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    • 1. 发明授权
    • Solid oral pharmaceutical product with increased efficacy and
predetermined steady state of solubility
    • 固体口服药物具有增加的疗效和预定的稳定状态的溶解度
    • US4199560A
    • 1980-04-22
    • US952932
    • 1978-10-19
    • Laszlo GyarmatiIstvan RaczPeter SzentmiklosiJanos Plachy
    • Laszlo GyarmatiIstvan RaczPeter SzentmiklosiJanos Plachy
    • A61K9/16A61K9/20A61K9/22A61K9/48A61K9/26A61K9/54A61K33/06
    • A61K9/1652A61K9/1617A61K9/2077A61K9/4841
    • 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.
    • 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。
    • 2. 发明授权
    • Proceeding for the production of pharmaceutical preparations of high
gastric acid binding capacity, of retarded effect and of increased
bioavailability
    • 开展生产具有高胃酸结合能力,延迟作用和提高生物利用度的药物制剂
    • US4921707A
    • 1990-05-01
    • US165102
    • 1988-03-28
    • Istvan RaczJanos PlachyPeter Szentmiklosi
    • Istvan RaczJanos PlachyPeter Szentmiklosi
    • A61K9/00A61K9/16A61K9/20A61K9/22A61K33/08
    • A61K9/0095A61K33/08A61K9/1635A61K9/1652A61K9/2027A61K9/2054A61K9/2072A61K9/2077
    • 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.
    • 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。
    • 8. 发明授权
    • Stabilized plant protecting carbofuran suspensions
    • 稳定植物保护呋喃丹悬浮液
    • US4734432A
    • 1988-03-29
    • US831467
    • 1986-02-19
    • Andras SzegoViktoria PeterdiFerenc KovatsJozsef SosIstvan RaczSandor ngyanKatalin Marmarosi nee Kellner
    • Andras SzegoViktoria PeterdiFerenc KovatsJozsef SosIstvan RaczSandor ngyanKatalin Marmarosi nee Kellner
    • A01N47/18A01N25/04A01N47/22A01N43/08
    • A01N25/04
    • The present invention relates to a stabilized plant protecting agent suspension which can be characterized by containing 10 to 60% by weight of one or more active ingredients, 30 to 5% by weight of oily layer, 0 to 10% by weight of emulsifier, 10 to 20% by weight of conventionally used excipient and water needed to 100% by weight while by increasing solid concentration oil concentration decreases. The invention also provides a process for the preparation of a stabilized plant protecting agent suspension by adding oil and optionally an emulsifier and/or water containing layer to a suspension of a suitable particle size of the active ingredient and water soluble excipients, such as surfactants, optionally emulsifiers, dispersing agents, viscosity modifying agents, protective colloids and mixing together the suspension layer and the layer containing the oil with a stirrer of great shearing force and optionally adding to the obtained stabilized suspension further excipients, e.g. viscosity modifying agents, anti-foaming agent, protective colloid and dispersing agent.
    • 本发明涉及稳定的植物保护剂悬浮液,其特征在于含有10至60重量%的一种或多种活性成分,30至5重量%的油层,0至10重量%的乳化剂,10 至20重量%的常规使用的赋形剂和水需要100重量%,同时通过提高固体浓度油浓度降低。 本发明还提供了一种制备稳定的植物保护剂悬浮液的方法,其通过将油和任选的乳化剂和/或含水层加入到适合的粒度的活性成分和水溶性赋形剂如表面活性剂的悬浮液中, 任选的乳化剂,分散剂,粘度调节剂,保护胶体,并将悬浮液层和含有油的层与具有大剪切力的搅拌器混合在一起,并任选地将所得稳定悬浮液中的其它赋形剂 粘度调节剂,消泡剂,保护胶体和分散剂。
    • 9. 发明授权
    • Stabilized plant protecting agent suspension
    • 稳定植物保护剂悬浮液
    • US4826863A
    • 1989-05-02
    • US84986
    • 1987-08-12
    • Andras SzegoViktoria PeterdiFerenc KovatsJozsef SosIstvan RaczSandor ngyanKatalin Marmarosi nee Kellner
    • Andras SzegoViktoria PeterdiFerenc KovatsJozsef SosIstvan RaczSandor ngyanKatalin Marmarosi nee Kellner
    • A01N47/18A01N25/04A01N47/22A01N43/52
    • A01N25/04
    • The present invention relates to a stabilized plant protecting agent suspension which can be characterized by containing 10 to 60% by weight of one or more active ingredients, 30 to 5% by weight of oily layer, 0 to 10% by weight of emulsifyer, 10 to 20% by weight of conventionally used excipient and water needed to 100% by weight while by increasing solid concentration oil concentration decreases.The invention also provides a process for the preparation of a stabilized plant protecting agent suspension by adding oil and optionally an emulsifyer and/or water containing layer to a suspension of a suitable particle size of the active ingredient and water soluble excipients, such as surfactants, optionally emulsifiers, dispersing agents, viscosity modifying agents, protective colloids and mixing together the suspension layer and the layer containing the oil with a stirrer of great shearing force and optionally adding to the obtained stabilized suspension further excipients, e.g. viscosity modifying agents, anti-foaming agent, protective colloid and dispersing agent.
    • 本发明涉及一种稳定的植物保护剂悬浮液,其特征在于含有10至60重量%的一种或多种活性成分,30至5重量%的油层,0至10重量%的乳化剂,10 至20重量%的常规使用的赋形剂和水需要100重量%,同时通过提高固体浓度油浓度降低。 本发明还提供了一种制备稳定的植物保护剂悬浮液的方法,其通过将油和任选的乳化剂和/或含水层添加到适合粒度的活性成分和水溶性赋形剂如表面活性剂的悬浮液中, 任选的乳化剂,分散剂,粘度调节剂,保护胶体,并将悬浮液层和含有油的层与具有大剪切力的搅拌器混合在一起,并任选地将所得稳定悬浮液中的其它赋形剂 粘度调节剂,消泡剂,保护胶体和分散剂。