首页> 外国专利> Injectable veterinary compositions formed by the association of sulfoxides derivatives of benzimidazole or a salt, acid or basic with lactones macrocu00ecclicas indicated for the treatment of parasites inteRnos and external cattle, sheep, pigs and goats.

Injectable veterinary compositions formed by the association of sulfoxides derivatives of benzimidazole or a salt, acid or basic with lactones macrocu00ecclicas indicated for the treatment of parasites inteRnos and external cattle, sheep, pigs and goats.

机译:由苯并咪唑的亚砜衍生物或盐,酸或碱与内酯的结合形成的可注射兽医用组合物,可用于治疗内寄生虫和外部牛,羊,猪和山羊的寄生虫。

摘要

"Injectable veterinary compositions formed by the association of sulfoxides derivatives of benzimidazoles or a salt, acid or basic with lactones macrocu00ecclicas indicated for the treatment of parasites intErnos and external of bovine, ovine and caprine animals, suu00ecnos ".The present invention relates new injectable veterinary pharmaceutical compositions formed by the combination of compounds of the a type MV the sulfoxides derivatives of benzimidazoles (Figure 1) Co.M composed of a b MV suckles member is represented by: lvermectin, abamectinas avermectin, doramectin, moxidectin,Milbemycin derivatives of such compounds and composition; this injectable veterinary may be presented in the following forms: 1, an injectable solution in which both the active compoundS a A and B MV, are dissolved in a solvent (s) in the formulation.II - an injectable suspension in which one of the active ingredients compounds of the a type A or B MV is dissolved in a solvent (s) that make up the formulation and the other active principle compounds of the a Type A or B MV is in suspension coated or not. III - an injectable suspension in which both active compounds of the a A and B MV are in suspension.IV - an injectable solution tank whose preparation is to make at the time of application, by the addition of solution of one of the active ingredients compounds of the a a MV ,Solution this prepared previously or prepared at the time of its implementation on the solution of other active ingredient compounds of the a b MV in solvent (s) appropriate (s).V - an injectable emulsion tank whose preparation is to make at the time of your application.Formed by the addition of solution of one of the active ingredients compounds of the a type MV dissolved in a solvent or mixture of solvents on the solution of the appropriate other active ingredient compoundS a b MV dissolved in a solvent or mixture of solvents emuisu00e3o if appropriate; the way in which the solvent in the solution of compounds of type a are not miscible with MV.The solvent in the solution of compounds of type B.I saw an emulsion tank whose preparation is carried out at the time of your application; the solution of compounds of type a MV is prepared at the time by the addition of the solvent (s) on a salt (u00e1ciOf or alkaline) of a compound of the a MV type or addition of solutions of acids or alkalis on the compounds of the type powder or suspension in the solvent (s) appropriate (s); then this solution REC.But prepared is mixed with a solution of compounds of a b MV.The emulsion is formed by the solvent in the solution of compounds of type a MV are not miscible with the solvent of the solution of compounds of a b MV; and VII - an EMULsu00e3o injectable preparation tank which is made at the time of its implementation.Initially we have a mixture formed by the suspension of the a type compounds to MV in solvents immiscible with the solvent dissolving the compounds are a b MV.When the application