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1.发明公开
公开(公告)号：EP1297840A3
公开(公告)日：2003-09-10
申请号：EP02078871.7
申请日：1996-11-25
IPC分类号： A61K38/09
CPC分类号： A61K38/09 , Y10S514/80 , A61K2300/00
摘要： Methods for treating sex hormone-dependent conditions are disclosed. The methods of the invention generally feature administration to a subject of an LHRH antagonist, in combination with a second therapy. In one embodiment, this second therapy is the performance of a procedure that removes or destroys tumor tissue, such as radical excision, cryosurgery or radiation therapy (external or interstitial). In another embodiment, the second therapy is treatment with an LHRH agonist, either simultaneously with or subsequent to LHRH antagonist therapy. The methods of the invention can further involve administering an antiandrogen and/or an inhibitor of sex steroid biosynthesis to the subject in combination with the LHRH antagonist. Methods for inhibiting the LHRH antagonist - induced hormone surge, whatever its clinical setting, are also disclosed. These methods generally involve administration of an LHRH antagonist in combination with the LHRH agonist. Complete suppression of the LHRH agonist-induced hormone surge has been achieved by pretreatment with a sustained-released formulation of LHRH antagonist.
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公开(公告)号：EP1878437A3
公开(公告)日：2008-11-12
申请号：EP07019134.1
申请日：1997-12-11
CPC分类号： B82Y5/00 , A61K38/09 , A61K47/61 , A61K47/6949 , Y10S514/80
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.
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3.发明公开Methods for treating sex hormone-dependent conditions with LHRH antagonists 失效用LHRH拮抗剂治疗性激素依赖性病症的方法
公开(公告)号：EP1297840A2
公开(公告)日：2003-04-02
申请号：EP02078871.7
申请日：1996-11-25
IPC分类号： A61K38/09
CPC分类号： A61K38/09 , Y10S514/80 , A61K2300/00
摘要： Methods for treating sex hormone-dependent conditions are disclosed. The methods of the invention generally feature administration to a subject of an LHRH antagonist, in combination with a second therapy. In one embodiment, this second therapy is the performance of a procedure that removes or destroys tumor tissue, such as radical excision, cryosurgery or radiation therapy (external or interstitial). In another embodiment, the second therapy is treatment with an LHRH agonist, either simultaneously with or subsequent to LHRH antagonist therapy. The methods of the invention can further involve administering an antiandrogen and/or an inhibitor of sex steroid biosynthesis to the subject in combination with the LHRH antagonist. Methods for inhibiting the LHRH antagonist - induced hormone surge, whatever its clinical setting, are also disclosed. These methods generally involve administration of an LHRH antagonist in combination with the LHRH agonist. Complete suppression of the LHRH agonist-induced hormone surge has been achieved by pretreatment with a sustained-released formulation of LHRH antagonist.
摘要翻译： 公开了治疗性激素依赖性病症的方法。 本发明的方法通常特征在于与第二疗法组合给予受试者LHRH拮抗剂。 在一个实施方案中，该第二疗法是去除或破坏肿瘤组织的程序的执行，例如自由基切除，冷冻手术或放射疗法（外部或间质）。 在另一个实施方案中，第二种疗法是在LHRH拮抗剂治疗的同时或之后用LHRH激动剂治疗。 本发明的方法可以进一步涉及与LHRH拮抗剂组合给予受试者抗雄激素和/或性类固醇生物合成抑制剂。 也公开了抑制LHRH拮抗剂诱导的激素激增的方法，无论其临床情况如何。 这些方法通常涉及与LHRH激动剂组合施用LHRH拮抗剂。 用LHRH拮抗剂的缓释制剂进行预处理已经完全抑制了LHRH激动剂诱导的激素激增。
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4.发明公开Pharmaceutical formulations comprising a water-insoluble complex for sustained drug delivery 失效含有药物缓释组合物，水不溶性配位化合物
公开(公告)号：EP1398037A2
公开(公告)日：2004-03-17
申请号：EP03017263.9
申请日：1997-12-11
CPC分类号： B82Y5/00 , A61K38/09 , A61K47/61 , A61K47/6949 , Y10S514/80
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： 组合物包含肽化合物和载体大分子的不溶于水的复合物。
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5.发明公开Pharmaceutical formulations comprising a water-insoluble complex for sustained drug delivery 失效含有药物缓释组合物，水不溶性配位化合物
公开(公告)号：EP1398037A3
公开(公告)日：2004-04-14
申请号：EP03017263.9
申请日：1997-12-11
CPC分类号： B82Y5/00 , A61K38/09 , A61K47/61 , A61K47/6949 , Y10S514/80
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.
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6.发明公开Pharmaceutical formulations for sustained drug delivery 失效Pharmazeutische Formulierungen zur kontinuierlichen Arzneimittelabgabe
公开(公告)号：EP2316471A1
公开(公告)日：2011-05-04
申请号：EP10012792.7
申请日：1997-12-11
CPC分类号： B82Y5/00 , A61K38/09 , A61K47/61 , A61K47/6949 , Y10S514/80
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-anatogue-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。 本发明的制剂允许以小体积装载高浓度的肽化合物和延长药物活性肽化合物的递送，例如， 一个月后，复杂的管理。 本发明的络合物可以研磨或粉碎成细粉末。 在粉末形式中，络合物形成适合于注射的稳定的水性悬浮液和分散体。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，以及使用含有LHRH-唾液酸的复合物来治疗可用LHRH类似物治疗的病症的方法。
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7.发明公开Pharmacuetical formulations for sustained drug delivery 失效Pharmazeutische Formulierungen zur anhaltenden Arzneimittelfreisetzung
公开(公告)号：EP1878437A2
公开(公告)日：2008-01-16
申请号：EP07019134.1
申请日：1997-12-11
CPC分类号： B82Y5/00 , A61K38/09 , A61K47/61 , A61K47/6949 , Y10S514/80
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。 本发明的制剂允许以小体积装载高浓度的肽化合物和延长药物活性肽化合物的递送，例如， 一个月后，复杂的管理。 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。
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8.发明授权Pharmaceutical formulations comprising a water-insoluble complex for sustained drug delivery 失效含有药物缓释组合物，水不溶性配位化合物
公开(公告)号：EP1398037B1
公开(公告)日：2008-01-09
申请号：EP03017263.9
申请日：1997-12-11
CPC分类号： B82Y5/00 , A61K38/09 , A61K47/61 , A61K47/6949 , Y10S514/80
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