盐酸阿苯达哩亚砜化学结构分析

建立了药物盐酸阿苯达唑亚砜的化学结构确证方法.通过高效液相色谱(HPLC)测定盐酸阿苯达唑亚砜纯度,采用紫外光谱(UV)、红外光谱(IR)、核磁共振(NMR)以及质谱(MS)等分析方法对盐酸阿苯达唑亚砜样品进行了结构测定.结果确证盐酸阿苯达唑亚砜的结构为[5-(丙亚砜基)-1H-苯并咪唑-2-基]氨基甲酸甲醋盐酸.本方法测定结果准确全面,为盐酸阿苯达唑亚砜的生产和鉴定提供了较为全面的参考数据.     

盐酸阿苯达哩亚砜化学结构分析

建立了药物盐酸阿苯达唑亚砜的化学结构确证方法.通过高效液相色谱(HPLC)测定盐酸阿苯达唑亚砜纯度,采用紫外光谱(UV)、红外光谱(IR)、核磁共振(NMR)以及质谱(MS)等分析方法对盐酸阿苯达唑亚砜样品进行了结构测定.结果确证盐酸阿苯达唑亚砜的结构为[5-(丙亚砜基)-1H-苯并咪唑-2-基]氨基甲酸甲醋盐酸.本方...     

阿苯达唑亚砜盐酸盐有关物质的HPLC检测

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。     

牛肉中阿苯达唑及其代谢产物残留的检测

阿苯达唑是一种广谱抗蠕虫药,但是由于用药不当等原因,其在动物可食性组织中的残留可能刺激神经系统及消化系统、触发过敏反应甚至出现肝功能异常。本试验基于5μg/kg的检验限建立牛肉中的阿苯达唑及其代谢产物的检测方法——高效液相色谱法。样品中残留的阿苯达唑及其主要代谢产物阿苯达唑砜和阿苯达唑亚砜,经乙醚提取,乙腈和己烷萃取,由高效液相色谱（配紫外检测器）测定得到阿苯达唑及其亚砜与砜的平均回收率分别为71.8%～88.6%、78.1%～85.6%和83.1%～91.9%,变异系数分别为2.8%～9.2%、0.9%～4.9%和1.4%～4.8%。     

盐酸阿苯达唑亚砜对照品候选物纯度检测方法的建立

以盐酸阿苯达唑亚砜原料为基础,通过反复提纯,得到盐酸阿苯达唑亚砜对照品候选物,该候选物经过熔点,薄层色谱法（TLC）和高效液相色谱法检测,初步确认符合对照品的要求,经过高效液相色谱检测,采用面积归一化法计算其纯度不小于99.5%。该方法的建立为盐酸阿苯达唑对照品进一步研究提供了帮助。     

超声波法制备阿苯达唑包合物工艺研究

采用超声波法制备阿苯达唑-β-环糊精包合物,用正交设计法筛选最佳工艺,经相溶解度图研究、熔点测定、紫外光谱分析及溶解度测定等对包合物的形成进行检验。包合反应最佳条件为:阿苯达唑与β-环糊精(β-CD)与比率为1∶2,超声时间40 min,β-CD水溶液浓度8%,此工艺条件下包合物性质稳定,重现性好。结果证明,采用超声波法可制备阿苯达唑-β-环糊精包合物,方法简便,工艺稳定,并可明显改善阿苯达唑水溶性。     

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

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。     

高效液相色谱法测定动物肌肉中的阿苯达唑及其代谢物

建立了动物肌肉组织中阿苯达唑及其代谢物阿苯达唑亚砜、阿苯达唑砜的多残留检测的高效液相色谱法。用乙酸乙酯提取肌肉组织样品中的药物,提取液浓缩后加入酸性乙醇和正己烷分配脱脂,过watersHLB固相萃取柱净化。以水-乙腈-甲酸为流动相,反相高效液相色谱紫外检测法检测。方法的平均回收率为86．4％,平均变异系数为1．96％。3种药物的检测限均为5μg／kg,定量限均为20μg／kg。     

