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    Sustained release pharmaceutical tablets and process for the preparation thereof
    1.
    发明授权
    Sustained release pharmaceutical tablets and process for the preparation thereof 失效
    缓释药片及其制备方法

    公开(公告)号：US4647599A

    公开(公告)日：1987-03-03

    申请号：US669945

    申请日：1984-11-09

    申请人： Denes Bezzegh ,  Pal Fekete ,  Zoltan Toth ,  Ilona Bor ,  Erzsebet Fellner

    发明人： Denes Bezzegh ,  Pal Fekete ,  Zoltan Toth ,  Ilona Bor ,  Erzsebet Fellner

    IPC分类号： A61K9/16 ,  A61K9/20 ,  A61K9/22 ,  A61K31/13 ,  A61K31/21 ,  A61K31/44 ,  A61K31/455 ,  A61K31/52 ,  A61K31/55 ,  A61K33/34 ,  A61K9/24

    CPC分类号： A61K9/2027

    摘要： The invention provides a method for preparing sustained release tablets comprising a hydrophilic polymer matrix, which amounts to at least 10% by weight of the composition, consisting of a 5:1-1:5 weight to weight ratio mixture of a VP-VA copolymer and of an acrylic acid homopolymer, cross-linked with polyallyl saccharose.The method of manufacturing of sustained release tablets according to the invention can be accomplished in two ways: either by manufacturing the granulate containing the active ingredient, or by supplementing the matrix granulate containing no active ingredient with the suitable amount of the active ingredient.The latter variant involves the advantage of a possible separation of large-scale manufacturing of pharmacons and that of a generally applicable retardizing system, the composition and, consequently, the retardizing ability of which can optionally be modified in accordance with the properties of the active ingredient(s) to be formulated.

    摘要翻译： 本发明提供一种制备持续释放片剂的方法，其包含亲水性聚合物基质，其相当于组合物重量的至少10重量％，由重量比为5:1-1:5的VP-VA共聚物 和丙烯酸均聚物，与聚烯丙基蔗糖交联。 根据本发明的缓释片剂的制造方法可以通过以下两种方法完成：通过制备含有活性成分的颗粒，或通过用不含活性成分的基质颗粒补充适量的活性成分。 后一种变体涉及药物的大规模制造可能分离的优点以及通常适用的延迟体系的优点，组合物以及因此其延迟能力可任选地根据活性成分的性质进行修饰 （s）将被制定。

    Process for the preparation of sustained release pharmaceutical compositions having a high active ingredient content
    2.
    发明授权
    Process for the preparation of sustained release pharmaceutical compositions having a high active ingredient content 失效
    制备具有高活性成分含量的缓释药物组合物的方法

    公开(公告)号：US4748023A

    公开(公告)日：1988-05-31

    申请号：US644835

    申请日：1984-08-27

    申请人： Eva Tamas ,  Pal Fekete ,  Tibor Kovacs ,  Denes Bezzegh ,  Ilona Bor nee Baumgartner ,  Zoltan Toth ,  Katalin Zukovics nee Sumeg

    发明人： Eva Tamas ,  Pal Fekete ,  Tibor Kovacs ,  Denes Bezzegh ,  Ilona Bor nee Baumgartner ,  Zoltan Toth ,  Katalin Zukovics nee Sumeg

    IPC分类号： A61K9/00 ,  A61K9/20 ,  A61K9/22 ,  A61K9/50 ,  A61K9/52 ,  A61K9/26

    CPC分类号： A61K9/2081

    摘要： The invention relates to a process for the preparation of sustained release solid pharmaceutical compositions having an active ingredient content of at least 80% and possessing a structure which loosens in aqueous medium but does not disintegrate to discrete particles within 4 hours which comprises coating the particles of the active ingredient in a liquid medium with a water insoluble polymer--preferably with an ethyl cellulose polymer film--and thereafter admixing the coated crystals with at least one disintegrating agent being capable of swelling in aqueous medium and other auxiliary agents conventionally used in pharmaceutical industry and pressing the mixture into tablets.The advantage of the process of the present invention is that it is readily feasible with a very wide range of active ingredients and provides sustained release tablets having a high active ingredient content.

    摘要翻译： PCT No.PCT / HU84 / 00006 Sec。 371日期1984年8月27日第 102（e）日期1984年8月27日PCT提交1984年1月25日PCT公布。 公开号WO84 / 02843 日本1984年8月2日。本发明涉及一种制备持续释放固体药物组合物的方法，其具有至少80％的活性成分含量，并且具有在水性介质中松动但不分解成4分内的离散颗粒的结构 其包括用水不溶性聚合物 - 优选与乙基纤维素聚合物膜在液体介质中涂覆活性成分的颗粒，然后将涂覆的晶体与至少一种能够在水性介质和其它助剂中溶胀的崩解剂混合 通常用于制药工业的药物并将混合物压制成片剂。 本发明方法的优点在于，使用非常宽范围的活性成分是容易可行的，并提供具有高活性成分含量的缓释片剂。

