首页> 外国专利> MICRO- AND NANOSTRUCTURED PHARMACEUTICAL AND VETERINARY COMPOSITIONS, CONTAINING BENZNIDAZOLE AND DERIVATIVES THEREOF, WHICH FORM MICRO- AND NANOSTRUCTURES IN THE GASTROINTESTINAL TRACT, AND BIOLOGICAL USES THEREOF

MICRO- AND NANOSTRUCTURED PHARMACEUTICAL AND VETERINARY COMPOSITIONS, CONTAINING BENZNIDAZOLE AND DERIVATIVES THEREOF, WHICH FORM MICRO- AND NANOSTRUCTURES IN THE GASTROINTESTINAL TRACT, AND BIOLOGICAL USES THEREOF

机译:包含苯并吲哚及其衍生物的微结构和纳米结构的药物和兽药成分,在胃肠道中形成的微结构和纳米结构,及其生物用途

摘要

The present invention describes methods for preparing micro- and nano-scale polymeric pharmaceutical forms encapsulating benznidazole for parenteral administration, and pharmaceutical forms for oral administration, which self-emulsify in contact with biological fluids, forming micro- or nanoemulsions. Microcapsules, microspheres, microemulsions, nanocapsules, nanospheres, nanoemulsions, solid, semi-solid and liquid lipid nanoparticles, lipid-core nanocapsules and self-emulsifying systems, which form micro- and nanoemulsions, are included. The formulations sought to be patented include pharmaceutical forms having a structure of emulsified globules, optionally coated with polymers, containing a benznidazole and/or nitroimidazole derivative. The pharmaceutical compositions developed improve the dissolution profile of benznidazole, control drug release and increase plasmatic bioavailability, with a consequent improvement in pharmacological activity.
机译:本发明描述了制备用于肠胃外给药的封装苯并硝唑的微米和纳米级聚合物药物形式的方法,以及用于口服给药的药物形式,其与生物流体接触而自乳化,形成微米或纳米乳液。包括形成微乳液和纳米乳液的微胶囊,微球,微乳液,纳米胶囊,纳米球,纳米乳液,固体,半固体和液体脂质纳米颗粒,脂质核心纳米胶囊和自乳化系统。寻求获得专利的制剂包括具有乳化小球结构的药物形式,可任选地用聚合物包衣,该聚合物含有苯并硝唑和/或硝基咪唑衍生物。开发的药物组合物改善了苯并硝唑的溶出度,控制了药物的释放并提高了血浆的生物利用度,从而改善了药理活性。

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