高效液相色谱法测定二甲基半胱胺截短侧耳素的研究

建立了以高效液相色谱法测定盐酸沃尼妙林关键中间体二甲基半胱胺截短侧耳素含量的检测方法。色谱条件为SepaxC18色谱柱(150×4.6mm,3μm)流动相为乙腈-磷酸缓冲液(pH2.5)(V/V= 40∶60), 流速为1ml/min,检测波长为205nm。 并对该检测方法进行了系统适用性、线性、精密度、重现性稳定性、检测限、定量限以及回收率的考察,结果均良好,可以用于盐酸沃尼妙林关键中间体的含量检测。     

The efficacy of valnemulin (Econor) in the control of disease caused by experimental infection of calves with Mycoplasma bovis

Mycoplasma bovis infection was experimentally induced in groups of six young calves. A further group was uninfected and served as a control. Ten days after infection, medication with either enrofloxacin (Baytril, Bayer) or valnemulin (Econor, Novartis) was instituted via the milk replacer for a further 10 days, after which all calves were killed. Infection resulted in depression, pyrexia, inappetance and prominent respiratory signs. Arthritis occurred in two animals and two (unmedicated) animals died. At post-mortem examination extensive lesions were present in the lungs and M. bovis was re-isolated from infected unmedicated calves' lungs. Medication with either enrofloxacin or valnemulin resulted in a rapid diminution of clinical signs, restoration of appetite and reversal of weight loss. Isolation of Pasteurella multocida from the calves' lungs was suppressed by both medicaments. Valnemulin resulted in a more rapid reduction of clinical scores and eliminated M. bovis from the lungs more effectively than enrofloxacin.     

新兽药盐酸沃尼妙林的合成

以精制的截短侧耳素为原料,经对甲苯磺酰氯磺化后,与二甲基半胱胺盐酸盐反应,制得截短侧耳素半胱胺取代物;另外由D-缬氨酸、乙酰乙酸甲酯和氢氧化钾反应制得（ R）-2-（1-甲氧羰基-2-烯丙基）氨基-3-甲基丁酸钾,经氯甲酸乙酯活化后与截短侧耳素半胱胺取代物反应,最后通过调节pH值,经反相萃取后,冻干得盐酸沃尼妙林,总收率为69％,所得产品按照EP6．0进行了质量检测,产品具有含量高、杂质少等优点。     

新药沃尼妙林的研究进展

沃尼妙林（Valnemulin）是以截短侧耳素为原料半合成的新一代抗生素,与泰妙菌素为同一类药物,其抗菌活性强,抗菌谱广,尤其对支原体和螺旋体有很强的活性。本文对沃尼妙林的作用机制、药效学、药动学、毒理学以及在临床上的应用方面的研究进展进行了综述。     

盐酸沃尼妙林应用于家禽的研究进展

从药效学、药动学、毒理学等多个方面对盐酸沃尼妙林在家禽上的应用及国内外主要研究进展进行对比概述,分析了盐酸沃尼妙林对于家禽的安全性、有效性等情况,以期为临床用药提供参考。     

Effect of zinc chelate and valnemulin for the treatment of swine dysentery in an experimental challenge study

The aim of study was to determine the influence of zinc chelate, valnemulin and it’s combination on Brachyspira hyodysenteriae shedding and morphological changes of colonic mucosa in an experimental model of swine dysentery (SD). The study was performed on pigs coming from a dysentery-free herd. Animals were inoculated by B. hyodysenteriae strain B204. When the clinical signs of SD and B. hyodysenteriae shedding developed, the pigs were divided into four treatment groups. The first group was treated with zinc chelate (250 ml/1000 L in water), second group was given valnemulin in feed at 75 ppm; the third group was given a combination of both and the fourth group was control. The results demonstrated therapeutic effect of valnemulin in pigs with serious SD and did not show therapeutic effect of chelated zinc.