公开(公告)号：US4199560A

公开(公告)日：1980-04-22

申请号：US952932

申请日：1978-10-19

申请人： Laszlo Gyarmati ,  Istvan Racz ,  Peter Szentmiklosi ,  Janos Plachy

发明人： Laszlo Gyarmati ,  Istvan Racz ,  Peter Szentmiklosi ,  Janos Plachy

IPC分类号： A61K9/16 ,  A61K9/20 ,  A61K9/22 ,  A61K9/48 ,  A61K9/26 ,  A61K9/54 ,  A61K33/06

CPC分类号： A61K9/1652 ,  A61K9/1617 ,  A61K9/2077 ,  A61K9/4841

摘要： The present invention relates to a solid oral pharmaceutical preparation with protracted release of the active ingredient consisting of discrete solid granules containing the active ingredient soluble in the stomach and auxiliary agents and of an equally solid external phase surrounding the said granules, whereby the granules forming the internal phase consist of granules prepared from a powder mixture which contains as active ingredient, or in addition to it a non-toxic metal compound, being capable of binding an acid, and being insoluble or but slightly soluble in neutral aqueous medium--particularly bismuth, aluminium or magnesium compound--and auxiliary materials prepared with an aqueous emulsion containing a hydrophobic component and hydrophylic emulsifiers, and the external phase contains a solid, dry, amphoteric gel forming substance in an amount of 1-50 percent w/w related to the total weight of the preparation in admixture with auxiliary agents.The preparation is produced by the wetting of the powder mixture containing the basic metal compound, auxiliary material and in given case additional active ingredient with the aqueous emulsion of the hydrophobic component prepared by applying the hydrophylic emulsifiers then by granulation and admixing the dried granules with the amphoteric gel forming substance, and pressing it into tablets, or filling into capsules.

摘要翻译： 本发明涉及具有长时间释放的活性成分的固体口服药物制剂，其由分散的固体颗粒组成，所述固体颗粒含有可溶于胃的活性成分和辅助剂以及围绕所述颗粒的同样固体的外部相，其中颗粒形成 内相包含由粉末混合物制成的颗粒，所述粉末混合物含有作为活性成分的粉末混合物，或除此之外，还含有无毒金属化合物，其能够结合酸，并且在中性水性介质（特别是铋）中不溶或略微溶解， 铝或镁化合物以及用含有疏水组分和亲水乳化剂的水性乳液制备的辅助材料，并且外相含有与总量相关的1-50％w / w的固体，干燥，两性凝胶形成物质 制剂的重量与助剂混合。 该制备是通过润湿包含碱性金属化合物，辅助材料的粉末混合物，并且在给定情况下，通过施用亲水性乳化剂制备疏水组分的水性乳液，然后通过造粒和将干燥颗粒与 两性凝胶形成物质，并将其压制成片剂或填充到胶囊中。

公开(公告)号：US4921707A

公开(公告)日：1990-05-01

申请号：US165102

申请日：1988-03-28

申请人： Istvan Racz ,  Janos Plachy ,  Peter Szentmiklosi

发明人： Istvan Racz ,  Janos Plachy ,  Peter Szentmiklosi

IPC分类号： A61K9/00 ,  A61K9/16 ,  A61K9/20 ,  A61K9/22 ,  A61K33/08

CPC分类号： A61K9/0095 ,  A61K33/08 ,  A61K9/1635 ,  A61K9/1652 ,  A61K9/2027 ,  A61K9/2054 ,  A61K9/2072 ,  A61K9/2077

摘要： The invention relates to the production of a new pharmaceutical preparation of high acid-binding capacity, of delayed effect, of increased bioavailability for neutralization of gastric acid and eventually to other pharmaceutical preparations acting in the gastrointestinal tract, first of all of laxative effect by mixing 100 parts by mass of a powdered basic magnesium compound or the powdered mixture of basic magnesium compounds and basic aluminum compounds with 2-2500 parts of a dry or water-swollen organic acid of polymeric character and therapeutically acceptable, e.g. cellulose-glycolic acid, starch-glycolic acid or polymer acrylic and/or methacrylic acid, letting this powdered mixture to stand for 1-24 hours at the temperature of 20.degree.-80.degree. C. after addition of 50-500 parts by mass of water and forming tablets or other pharmaceutical preparations, optionally after addition of 5-60 parts by mass of smoothing agents and/or other pharmaceutical excipients, or transforming the mixture containing the basic active ingredients and the polymeric organic acid in liquid suspension by adding water and optionally excipients.

摘要翻译： PCT No.PCT / HU87 / 00026 Sec。 371日期：1988年3月28日 102（e）1988年3月28日PCT申请1987年6月24日PCT公布。 第WO88 / 00051号公报 日期：1988年1月14日。本发明涉及生产具有较高的酸结合能力，延迟作用，增加生物利用度的中和酸性药物，最终涉及作用于胃肠道的其他药物制剂的新型药物制剂 通过将100质量份的粉状碱性镁化合物或碱性镁化合物和碱性铝化合物的粉末混合物与2-2500份具有聚合特性的干燥或水溶胀的有机酸和治疗上可接受的混合物混合， 例如 纤维素 - 乙醇酸，淀粉 - 乙醇酸或聚合物丙烯酸和/或甲基丙烯酸，使该粉末混合物在20〜80℃的温度下静置1-24小时，加入50-500质量份 水和成型片剂或其它药物制剂，任选地在加入5-60质量份平滑剂和/或其它药物赋形剂之后，或通过加入水和/或将其中含有碱性活性成分和聚合有机酸的混合物转化为液体悬浮液 任选的赋形剂。

公开(公告)号：US5087447A

公开(公告)日：1992-02-11

申请号：US420280

申请日：1989-10-12

申请人： Istvan Racz ,  Janos Plachy ,  Peter Szentmiklost

发明人： Istvan Racz ,  Janos Plachy ,  Peter Szentmiklost

IPC分类号： A61K9/00 ,  A61K9/16 ,  A61K9/20 ,  A61K9/22 ,  A61K33/08

CPC分类号： A61K9/0095 ,  A61K33/08 ,  A61K9/1635 ,  A61K9/1652 ,  A61K9/2027 ,  A61K9/2054 ,  A61K9/2072 ,  A61K9/2077

摘要： The invention relates to a new pharmaceutical preparation of high acid-binding capacity, of delayed effect, of increased bioavailability for neutralization of gastric acid and optionally to other pharmaceutical preparations acting in the gastrointestinal tract, first of all of laxative effect by mixing 100 parts by mass of a powdered basic magnesium compound or the powdered mixture of basic magnesium compounds and basic aluminium compounds with 2-2500 parts of a dry or swollen organic acid of polymeric character and therapeutically acceptable, e.g. cellulose-glycolic acid, starch-glycolic acid or polymer acrylic and/or methacrylic acid, letting this powdered mixture to stand for 1-24 hours at the temperature of 20.degree.-80.degree. C. after addition of 50-500 parts by mass of water and forming tablets or other pharmaceutical preparations, optionally after addition of 5-60 parts by mass of smoothing agents and/or other pharmaceutical excipients, or transforming the mixture containing the basic active ingredients and the polymeric organic acid in liquid suspension by adding water and optionally excipients.