五氯柳胺阿苯达唑复方混悬液的制备及其含量测定

为制备五氯柳胺阿苯达唑复方混悬液,对其质量评价并建立含量测定方法。通过辅料相容性、单因素筛选及回归正交设计,以沉降体积比、再分散性等为考察因素,优化处方制备五氯柳胺阿苯达唑复方混悬液,用激光粒度测定仪、透射电子显微镜,对其粒径和形态进行测定,考察制剂的稳定性,建立测定五氯柳胺阿苯达唑复方混悬液含量的高效液相色谱方法。结果显示,五氯柳胺阿苯达唑复方混悬液每100 mL中含五氯柳胺4.00 g,阿苯达唑4.00 g,黄蓍树胶0.25 g,十二烷基硫酸钠0.20 g,甘油3.00 mL,柠檬酸钠1.20 g,苯甲酸0.15 g。混悬液沉降体积比为0.99,再分散性良好。1～100 mg/L的五氯柳胺、阿苯达唑与峰面积呈良好的线性关系(R~2=0.999 9,R~2=0.999 7),平均回收率为101.15%和100.89%,RSD为0.13%和0.10%(n=9)。结果表明,制备的五氯柳胺阿苯达唑复方混悬液工艺简单,性状良好,稳定性和分散性好,质量可控。所建立的高效液相色谱法快速简便、准确可靠,可用于复方混悬液中五氯柳胺、阿苯达唑含量的测定。     

阜康市羊消化道线虫驱虫药物筛选

目的:通过试验为阜康市筛选出科学合理的、针对性强的、安全高效的驱虫药物。方法:采用随机对照实验比较阿苯达唑+虫克星与单用阿苯达唑驱虫效果。结果:阿苯达唑+虫克星与单用阿苯达唑驱虫效果之间差异具有统计学意义。结论:"一次驱虫,两次投药"的驱虫方案联合阿苯达唑+虫克星驱虫效果明显优于单用阿苯达唑驱虫效果,从而为阜康市制定合理有效的羊驱虫方案提供可靠的科学依据,以达到提高羊生产性能和经济效益的目的。     

复方伊维菌素乳液在山羊体内的药代动力学研究

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。     

丙硫苯咪唑一次性驱除猪蛔虫效果观察

针对目前驱虫药物种类虽多，但普遍因毒副作用大、成本高而在实际生产应用中不易普及。为了证实毒副作用小，成本低的丙硫苯咪唑的理论效果，我们在实行计划免疫的地区随机选取4个村寨对双月龄以上的健康猪只进行一次性投药驱虫观察，结果平均虫卵减少率达90．9％，虫卵转阴率达86．5％，效果十分明显，为今后应用该药普及农村生猪驱虫保健找到了实践依据。     

不同剂量阿苯达唑治疗鼠旋毛虫病效果初探

使用不同剂量阿苯达唑对人工感染旋毛虫的小白鼠进行疗效试验,观察其不同剂量的杀虫效果.结果表明：应用阿苯达唑20 mg/（kg·d）×7治疗鼠旋毛虫病有很好的治疗效果,为阿苯达唑临床应用提供科学参考.     

Efficacy of two formulations of albendazole against liver flukes in cattle.

Albendazole (10 mg/kg of body weight) was administered as a drench suspension or as a feed additive to 24 cattle with naturally acquired infections of Fasciola hepatica and Fascioloides magna. Cattle were euthanatized 16 to 30 days after treatment, and the number of viable flukes was counted. Viable F hepatica and F magna were decreased by 91.4% and 70.6% for drench administration and by 82.9% and 71.9% for the feed additive treatment, respectively. There was no significant difference between the efficacy of the 2 formulations in decreasing viable fluke numbers, compared with untreated controls.     

阿维菌素复方缓释制剂在绵羊寄生虫病防治中的应用

选择伊维菌素-丙硫咪唑复方片剂、伊维菌素-丙硫咪唑亚砜注射液和阿维菌素-丙硫咪唑亚砜复方长效油胶,对新疆阿克苏一群未进行驱虫和药浴的当年生羔羊进行试验。结果表明,复方片剂、伊维菌素-丙硫咪唑亚砜注射剂和阿维菌素-丙硫咪唑亚砜长效油胶在用药以后7 d就可以100%地杀灭发病绵羊的多种体内外寄生虫,第25天绵羊痒螨病的临床症状均已缓解或消除,并开始生长新毛。用药后40 d复方片剂组就出现了再感染现象,而阿维菌素-丙硫咪唑亚砜长效油胶组,维持100 d左右才出现肠道线虫感染,感染率为80%,但感染强度只是复方片剂组的10%,对绵羊疥癣可基本控制。     

