首页> 外国专利> Long-acting parasiticidal composition with improved bioavailability comprising an avermectin or milbemycin, plus a salicylanilide amp; a polymeric species

Long-acting parasiticidal composition with improved bioavailability comprising an avermectin or milbemycin, plus a salicylanilide amp; a polymeric species

机译:具有改善的生物利用度的长效杀虫组合物,包含阿维菌素或米尔贝霉素,以及水杨酰苯胺和聚合物

摘要

An injectable composition prepared for treating animals suffering from parasites, which parasites are known to be susceptible to at least one of the avermectins, milbemycins or salicylanilides, comprises a first parasiticidal agent selected from amongst the avermectins and the milbemycins, together with another parasiticidal agent selected from the salicylanilides in an amount such that the injectable composition delivers at least about 2.5 mg salicylanilide per kilogram live weight of the animal to be treated, in a physiologically tolerable solvent system suitable for injection, and an amount of a polymeric species that is effective to improve bioavailability of the salicylanilide parasiticidal agent over a period of treatment. H preferably comprises ivermectin in an amount of from 0.1 to 10%(w/v), a solvent selected from the group consisting of glycerol formal, propylene glycol, polyethylene glycol and combinations thereof, and a salicylanilide such as closantel. The polymeric species is preferably selected from the group consisting of polyvinylpyrrolidone and polyoxypropylene/polyoxyethylene block copolymers. The polymeric species improves the bioavailability of the salicylanilide as determined by blood plasma levels.
机译:制备用于治疗患有寄生虫的动物的注射用组合物,已知该寄生虫对阿维菌素,米尔倍霉素或水杨酰苯胺中的至少一种敏感,其包含选自阿维菌素和米尔倍霉素的第一杀寄生虫剂,以及选自另一种杀寄生虫剂。在适合于注射的生理上可耐受的溶剂系统中,从水杨酰苯胺中提取的量应使可注射组合物每千克待治疗动物的活重能递送至少约2.5 mg水杨酰苯胺,以及一定量的有效在一段时间内改善了水杨基苯胺杀虫剂的生物利用度。 H优选包含0.1至10%(w / v)的伊维菌素,选自甘油缩甲醛,丙二醇,聚乙二醇及其组合的溶剂,以及水杨酰苯胺例如氯生沙坦。聚合物种类优选选自聚乙烯吡咯烷酮和聚氧化丙烯/聚氧化乙烯嵌段共聚物。如血浆水平所确定的,聚合物种类改善了水杨酰苯胺的生物利用度。

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