is added to the mixture described above.A solution of an acid or a base dissolved in water, and is stirred to obtain a stable emulsion or microemulsion formed by solution of compounds of type a MV with the solution of the comp.The a ostos type B MV ; the structure of compounds of type a MV is the following: (Figure 1) where R ^ 1 ^ is a chain alkyl or phenyl alkyl and R ^ 2 ^ is an alkyl chain lengths.As well as their salts, acid or basic, used in several injectable formulations to increase the solubility of sulfoxides derivatives of a strains; as an example we have sulfu00f3xidThe of albendazole, where R ^ 1 ^ is propyl and R ^ 2 - methyl, oxfendazole where R ^ 1 ^ is phenyl, and R ^ 2 ^ methyl; and salts derived from these examples we have, the cioridrato of albendazole sulphoxide.The methane of albendazole sulphoxide, the sodium salt of albendazole sulphoxide, the potassium salt of albendazoi sulfoxide and etc; for the structure.And characterization of compounds of type a b MV can refer to the technical and commercial literature widely available: for avermectin, ivermectin and abamectin.Reference may be made, for example, to work a ivermectin and abamectin MV, 1989 by M. h. Fischer and H. mrozik, William C. Campbell ed. Springer Verlag or Albers schu00f7nberg et al.(1981) a avermectins structure deternlination MV. J. am. Chem. SOC. 103: 4216 - 4221; for doramectin can consult especially a veterinary parasitology MV Vol.49 n 0 1, July 1993: 5 - 15; for the milbemycin, we can refer to, among others, the Davies H. G. et al. 1986, a avermectins and milbemvcins MV ; NAT. Prod. Rep.3: 87 - 121, mrozik h et al., 1983, a synthesis of milbemycins from avermectins MV , a tetrahedron lett MV.24: 5333 - 5336, like us - - 4 134 973; the resulting solutions can be administered to cattle, sheep,Pigs and goats infected with parasites and internal or external in a single dose; the concentration of the active principles varies from 2.5% to 15% to the sulfoxide derivatives of benzimidazoles (compounds of the type A) and 0.4% to 1.5% of the macrocu00ecclicas lactones (compounds of type (b) in the final composition of the specialty of veterinary pharmaceuticals; pharmaceutical composition for use is also provided; the dose of active principlesFor body weight is the following: - for the sulfoxides derivatives of benzimidazoles (compounds of a type MV ) varies from 1.5 mg per kilogram of body weight 6,0 mg per kilogram of body weight.For the macrocu00ecclicas lactones (compounds of a b MV) varies from 0.1 mg per kilogram of body weight to 0.4 mg per kilogram of body weight.
机译:“由苯并咪唑的亚砜衍生物或盐,酸或碱与内酯形成的可注射兽医用组合物,可用于治疗内寄生虫以及牛,绵羊和山羊动物体内的寄生虫。”本发明涉及由苯并咪唑的亚砜衍生物(图1)由 b 乳头组成的Co.M的化合物的组合形成的新的注射用兽用药物组合物,其表示为:依维菌素,阿维菌素,阿维菌素,多拉菌素,莫昔克丁,米尔倍霉素衍生物等化合物和组成;该注射用兽药可以以下列形式存在:1,一种注射剂溶液,其中活性化合物S A和B A和B 的两种活性化合物均处于悬浮状态。IV-一种可注射的溶液罐,其制备应在使用时通过添加以下一种溶液制成(a)a 的活性成分化合物,此溶液事先制备或在其实施时在其他 b> 型活性成分之一的溶液而形成适当的其他活性成分化合物S b 的溶液中的溶剂溶解在溶剂或适当的溶剂混合物中; B型化合物的溶液中的溶剂不能与MV混溶的方式。我看到了一个乳液罐,在您应用时已经进行了制备;通过在 b> 类型的化合物的溶液中的溶剂形成的,与 b> 型化合物悬浮于 b> 型化合物溶液形成的稳定乳液或微乳液 ostos类型B ;类型 的化合物的结构如下:(图1)其中R ^ 1 ^是链状烷基或苯基烷基,R ^ 2 ^是烷基链长,以及它们的盐,酸碱性或碱性,用于几种注射制剂中,以增加菌株亚砜衍生物的溶解度;例如,我们有阿苯达唑的硫磺,其中R ^ 1 ^是丙基,R ^ 2-甲基,奥芬达唑,其中R ^ 1 ^是苯基​​,R ^ 2 ^甲基;从这些例子中得到的盐是阿苯达唑亚砜的cioridrato。阿苯达唑亚砜的甲烷,阿苯达唑亚砜的钠盐,阿苯达唑亚砜的钾盐等; b 类型的化合物的表征和表征可参考广泛使用的技术和商业文献:阿维菌素,伊维菌素和阿维菌素,例如可以参考 b伊维菌素和阿维菌素阿维菌素结构脱位兽医寄生虫学第49卷<0> 1993年7月1日:5-15;关于milbemycin,我们可以参考,Davies H. G.等。 1986,阿维菌素和milbemvcins ; NAT。产品Rep.3:87-121,mrozik h等人,1983,由阿维菌素四面体lett 的化合物)为每公斤1.5 mg体重6,0 mg / kg体重。对于大内酯( b>

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