The transport of albendazole and albendazole sulphoxide in the lancet fluke (Dicrocoelium dendriticum)

Albendazole (ABZ) is one of the most important benzimidazole compounds possessing high activity against the lancet fluke, Dicrocoelium dendriticum. ABZ sulphoxide (ABZ.SO) is the main molecule present in the bloodstream of an ABZ-treated host. The aim of this study was to characterise the pattern of ex vivo uptake of ABZ and ABZ.SO by lancet flukes and the export of both anthelmintics from these parasites. Transport of these anthelmintics in both living and dead flukes was compared. The adult flukes were collected from mouflons (Ovis musimon) which had been infected naturally. Results showed that more lipophilic ABZ was imported to a higher extent than ABZ.SO, and that significantly higher concentrations of ABZ were detected within living flukes as compared to dead ones. The same pattern was revealed in the study of ABZ and ABZ.SO export from the flukes' bodies. In addition to passive diffusion, active ABZ uptake and active efflux of ABZ and ABZ.SO in D. dendriticum could be assumed.     

Efficacy of tiamulin as a growth promotant for growing swine

A study involving 244 pigs initially averaging 13 kg was conducted at two stations to evaluate tiamulin as a growth promotant for growing swine. In each experiment, four replicate pens of five (Exp. 1) or six (Exp. 2) pigs/pen were used to evaluate each treatment. In Exp. 1, pigs were fed 0, 11, 22 or 44 ppm tiamulin from 15 to 58 kg, then fed a nonmedicated control diet for the remainder of the experiment (to 95 kg). In Exp. 2, pigs were fed 0, 2.75, 5.5, 11 or 22 ppm tiamulin from 11 to 56 kg, followed by the nonmedicated control diet (to 95 kg). In each experiment, carbadox (55 ppm) was included as a positive control and was fed to an average weight of 35 kg, followed by the control diet. Averaged across all dietary levels, tiamulin resulted in a 14.1% improvement in gain and a 5.7% improvement in feed:gain ratio during the first 28 to 35 d of the experiment (to 30 kg). These improvements were slightly less than those resulting from the feeding of carbadox during the same period (21.5 and 6.9%, respectively). From 13 to 57 kg, pigs fed tiamulin gained 11.6% faster and 3.1% more efficiently than did controls. Over the entire experiment (13 to 95 kg), tiamulin-fed pigs gained 5.7% faster than did controls, even though the tiamulin was withdrawn at 57 kg body weight. Growth rate from 13 to 57 kg plateaued at the 11-ppm dietary level of tiamulin; whereas, feed:gain ratio plateaued at the 22-ppm level. The results indicate that tiamulin is an effective growth promotant for growing swine.     

Effect of apparent ileal digestible lysine to energy ratio on performance of finishing pigs at different dietary metabolizable energy levels

A study with a total of 96 crossbred barrows and gilts fed ad libitum in a body weight range of 56-110 kg was carried out in order to investigate whether the optimum ratio of apparent ileal digestible lysine : energy (ME) depends on the energy density of the diet. Dietary treatments were ratios of 0.34, 0.42, 0.50 and 0.58 g digestible lysine/MJ ME either at an energy density of 13 or 14 MJ ME. Body weight gain as well as feed and ME conversion rate were improved when lysine : ME ratio increased from 0.34 to 0.50, whereby all parameters showed a significant ratio x sex interaction. Feed intake and feed conversion rate were higher at a dietary energy density of 13 MJ ME than at an energy density of 14 MJ ME but energy density did not influence daily growth rate, ME intake and ME conversion rate. Fat area above eye muscle and meat : fat ratio were lower and eye muscle area and lean percentage were higher at a ratio of 0.42 compared with a ratio of 0.34. Daily feed intake, body weight gain, feed conversion rate and parameters of fatness were higher in barrows than in gilts. Conversely, gilts had higher eye muscle area and lean percentage. Optimum ratio for body weight gain, feed and ME conversion rate calculated by exponential regression analysis were 0.42-0.43 in barrows. In gilts, feed and ME conversion rate were optimized at a ratio of 0.53 and 0.54. Because growth showed a linear response to increasing digestible lysine : ME ratios, optimum ratio for daily gain in gilts is considered to be at least 0.58.