    Process for preparing microcapsules providing the rapid release of a drug as active ingredient
    4.
    发明授权
    Process for preparing microcapsules providing the rapid release of a drug as active ingredient 失效
    制备作为活性成分提供药物快速释放的微生物的方法

    公开(公告)号：US5192552A

    公开(公告)日：1993-03-09

    申请号：US458600

    申请日：1989-12-29

    申请人： Pal Fekete ,  Denes Bezzegh ,  Katalin Zukovics neSte,uml/u/ megh ,  Zsuzsanna Jambor neHoffmann ,  Janos Tombor

    发明人： Pal Fekete ,  Denes Bezzegh ,  Katalin Zukovics neSte,uml/u/ megh ,  Zsuzsanna Jambor neHoffmann ,  Janos Tombor

    IPC分类号： A61K9/20 ,  A61K9/50 ,  A61K9/62 ,  A61K47/38

    CPC分类号： A61K9/5015 ,  A61K9/2081 ,  A61K9/5047 ,  A61K9/5073 ,  Y10T428/2989

    摘要： The invention relates to the preparation of microcapsules ensuring direct tablet compression of a drug and rapid release of the drug as active ingredient from the tablets, which comprises microencapsulating the crystal granules of cyclohexane-insoluble active ingredients with a particle size of at most 1000 .mu.m, preferably smaller than 60 .mu.m and particularly preferably smaller than 30 .mu.m, in cyclohexane medium with ethylcellulose taken in an amount of 1:30 to 1:5, preferably 1:20 to 1:10, in relation to the core material, if desired, in the presence of 0.001 to 1.0% by weight/volume, preferably 0.01 to 0.05% by weight/volume, of an anionic surface-active agent; or post-treating the drug granules microencapsulated with ethylcellulose by a cyclohexane-dissolved surface-active agent taken in an amount of 0.001 to 1.0% by weight/volume, preferably 0.1 to 0.5% by weight/volume, in relation to cyclohexane.

    摘要翻译： 本发明涉及微胶囊的制备，确保药物直接压片，药物作为活性成分从片中快速释放，其中包括微粒化粒径至多1000μm的环己烷不溶性活性成分的晶粒 ，优选小于60μm，特别优选小于30μm，相对于芯材料，乙基纤维素的采用量为1:30至1:5，优选1:20至1:10的环己烷介质中， 如果需要，在0.001至1.0重量％/体积，优选0.01至0.05重量/体积的阴离子表面活性剂的存在下， 或者用环己烷溶解的表面活性剂用乙基纤维素微胶囊化的药物颗粒，其用量相对于环己烷为0.001〜1.0重量/体积，优选为0.1〜0.5重量/体积。

    Process for the preparation of solid pharmaceutical compositions
    6.
    发明授权
    Process for the preparation of solid pharmaceutical compositions 失效
    制备固体药物组合物的方法

    公开(公告)号：US5240662A

    公开(公告)日：1993-08-31

    申请号：US827397

    申请日：1992-01-29

    申请人： Sandor Erdos ,  Denes Bezzegh ,  Janos Egri ,  Erzsebet Barczay ,  Olga Magyar ,  Katalin Sumeg

    发明人： Sandor Erdos ,  Denes Bezzegh ,  Janos Egri ,  Erzsebet Barczay ,  Olga Magyar ,  Katalin Sumeg

    IPC分类号： A61K9/22 ,  A61K9/20 ,  A61K9/28 ,  A61K31/19 ,  A61K31/195 ,  A61K31/198 ,  A61K47/20 ,  A61K47/38 ,  A61P25/14 ,  C07C229/36 ,  C07C243/18

    CPC分类号： A61K9/2077 ,  A61K31/195 ,  A61K9/2004

    摘要： The invention relates to a process for the preparation of solid pharmaceutical compositions. More specifically, the invention relates to a process for the preparation of tablets ensuring an increased active ingredient release, where said tablets comprise as active ingredient a mixture of L-3,4-dihydroxyphenylalanine and L-alpha-hydrazino-alpha-methyl-3,4-dihydroxyphenyl propionic acid in a (3-12):1 mass to mass ratio, which comprises admixing any of L-3,4-dihydroxyphenylalanine and L-alpha-hydrazino-alpha-methyl-3,4-dihydroxyphenyl propionic acid, or both of them, with a hydrophilic diluent, preferably lactose and/or microcrystalline cellulose, and optionally with a colouring agent, blending the mixture thus obtained with auxiliary agents conventionally used for the preparation of tablets and optionally with the other active ingredient, furthermore with a solution of stearin in an appropriate solvent, preferably an alkanol comprising 2 to 4 carbon atoms, drying and granulating the mixture thus obtained, optionally admixing further auxiliary agent(s) to the dry granulate, compressing it into tablets comprising 50 to 70% by mass of active ingredient and, if desired, applying a film-coating onto the surface of the tablets thus obtained. The process according to the invention provides tablets of appropriate quality with rapid active ingredient release.