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    COLLOIDAL NANOSCALE CARRIERS FOR ACTIVE HYDROPHILIC SUBSTANCES AND METHOD FOR PRODUCING SAME
    9.
    发明公开
    COLLOIDAL NANOSCALE CARRIERS FOR ACTIVE HYDROPHILIC SUBSTANCES AND METHOD FOR PRODUCING SAME 审中-公开
    胶体纳米级CARRIER用于生产活性亲水性物质和方法

    公开(公告)号：EP2583671A1

    公开(公告)日：2013-04-24

    申请号：EP11794970.1

    申请日：2011-06-14

    申请人： Instituto de Pesquisas Tecnologicas do Estado de São Paulo S.A. IPT ,  Universidade De São Paulo-USP ,  Fundação de Amparo à Pesquisa do Estado de São Paulo - FAPESP

    发明人： NETO PEREIRA CERIZE, Natália ,  MARIM DE OLIVEIRA, Adriano ,  RÉ, Maria Inês ,  TEDESCO, Antônio Cláudio

    IPC分类号： A61K9/107 ,  A61K47/36 ,  A61K47/34 ,  A61K47/38 ,  A61K47/32

    CPC分类号： A61K9/107 ,  A61K47/32 ,  A61K47/34 ,  A61K47/36

    摘要： The invention "colloidal nanoscale carriers for active hydrophilic substances and method for producing same" pertains to the field of medical, odontological or hygiene preparations, and is characterized by structures formed by hydrophilic polymers that contain active hydrophilic substances coated with a non-hydrophilic phase and surfactants with affinity for the components, forming an invert emulsion that allows the incorporation and controlled delivery of active hydrophilic substances, conferring properties such as protection against degradation processes, improvement of compatibility with the other components of the formulation in the final product, increase in the availability and/or bioavailability of the active substance in the medium of interest (including improvements in permeation processes in biological materials, reduction of the exposure and volatilization of the active substance in the medium) and controlled release of the active substance(s). The nanoscale carrier obtained by this method, called colloidal nanoscale carrier (NC), can be used in various fields, such as the pharmaceutical field (including dermatology), cosmetics, personal hygiene products, veterinary medicine, agrochemicals and fertilizers, the food industry and the like. The invention proposes a kinetically stable system with an effective nanoscale structure that consists of nanoscale carriers formed by polymers emulsified in a non-aqueous medium in the presence of a surfactant with affinity for the two phases (the dispersion medium and the encapsulating agent). This system is obtained by nanoemulsification of an aqueous phase of hydrophilic polymers emulsified in a non-hydrophilic (lipophilic or silophilic) phase that contains the surfactants, and is characterized by the implementation of two concepts that encompass the generation of an invert nanoscale emulsion and of polymer nanoparticles. The formulation has the novel technical effect of providing a polymer excipient with a nanoscale structure for delivering hydrophilic molecules suspended in a non-hydrophilic phase, which allows controlling the size of the nanoscale particles and modulating colloidal stability by means of process parameters.

    摘要翻译： 本发明的“胶态纳米级载体为活性的亲水性物质及其制造方法”涉及医疗，齿科或卫生制剂领域，并且通过由亲水性聚合物形成的结构为特征的并包含涂覆有一种非亲水相活性的亲水性物质和 与部件亲和力表面活性剂，反相乳液的形成并允许掺入和的活性亲水性物质受控输送，赋予属性：例如对降解过程，改善在最终产品中的制剂中的其它组分的相容性的保护，在增加 可用性和/或在感兴趣（包括在渗透过程中的改进的生物材料，减少了活性物质在培养基中的曝光和挥发的）和活性物质（S）的控制释放的介质中的活性物质的生物利用度。 通过这种方法获得的纳米载体，被称为胶体纳米载体（NC），可在各种领域，：如制药领域（包括皮肤科），化妆品，个人护理用品，兽药，农药和化肥，食品工业和使用 等。 本发明提出了与有效的纳米级结构的动力学稳定的系统做了通过在表面活性剂的存在下与用于两个相的亲和性（分散介质和封装剂）在非水介质中乳化的聚合物纳米FORMED载波的besteht。 该系统由在非亲水性（亲脂性或silophilic）相中乳化做亲水性聚合物的水相中的纳米乳化获得包含表面活性剂，并且通过两个概念的实施特点也包括反相纳米乳液和的产生 聚合物纳米颗粒。 制剂具有提供聚合物赋形剂与纳米级结构用于输送悬浮在非亲水相，这允许控制所述纳米颗粒的尺寸和通过的过程参数的装置调制的胶体稳定性的亲水性分子的新的技术效果。