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    Pharmaceutical formulations for sustained drug delivery
    1.
    发明申请
    Pharmaceutical formulations for sustained drug delivery 审中-公开

    公开(公告)号：US20070185032A1

    公开(公告)日：2007-08-09

    申请号：US11265520

    申请日：2005-11-02

    申请人： Malcolm Gefter ,  Nicholas Barker ,  Gary Musso ,  Christopher Molineaux

    发明人： Malcolm Gefter ,  Nicholas Barker ,  Gary Musso ,  Christopher Molineaux

    IPC分类号： A61K38/09 ,  A61K38/08 ,  A61K9/14

    CPC分类号： A61K38/09 ,  A61K47/61

    摘要： Sustained delivery formulations comprising a water-insoluble complex of a peptidic compound (e.g., a peptide, polypeptide, protein, peptidomimetic or the like) and a carrier macromolecule are disclosed. The formulations of the invention allow for loading of high concentrations of peptidic compound in a small volume and for delivery of a pharmaceutically active peptidic compound for prolonged periods, e.g., one month, after administration of the complex. The complexes of the invention can be milled or crushed to a fine powder. In powdered form, the complexes form stable aqueous suspensions and dispersions, suitable for injection. In a preferred embodiment, the peptidic compound of the complex is an LHRH analogue, preferably an LHRH antagonist, and the carrier macromolecule is an anionic polymer, preferably carboxymethylcellulose. Methods of making the complexes of the invention, and methods of using LHRH-analogue-containing complexes to treat conditions treatable with an LHRH analogue, are also disclosed.

    Pharmaceutical formulations for sustained drug delivery
    2.
    发明申请
    Pharmaceutical formulations for sustained drug delivery 审中-公开
    用于持续给药的药物制剂

    公开(公告)号：US20070185033A1

    公开(公告)日：2007-08-09

    申请号：US11205270

    申请日：2005-08-15

    申请人： Malcolm Gefter ,  Nicholas Barker ,  Gary Musso ,  Christopher Molineaux

    发明人： Malcolm Gefter ,  Nicholas Barker ,  Gary Musso ,  Christopher Molineaux

    IPC分类号： A61K38/09 ,  A61K38/08 ,  A61K9/14

    CPC分类号： A61K9/146 ,  A61K9/0019 ,  A61K38/09

    摘要： Sustained delivery formulations comprising a water-insoluble complex of a peptidic compound (e.g., a peptide, polypeptide, protein, peptidomimetic or the like) and a carrier macromolecule are disclosed. The formulations of the invention allow for loading of high concentrations of peptidic compound in a small volume and for delivery of a pharmaceutically active peptidic compound for prolonged periods, e.g., one month, after administration of the complex. The complexes of the invention can be milled or crushed to a fine powder. In powdered form, the complexes form stable aqueous suspensions and dispersions, suitable for injection. In a preferred embodiment, the peptidic compound of the complex is an LHRH analogue, preferably an LHRH antagonist, and the carrier macromolecule is an anionic polymer, preferably carboxymethylcellulose. Methods of making the complexes of the invention, and methods of using LHRH-analogue-containing complexes to treat conditions treatable with an LHRH analogue, are also disclosed.

    摘要翻译： 公开了包含肽化合物（例如肽，多肽，蛋白质，拟肽等）和载体大分子的水不溶性络合物的持续递送制剂。 本发明的制剂允许在施用复合物之后将较高体积的肽化合物加载至少量的药物活性肽化合物延长的时期，例如一个月。 本发明的络合物可以研磨或粉碎成细粉末。 以粉末形式，络合物形成稳定的水性悬浮液和分散体，适于注射。 在优选的实施方案中，复合物的肽化合物是LHRH类似物，优选LHRH拮抗剂，载体大分子是阴离子聚合物，优选羧甲基纤维素。 还公开了制备本发明复合物的方法，以及使用含LHRH类似物的复合物治疗可用LHRH类似物治疗的病症的方法。

    Methods for treating FSH related conditions with GnRH antagonists
    3.
    发明申请
    Methods for treating FSH related conditions with GnRH antagonists 审中-公开
    用GnRH拮抗剂治疗FSH相关病症的方法

    公开(公告)号：US20070015714A1

    公开(公告)日：2007-01-18

    申请号：US11343283

    申请日：2006-01-30

    申请人： Marc Garnick ,  Paul Martha ,  Christopher Molineaux ,  Alex DePaoli

    发明人： Marc Garnick ,  Paul Martha ,  Christopher Molineaux ,  Alex DePaoli

    IPC分类号： A61K38/09

    CPC分类号： A61K38/09 ,  A61K47/46

    摘要： Methods for treating FSH related conditions, such as prostatic intraepithelial neoplasia, pedophilia, infertility, or vaginal bleeding, with GnRH antagonists are disclosed. The methods of the invention generally feature administering to a subject a GnRH antagonist suitable for in vivo administration and able to reduce both plasma FSH and LH levels in a subject, in an amount or in a formulation effective to reduce plasma FSH levels in the subject to a symptom alleviating level. In vitro fertilization and male contraceptive methods are also provided.

    摘要翻译： 公开了用GnRH拮抗剂治疗FSH相关病症如前列腺上皮内瘤变，恋童癖，不育症或阴道出血的方法。 本发明的方法通常特征在于向受试者施用适于体内施用的GnRH拮抗剂，并且能够降低受试者中的血浆FSH和LH水平，其量可以有效地降低受试者的血浆FSH水平， 症状缓解水平。 还提供体外受精和男性避孕方法。