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    Process for preparing microcapsules providing the rapid release of a drug as active ingredient
    1.
    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 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。

    Sustained release pharmaceutical tablets and process for the preparation thereof
    3.
    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。

    Diffusion-osmotic controlled drug-release pharmaceutical composition and process for preparing same
    5.
    发明授权
    Diffusion-osmotic controlled drug-release pharmaceutical composition and process for preparing same 失效
    扩散渗透控制药物释放药物组合物及其制备方法

    公开(公告)号：US5543155A

    公开(公告)日：1996-08-06

    申请号：US341209

    申请日：1994-12-05

    申请人： Pal Fekete ,  Maria Kiraly nee Ignacz ,  Gabor Sipos ,  Zsuzsanna Jambor nee Hoffmann ,  Gyorgy Ujfalussy ,  Magdolna Gora nee Hernyes ,  Imre Klebovich ,  Sandor Drabant ,  Attila Mandi ,  Gizella Kiss nee Szabo ,  Erzsebet Barczay ,  Maria Krisztian

    发明人： Pal Fekete ,  Maria Kiraly nee Ignacz ,  Gabor Sipos ,  Zsuzsanna Jambor nee Hoffmann ,  Gyorgy Ujfalussy ,  Magdolna Gora nee Hernyes ,  Imre Klebovich ,  Sandor Drabant ,  Attila Mandi ,  Gizella Kiss nee Szabo ,  Erzsebet Barczay ,  Maria Krisztian

    IPC分类号： A61K9/36 ,  A61J3/10 ,  A61K9/00 ,  A61K9/22 ,  A61K9/32 ,  A61K47/34 ,  A61K9/24

    CPC分类号： A61K9/0004 ,  Y10S514/96

    摘要： The invention relates to a novel diffusion-osmotic controlled drug-release pharmaceutical composition containing a one-layer tablet core including a polymeric film-coat, a therapeutically active agent and a hydrophilic polymer; if desired, a two-layer tablet core including active agent and hydrophilic polymer in the first layer thereof and a hydrophilic polymer in the second layer thereof; at least one bore on the part of film-coat in contact with the core or core layer containing the active agent; and, if desired, containing one or more bore(s) in the part thereof in contact with the second layer containing the hydrophilic polymer, which comprises an ammonium methacrylate copolymer as coating material and hydroxypropyl-methylcellulose as hydrophilic polymer. The composition according to the invention is useful for preparing controlled drug-release tablets containing as active agents e.g. .beta.-adrenergic inhibitors (e.g. propranolol) calcium-antagonists (e.g. nifedipine), angiotensin convertase enzyme (ACE) inhibitors (e.g. captopril); prazosin; or nitroglycerol, all used in heart and circulation diseases; vasodilatory active agents (e.g. pentoxyfylline), nonsteroidal antiinflammatory agents (e.g. naproxene), analgetic drugs (e.g. morphine) and drugs acting on the central nervous system (e.g. amitriptyline, buspiron). The invention furthermore relates to a process for the preparation of the above compositions.

    摘要翻译： 本发明涉及一种新颖的扩散渗透控制药物释放药物组合物，其含有包含聚合物膜包衣，治疗活性剂和亲水性聚合物的单层片芯; 如果需要，在其第一层中包含活性剂和亲水性聚合物的两层片芯和其第二层中的亲水性聚合物; 膜包衣部分的至少一个孔与含有活性剂的芯层或芯层接触; 并且如果需要，在其部分中含有与包含亲水性聚合物的第二层接触的一个或多个孔，其包含作为涂层材料的甲基丙烯酸铵共聚物和作为亲水性聚合物的羟丙基甲基纤维素。 根据本发明的组合物可用于制备包含作为活性剂的受控药物释放片剂，例如， β-肾上腺素能抑制剂（如普萘洛尔）钙拮抗剂（如硝苯地平），血管紧张素转化酶（ACE）抑制剂（如卡托普利）; 哌唑嗪 或硝酸甘油，均用于心脏和循环疾病; 血管舒张活性剂（例如戊氧基线），非甾体抗炎剂（例如萘普生），止痛药（例如吗啡）和作用于中枢神经系统的药物（例如阿米替林，buspiron）。 本发明还涉及制备上述组合物的方法。

    Synergistically active veterinary compositions and process for preparing same
    7.
    发明授权
    Synergistically active veterinary compositions and process for preparing same 失效
    合成活性兽药组合物及其制备方法

    公开(公告)号：US5120711A

    公开(公告)日：1992-06-09

    申请号：US616813

    申请日：1990-11-20

    申请人： Karoly Magyar ,  Ferenc Simon ,  Janos Varga ,  Attila Nagy ,  Laszlo Puskas ,  Pal Fekete ,  Janos Egri ,  Katalin Zukovics

    发明人： Karoly Magyar ,  Ferenc Simon ,  Janos Varga ,  Attila Nagy ,  Laszlo Puskas ,  Pal Fekete ,  Janos Egri ,  Katalin Zukovics

    IPC分类号： A61K38/00 ,  A61K38/04 ,  A61P15/00 ,  A61P15/14

    CPC分类号： A61K38/04

    摘要： The invention relates to synergistically active veterinary compositions useful particularly for the treatment of mastitis and metritis. The invention further relates to a process for preparing these compositions. The compositions according to the invention comprise, based on 1 part by weight of 6,9,18-tris(2-aminoethyl) -15-benzyl-21-[.sup.- 2,8-bis(2-aminoethyl)-5-(1-hydroxyethyl) -15-methyl-4,7,10-trioxo-3,6,9-triazaheptadecanamido]-3-(1-hydroxyethyl)-12-isobutyl-1,4,7,10,13,16,19-heptaazacyclotricosane-2, 5,8,11,14,17,20-heptaone or a pharmaceutically acceptable acid addition salt thereof, 1 to 1000 parts by weight of 1-(2-chlorophenyl)-diphenylmethyl-1H-imidazole or 1 to 400 parts by weight of 2-methyl-5,7-dichloro-8-hydroxyquinoline, respectively, optionally in admixture with carriers and/or additives commonly used in the pharmaceutical industry.

