Slow-release matrix pellets and the production thereof
    5.
    发明授权
    Slow-release matrix pellets and the production thereof 失效
    缓释基质颗粒及其制备

    公开(公告)号:US06290990B1

    公开(公告)日:2001-09-18

    申请号:US08727666

    申请日:1996-10-17

    IPC分类号: A61K916

    摘要: Slow-release matrix pellets with a spherical or lenticular shape and uniform maximum diameters in the range from 0.5 to 4 mm, composed of a) 0.1-87% by weight of at least one biologically active compound, b) 5-50% by weight of at least one water-insoluble polymer, c) 5-45% by weight of at least one lipophilic component as plasticizer for polymer b), d) 3-40% by weight of a natural or semisynthetic gel former, e) 0-50% by weight of one or more conventional formulation aids.

    摘要翻译: 具有球形或透镜形状的缓释基质颗粒和0.5至4mm范围内的均匀最大直径,由a)0.1-87重量%的至少一种生物活性化合物组成,b)5-50重量% 至少一种水不溶性聚合物,c)5-45重量%的至少一种亲脂性组分作为聚合物b)的增塑剂,d)3-40重量%的天然或半合成凝胶成型剂,e)0-50 重量%的一种或多种常规制剂助剂。

    Compositions which contain active substances and are in the form of
solid particles
    6.
    发明授权
    Compositions which contain active substances and are in the form of solid particles 失效
    含有活性物质并呈固体颗粒形式的组合物

    公开(公告)号:US5641516A

    公开(公告)日:1997-06-24

    申请号:US511489

    申请日:1995-08-07

    CPC分类号: A61K9/146 A61K9/2095

    摘要: Compositions which contain active substances and are in the form of solid particles can be obtained by intimately mixing the active substance with a water-soluble melt composed ofa) 10-90% by weight of a water-soluble polymer A with a viscosity V.sub.a of 1,000-120,000 cps andb) 10-90% by weight of a water-soluble polymer B with a viscosity V.sub.b of 1-500 cpsas carrier substance, where the viscosities V.sub.a and V.sub.b are those of a 2% by weight aqueous solution at 20.degree. C., measured by the ASTM D 2363-72 capillary method (European Pharmacopoeia, Vol. III, p. 37), and processing the melt with shaping to give the particles.

    摘要翻译: 包含活性物质并且为固体颗粒形式的组合物可以通过将活性物质与由水溶性聚合物A的10-90重量%组成的水溶性熔体紧密混合而获得,其中粘度Va为 1,000-120,000cps和b)10-90重量%的粘度Vb为1-500cps的水溶性聚合物B作为载体物质,其中粘度Va和Vb是2重量%水溶液中的粘度 通过ASTM D 2363-72毛细管法(欧洲药典,第III卷,第37页)测量,并通过成型加工熔体以得到颗粒。

    Solid depot drug form
    7.
    发明授权
    Solid depot drug form 失效
    固体贮库药物形式

    公开(公告)号:US5552159A

    公开(公告)日:1996-09-03

    申请号:US125133

    申请日:1993-09-23

    IPC分类号: A61K9/20 A61K9/22

    摘要: A solid depot drug form produced by melt extrusion at from 50.degree. to 200.degree. C. and continuous shaping of a mixture of from 0.1 to 70% by weight, based on the finished depot form, of a pharmaceutical active ingredient with a polymer melt of the following composition:a) at least 6% by weight, based on the complete depot form, of at least one water-insoluble poly(meth) acrylate with a glass transition temperature Tg in the range from -60.degree. to 180.degree. C.,b) a water-soluble hydroxyalkylcellulose or hydroxy-alkylmethylcellulose with 2 or 3 carbons in the hydroxyalkyl, or an N-vinylpyrrolidone polymer with from 0 to 50% by weight of vinyl acetate or a mixture of the two in the ratio a):b) =5:95 to 95:5, andc) 0-30% by weight, based on the finished depot form, of one or more conventional pharmaceutical auxiliaries.

    摘要翻译: 一种固体贮库药物形式,其通过在50℃至200℃的熔融挤出而制备,并且基于最终的贮库形式连续成型0.1至70重量%的混合物,药物活性成分与聚合物熔体 以下组合物:a)至少6重量%,基于完整的储存形式,至少一种水不溶性聚(甲基)丙烯酸酯的玻璃化转变温度Tg在-60℃至180℃的范围内。 ,b)在羟烷基中具有2或3个碳原子的水溶性羟烷基纤维素或羟基烷基甲基纤维素,或0-50重量%乙酸乙烯酯的N-乙烯基吡咯烷酮聚合物或两者的混合物,其比例a): b)= 5:95至95:5,和c)基于成品仓库形式的一种或多种常规药物助剂的0-30重量%。

    Production of solid pharmaceutical depot forms
    9.
    发明授权
    Production of solid pharmaceutical depot forms 失效
    生产固体药剂库

    公开(公告)号:US5490990A

    公开(公告)日:1996-02-13

    申请号:US78824

    申请日:1993-06-21

    摘要: A process for the production of solid pharmaceutical depot forms by application of a reconstituted aqueous dispersion of a pharmaceutically acceptable binder to a core which contains active substance or by wet granulation of the pharmaceutical active substance with such a binder dispersion or by direct tableting of an active substance with the redispersible binder powder, wherein the binder has been obtained by emulsion polymerization and subsequent spray drying of the resulting aqueous dispersion with a water-soluble pharmaceutically acceptable spraying aid with a glass transition temperature of at least 60.degree. C. and with or without a pharmaceutically acceptable antiblocking agent.

    摘要翻译: 通过将药学上可接受的粘合剂的重构水性分散体应用于含有活性物质的核心或通过用这种粘合剂分散体湿法制粒药物活性物质或通过直接压片活性物质来生产固体药物贮库的方法 物质与可再分散的粘合剂粉末,其中粘合剂已经通过乳液聚合获得并随后用水溶性药学上可接受的喷雾助剂喷雾干燥所得水性分散体,玻璃化转变温度至少为60℃,有或没有 药学上可接受的防粘连剂。

    Coating of drug forms
    10.
    发明授权
    Coating of drug forms 失效
    药物形式的涂层

    公开(公告)号:US5326586A

    公开(公告)日:1994-07-05

    申请号:US957375

    申请日:1992-10-07

    摘要: A process for coating drug forms by application of an aqueous dispersion which contains as binder a redispersed latex of an emulsion polymer onto the drug form and evaporating the water at a temperature at which the latex particles form a film, comprises employing a polymer dispersion which has been prepared by emulsion polymerization of one part by weight of at least one ethylenically unsaturated polymerizable monomer, by means of initiators which provide free radicals, in the presence of from 0.1 to 2 parts by weight of saccharified starch, and from 0 to 5% by weight, based on the monomer or monomers, of a surfactant, with or without further conventional additives, drying to a powder and redispersing in water.

    摘要翻译: 通过应用含水分散体涂覆药物形式的方法,该水性分散体含有作为粘合剂的乳液聚合物的再分散胶乳到药物形式上并在胶乳颗粒形成膜的温度下蒸发水,包括使用聚合物分散体,其具有 通过在0.1至2重量份的糖化淀粉和0至5重量%的糖化淀粉存在下,通过使用1重量份的至少一种烯键式不饱和可聚合单体,通过提供自由基的引发剂, 重量,基于单体或单体的表面活性剂,含或不含其它常规添加剂,干燥至粉末并再分散于水中。