi and Paranoplace phala mamillana;on the 3rd day after expelling passasit, EPG was reached 13 500/g in fresh faeces;on the 6th day,the infection rate was 6.37%, the worm eggs reducing rate was 90.59%,the worm eggs flooding rate was 93.63%;On the 18th day, the infection rate was 13.33%,the worm eggs reducing rate was 71.91%,the worm eggs flooding rate was 86.67%.Therefore,there were more categories intestinal parasitic in six months old Yili horse in Xinjiang,rafoxanide had a good effect,and the effect of rafoxanide reduced after expelling passasite 18th day.     

碘醚柳胺脂质体定向剂在绵羊体内的药代动力学及组织残留量

应用碘醚柳胺脂质体定向剂 (包封率 58%)给绵羊单剂量皮下注射 ( 0 .3m g/ kg) ,用反相高效液相色谱法 ( RP- HPLC)测定了该药在绵羊体内不同时间的血浆药物浓度以及组织中的药物残留量。利用 3p87实用药代动力学软件分析 ,结果表明 ,该药的药代动力学符合一室模型 ,动力学方程为 :C =3.116 4( e- 0 .0 192 t- e- 1.5 15 5 t)。药代动力学参数为 :达峰时间 ( Tmax)为 ( 2 .8112± 0 .74 92 ) d,峰浓度 ( Cmax)为 ( 2 .874 2±0 .8716 ) mg/ L,生物半衰期 ( t1/2β)为 ( 36 .386 1± 3.0 385) d,曲线下面积 ( AU C)为 ( 14 3.5530± 4 7.2 354 )μg·m L- 1· d- 1。与皮下注射碘醚柳胺注射液 ( 3mg/ kg)相比 ,达峰浓度时间提前了 1.4 6 47d,半衰期延长了 16 .2 0 97d。碘醚柳胺在绵羊组织中的残留量 ,2 8d时肝脏中为 ( 2 3.0 331± 3.2 0 4 8) μg/ g。肾脏、肌肉和胆汁中一直检测不到药物。与皮下注射碘醚柳胺注射液相比 ,肝脏等富含巨噬细胞的脏器中药物含量明显增高 ,肾脏、肌肉中药物含量相对较低。本试验结果表明 ,碘醚柳胺脂质体定向剂优于碘醚柳胺注射液。     

国产碘醚柳胺在绵羊体内的药代动力学及组织残留量的研究

给绵羊单剂量口服碘醚柳胺(7.5mg/kg),用HPLC法测定不同时间的血浆药物浓度。结果,碘醚柳胺在血浆中药物代谢动力学符合开放性二室模型,动力学方程为: C_t=208.586 8e~(-0.4756(t-0.5426)) 18.760 5e~(-0.0439(t-0.5426))-227.445e~(-0.5328(t-0.5426))口服碘醚柳胺后,达峰时间(Tmax)为3.698 9±0.197 4d;峰浓度(Cmax)为18.760 5±1.564 6μg/mL;消除半衰期(T(1/2)β)为15.800 6±0.445 7d;曲线下面积(Auc)为459.000 0±62.531 3μg·d/mL。碘醚柳胺在绵羊的肝、肾、胆汁、肌肉中的残留量:停药后28d分别为0.359 9、0.243 2、0.157 9、0.100 0μg/g;停药后50d,肝脏中的残留量为0.100 0μg/g,其它组织中均检测不到;停药后60d,各组织中均无残留。     

豆磷脂替代卵磷脂制备碘醚柳胺脂质体研究

采用改良的冷冻溶融法，用豆磷脂替代卵磷脂制备了碘醚柳胺(Rafoxanide，Raf)脂质体，并对其药物特性进行了测定与观察。用此法制备出的碘醚柳胺豆磷脂脂质体包封率高达57．54％。电镜下显示碘醚柳胺脂质体以多层脂质体为主，粒径大多分布在0．1～1．0μm之间。室温条件下贮存75d后，其包封率由原来的57．54％下降到52．32％，提示用豆磷脂脂质体具有良好的稳定性。分别按0．15mg／kg，0．3mg／kg，0．6mg／kg体重剂量给肝片吸虫病患羊皮下注射碘醚柳胺脂质体，3d后剖杀，发现0．3mg／kg体重以上剂量组的患羊肝脏内的虫体全部崩解死亡。     

碘醚柳胺对6月龄伊犁马驹驱虫效果的研究

试验旨在研究碘醚柳胺对6月龄伊犁马驹驱虫的效果。选取体重（117.60±15.84）kg、出生日期相近、在同一放牧草场放牧的6月龄伊犁马公马驹10匹,随机分为两组：对照组和试验组,每组5匹。两组马驹饲喂相同营养水平的粗饲料和精料补充料。试验组马匹用碘醚柳胺混悬液驱虫剂驱虫,对照组不进行驱虫。驱虫后,进行为期18 d的饲养试验,统计各组马驹粪便中虫卵排出的种类及数量并计算驱虫效果。结果表明,6月龄马驹粪便中共鉴别出9种虫卵,包括马副蛔虫、毛圆线虫、盅口线虫、细颈三齿线虫、埃及腹盘吸虫、韦氏类圆线虫、安氏网尾线虫、马蛲虫、侏儒副裸头绦虫;碘醚柳胺驱虫后第3天每克粪便的虫卵数（EPG）达到最高（13 500个/g）;驱虫后第6天,马驹寄生虫感染率降为6.37%,虫卵减少率为90.59%,转阴率为93.63%;驱虫后第18天,感染率降为13.33%,虫卵减少率为71.91%,转阴率为86.67%。结果表明,新疆昭苏马场6月龄马驹肠道寄生虫感染的种类较多,碘醚柳胺的驱虫效果在用药后的前6 d内最明显,用药后第18天药效减弱。     

碘醚柳胺驱虫对6月龄伊犁马营养物质消化代谢及生长发育的影响

本试验旨在研究碘醚柳胺驱虫对6月龄伊犁马驹营养物质消化代谢及生长发育的影响。试验选取在同一草场饲养的6月龄(出生日期±5 d)、平均体重为(117.60±15.84)kg的伊犁马公马马驹10匹,在相同的饲喂条件下随机分为2组,分别为对照组和试验组,每组5匹。试验组马驹灌服碘醚柳胺混悬液驱虫剂驱虫,每匹14 m L,对照组马驹不进行驱虫。驱虫后,进行为期20 d的消化代谢试验,其中预试期15 d,正试期5 d。结果显示:碘醚柳胺驱虫对马驹各营养物质摄入量、消化量、排出量和消化率均没有产生显著影响(P0.05),但试验组中性洗涤纤维、酸性洗涤纤维、钙消化率分别比对照组高18.17%、16.37%、17.36%;试验组马驹氮的沉积量和沉积率分别比对照组高65.90%(P0.05)和73.20%(P0.05);试验组马驹体高和胸围的总增长分别比对照组高123.58%(P0.05)和48.31%(P0.05)。因此,碘醚柳胺驱虫对6月龄伊犁马营养物质消化代谢的积极作用主要体现在氮沉积量和沉积率的增加以及体高和胸围的增长上。     

Anthelmintic Resistance on an Organized Sheep Farm in India

Monitoring anthelmintic resistance in strongyle nematodes by the faecal egg count reduction test and a commercial larval development assay on an organized sheep farm in the semi-arid area of Rajasthan revealed the emergence of resistance to benzimidazoles and rafoxanide and a potential risk of the development of levamisole/tetramisole resistance. A benzimidazole/levamisole combination, avermectins and closantel were each found to be efficacious.