    摘要翻译： 本发明涉及特别用于治疗乳腺炎和子宫炎的协同作用的兽医学组合物。 本发明还涉及制备这些组合物的方法。 根据本发明的组合物包含基于1重量份的6,9,18-三（2-氨基乙基）-15-苄基-21 - [ - 2,8-双（2-氨基乙基）-5-（ 1-羟乙基）-15-甲基-4,7,10-三氧代-3,6,9-三氮杂十七烷酰胺基] -3-（1-羟基乙基）-12-异丁基-1,4,7,10,13,16 ，19-七氮杂环五烷-2,5,8,11,14,17,20-七酮或其药学上可接受的酸加成盐，1〜1000重量份的1-（2-氯苯基） - 二苯基甲基-1H-咪唑或 1至400份（重量）的2-甲基-5,7-二氯-8-羟基喹啉，分别任选与制药工业中通常使用的载体和/或添加剂混合。

    Plant growth regulating compounds and compositions and a process for the preparation thereof
    9.
    发明授权
    Plant growth regulating compounds and compositions and a process for the preparation thereof 失效
    植物生长调节化合物和组合物及其制备方法

    公开(公告)号：US4740228A

    公开(公告)日：1988-04-26

    申请号：US569594

    申请日：1984-01-10

    申请人： Attila Kis-Tamas ,  Ferenc Jurak ,  Zoltan Vig ,  Pal Fekete ,  Judit Kulcsar

    发明人： Attila Kis-Tamas ,  Ferenc Jurak ,  Zoltan Vig ,  Pal Fekete ,  Judit Kulcsar

    IPC分类号： A01N37/18 ,  A01N37/34 ,  A01N43/46 ,  A01P21/00 ,  A47B13/04 ,  C07C67/00 ,  C07C253/00 ,  C07C255/32 ,  C07C255/35 ,  C07C255/41 ,  C07C255/56 ,  C07C255/58 ,  C07D295/10 ,  C07D295/16 ,  C07D295/18 ,  A01N37/22 ,  A01N37/20

    CPC分类号： C07C255/00 ,  A01N37/34

    摘要： The invention relates to new plant growth regulating compositions, which contain as active agent 0.001 to 95% by weight of one or more compound(s) of the general formula (I), ##STR1## wherein R.sup.1 and R.sup.2 each represent hydrogen atom, a C.sub.1-5 alkyl group, a C.sub.5-7 cycloalkyl group, an aryl group, a halogen-substituted aryl group, an aralkyl group, a C.sub.2-5 alkenyl group or a C.sub.2-5 alkynyl group, orR.sup.1 and R.sup.2 form, together with the adjacent nitrogen atom, a morpholino, pyrrolidino, piperidino or perhydroazepinyl group, andR.sup.3 stands for hydrogen or a C.sub.1-5 alkyl group,together with an inert, solid, liquid and/or gaseous carrier or diluent, and optionally one or more additives, such as surfactants or other substances of plant biological activity.The compounds of the general formula (I) in which R.sup.1 is hydrogen and R.sup.2 stands for hydrogen, C.sub.1-3 alkyl, aralkyl or C.sub.3-5 alkenyl group, furthermore in which R.sup.1 and R.sup.3 are hydrogen and R.sup.2 is an aryl group have already been described in the literature, whereas the remaining derivatives of the general formula (I) are new. These compounds can be prepared by reacting a compound of the general formula (II) ##STR2## with an amine of the general formula (III), ##STR3## or by alkylating a compound of the general formula (IV). ##STR4## In the above formulae X stands for halogen, hydroxy or C.sub.1-4 alkoxy, whereas R.sup.1, R.sup.2 and R.sup.3 have the meanings as defined above.

    摘要翻译： 本发明涉及新的植物生长调节组合物，其含有0.001至95重量％的一种或多种通式（I）化合物，其中R 1和R 2各自表示氢的活性剂 原子，C1-5烷基，C5-7环烷​​基，芳基，卤素取代的芳基，芳烷基，C2-5烯基或C2-5炔基，或R1和R2形式 与相邻的氮原子一起形成吗啉代，吡咯烷子基，哌啶子基或全氢氮杂基，R3代表氢或C1-5烷基，与惰性，固体，液体和/或气态载体或稀释剂一起使用， 或更多的添加剂，例如表面活性剂或植物生物活性的其它物质。 其中R1是氢并且R2代表氢，C1-3烷基，芳烷基或C3-5烯基的通式（Ⅰ）化合物，此外R1和R3是氢，R2是芳基， 文献中描述的，而通式（I）的剩余衍生物是新的。 这些化合物可以通过使通式（II）的化合物（II）与通式（III）的胺，（IMAGE）（III）反应或通过烷基化通式（IV）的化合物 ）。 （IV）在上式中，X表示卤素，羟基或C 1-4烷氧基，而R 1，R 2和R 3具有如上定义的含义。