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    Self-precipitating pharmaceutical formulations for the moified release of an active principle
    1.
    发明申请
    Self-precipitating pharmaceutical formulations for the moified release of an active principle 失效
    用于释放活性成分的自沉淀药物制剂

    公开(公告)号：US20090011028A1

    公开(公告)日：2009-01-08

    申请号：US12149541

    申请日：2008-05-05

    申请人： Frederic Checot ,  Cecile Bonnet-Gonnet ,  You-Ping Chan ,  Olivier Breyne ,  Remi Meyrueix

    发明人： Frederic Checot ,  Cecile Bonnet-Gonnet ,  You-Ping Chan ,  Olivier Breyne ,  Remi Meyrueix

    IPC分类号： A61K47/42 ,  A61K9/10 ,  A61K38/20

    CPC分类号： A61K9/0019 ,  A61K9/10 ,  A61K9/1641 ,  A61K38/02 ,  A61K47/645 ,  A61K48/00

    摘要： The present invention relates to novel pharmaceutical formulations for the release of an active principle (AP) over a sustained period of time of several days, or even several weeks.The invention relates, in a first aspect, to a liquid formulation comprising at least one active principle (AP) and an aqueous suspension based on colloïdal particles of a polymer (PO), wherein said formulation satisfies the following four conditions:(a) the polymer (PO) is a polyamino acid comprising glutamic residues, wherein some glutamic residues each carry a pendant cationic group (CG), said cationic groups being identical or different from one another, and other glutamic residues each carry a pendent hydrophobic group (GH), said hydrophobic groups (GH) being identical or different from one another, (b) the pHf value of the pH of said formulation is between 3.0 and 6.5; (c) at the pHf value, the polymer (PO) forms a colloïdal solution which associates spontaneously and noncovalently with the active principle (AP); (d) 1 ml of said formulation precipitates during mixing with a volume of 1 ml of a test buffer solution Tp. The invention also relates to a process for the preparation of such formulations and to a process for the preparation of medicaments including such formulations.

    摘要翻译： 本发明涉及用于在持续的几天甚至几周的时间内释放活性成分（AP）的新型药物制剂。 本发明在第一方面涉及包含至少一种活性成分（AP）和基于聚合物（PO）的胶体颗粒的水性悬浮液的液体制剂，其中所述制剂满足以下四个条件：（a） 聚合物（PO）是包含谷氨酸残基的聚氨基酸，其中一些谷氨酸残基各自携带阳离子基团（CG），所述阳离子基团彼此相同或不同，并且其它谷氨酸残基各自携带悬垂疏水基团（GH） ，所述疏水基团（GH）彼此相同或不同，（b）所述制剂的pH值的pHf值为3.0至6.5; （c）在pHf值下，聚合物（PO）形成一种自发和非共价结合活性成分（AP）的胶体溶液; （d）1ml所述制剂在与1ml测试缓冲溶液Tp的体积混合期间沉淀。 本发明还涉及一种制备这些制剂的方法以及制备包括这些制剂的药物的方法。

    Modified-release particles of polyelectrolytes and pharmaceutical formulations thereof
    2.
    发明申请
    Modified-release particles of polyelectrolytes and pharmaceutical formulations thereof 失效
    聚电解质的改性释放颗粒及其药物制剂

    公开(公告)号：US20090011039A1

    公开(公告)日：2009-01-08

    申请号：US12149552

    申请日：2008-05-05

    申请人： Cecile Bonnet-Gonnet ,  Frederic Checot ,  You-Ping Chan ,  Olivier Breyne

    发明人： Cecile Bonnet-Gonnet ,  Frederic Checot ,  You-Ping Chan ,  Olivier Breyne

    IPC分类号： A61K47/30 ,  A61K9/14

    CPC分类号： A61K9/5146 ,  A61K9/1641

    摘要： The present invention relates to novel particles comprising polyelectrolyte polymers which are transporters of active principle (AP), in particular protein and peptide active principle, and to novel modified-release pharmaceutical formulations comprising said AP microparticles.These novel particles loaded with AP release the AP over a prolonged period of time of several days, or even several weeks.The invention relates, in a first aspect, to particles comprising: a) a first polyelectrolyte polymer (PE1) in a charged state, carrying side hydrophobic groups (GH), wherein said first polyelectrolyte polymer (PE1) can spontaneously form, in water, a colloidal solution of particles at least one pHm value of the pH of between 3 and 8; b) a second polyelectrolyte polymer (PE2) of opposite polarity to the first polyelectrolyte polymer (PE1), wherein said second polyelectrolyte polymer (PE2) forms, in water, a solution or a colloidal solution at said pHm value of the pH; and c) at least one active principle (AP) associated noncovalently with the particles of the colloidal solution of the first polyelectrolyte polymer (PE1); wherein said particles are obtained by mixing, at a pH equal to pHm, the first polyelectrolyte polymer (PE1), in the form of a colloidal solution of particles associated with the active principle (AP), with the second polyelectrolyte polymer (PE2), in the form of a solution or colloidal solution. The invention also relates to the process for the preparation of these particles, to a pharmaceutical formulation comprising such particles and to a process for the preparation of medicaments.

    摘要翻译： 本发明涉及包含聚电解质聚合物的新型颗粒，其为活性成分（AP）的转运体，特别是蛋白质和肽活性成分，以及包含所述AP微粒的新型改性释放药物制剂。 装载AP的这些新型颗粒在几天甚至几周的较长时间内释放AP。 本发明在第一方面涉及包含以下的颗粒：a）带电状态的第一聚电解质聚合物（PE1），其携带侧疏水基团（GH），其中所述第一聚电解质聚合物（PE1）可在水中自发形成， 颗粒的胶体溶液，其pH值在3至8之间的至少一个pHm值; b）与第一聚电解质聚合物（PE1）相反极性的第二聚电解质聚合物（PE2），其中所述第二聚电解质聚合物（PE2）在水中以所述pHm的pH值在水中形成溶液或胶体溶液; 和c）与第一聚电解质聚合物（PE1）的胶体溶液的颗粒非共价结合的至少一种活性成分（AP）; 其中所述颗粒是通过在等于pHm的pH下，以与活性成分（AP）相关的颗粒的胶态溶液与第二聚电解质聚合物（PE2）的形式混合第一聚电解质聚合物（PE1）而获得的， 以溶液或胶体溶液的形式存在。 本发明还涉及制备这些颗粒的方法，包括这种颗粒的药物制剂和制备药物的方法。