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    • 3. 发明授权
    • Pharmaceutical compositions for the controlled release of active substances
    • 用于控释活性物质的药物组合物
    • US07083807B2
    • 2006-08-01
    • US10607047
    • 2003-06-27
    • Domenico FanaraMonique BerwaerAnne BouquelleMichel Deleers
    • Domenico FanaraMonique BerwaerAnne BouquelleMichel Deleers
    • A61K9/14A61K9/20A61K9/22A61K9/24
    • A61K9/2009A61K9/2054A61K9/209
    • The invention relates to pharmaceutical compositions which can be administrated orally, allowing the controlled release of at least one active substance comprising a) the said at least one active substance, b) between 5 and 60% by weight, relative to the total weight of the composition, of at least one excipient, selected from inert matrices, hydrophilic matrices, lipid matrices, mixtures of inert matrices and of lipid matrices, mixtures of hydrophilic matrices and of inert matrices, with the exception of mixtures comprising a polyacrylic acid and at least one hydrophilic matrix of the cellulose type; c) between 5 and 50% by weight, relative to the total weight of the composition, of at least one alkalinizing agent soluble in an aqueous phase under physiological pH conditions, selected from alkali or alkaline-earth metal hydroxidcs, carbonates, bicarbonates and phosphates, sodium borate as well as the basic salts of organic acids. It also relates to processes for the preparation of said compositions, multi-layered pharmaceutical compositions comprising at least one layer with this composition, as well as processes for the preparation of said multi-layered composition.
    • 本发明涉及可以口服给药的药物组合物,允许控制释放至少一种活性物质,所述活性物质包含a)所述至少一种活性物质,b)相对于所述至少一种活性物质的总重量为5至60重量% 至少一种赋形剂,选自惰性基质,亲水基质,脂质基质,惰性基质和脂质基质的混合物,亲水基质和惰性基质的混合物,除了包含聚丙烯酸和至少一种 纤维素类型的亲水基质; c)在生理pH条件下,选自碱金属或碱土金属氢氧化物,碳酸盐,碳酸氢盐和磷酸盐的至少一种可溶于水相的至少一种碱化剂,相对于组合物的总重量为5至50重量% ,硼酸钠以及有机酸的碱性盐。 它还涉及制备所述组合物的方法,包含至少一层具有该组合物的多层药物组合物,以及制备所述多层组合物的方法。
    • 10. 发明授权
    • Pharmaceutical compositions for controlled release of active substances
    • 用于控制释放活性物质的药物组合物
    • US06699502B1
    • 2004-03-02
    • US09381044
    • 1999-09-29
    • Domenico FanaraMonique BerwaerAnne BouquelleMichel Deleers
    • Domenico FanaraMonique BerwaerAnne BouquelleMichel Deleers
    • A61K914
    • A61K9/2009A61K9/2054A61K9/209
    • The present invention is directed a pharmaceutical composition which can be administered orally, allowing for the controlled release of at least one active substance. The composition includes at least one active substance, between 5 and 60% by weight, relative to the total weight of the composition, of at least one excipient, selected from inert matrices, hydrophilic matrices, lipid matrices, mixtures of inert matrices and of lipid matrices, and mixtures of hydrophilic matrices and of inert matrices, with the exception of mixtures including a polyacrylic acid and at least one hydrophilic matrix of the cellulose type; and between 5 and 50% by weight, relative to the total weight of the composition, of at least one alkalinizing agent soluble in an aqueous phase under physiological pH conditions, selected from alkali or alkaline-earth metal hydroxides, carbonates, bicarbonates, phosphates, sodium borate and basic salts of organic acids. The invention further includes a process for preparation of the composition, multi-layered pharmaceutical compositions including at least one layer of the inventive composition, and processes for producing same.
    • 本发明涉及可以口服给药,允许至少一种活性物质的受控释放的药物组合物。 所述组合物包含至少一种活性物质,相对于组合物的总重量为5至60重量%,至少一种选自惰性基质,亲水基质,脂质基质,惰性基质和脂质的混合物的赋形剂 基质,以及亲水基质和惰性基质的混合物,除了包括聚丙烯酸和纤维素类型的至少一种亲水基质的混合物外; 和相对于组合物的总重量为5至50重量%的至少一种在生理pH条件下可溶于水相的碱化剂,其选自碱金属或碱土金属氢氧化物,碳酸盐,碳酸氢盐,磷酸盐, 硼酸钠和有机酸的碱式盐。 本发明还包括制备组合物的方法,包括至少一层本发明组合物的多层药物组合物及其制备方法。