Controlled release formulation having a preformed passageway
    91.
    发明授权
    Controlled release formulation having a preformed passageway 失效
    具有预制通道的控制释放制剂

    公开(公告)号:US5654005A

    公开(公告)日:1997-08-05

    申请号:US476455

    申请日:1995-06-07

    IPC分类号: A61K9/00 A61K9/22 A61K9/36

    CPC分类号: A61K9/0004

    摘要: A controlled release pharmaceutical tablet having at least one passageway, said tablet having:(a) a compressed core which comprises:(i) a medicament;(ii) an amount of a water soluble osmotic agent which is effective to cause the medicament to be delivered from said passageway in the presence of aqueous media;(iii) a water-swellable pharmaceutically acceptable polymer; and(b) a membrane coating around said core tablet which comprises a water insoluble pharmaceutically acceptable polymer.

    摘要翻译: 一种具有至少一个通道的控释药物片剂,所述片剂具有:(a)压缩芯,其包含:(i)药物; (ii)一定量的水溶性渗透剂,其有效地引起药物在水介质存在下从所述通道递送; (iii)水溶胀性药学上可接受的聚合物; 和(b)围绕所述芯片的膜包衣,其包含水不溶性的药学上可接受的聚合物。

    Diffusion-osmotic controlled drug-release pharmaceutical composition and
process for preparing same
    94.
    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

    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。

    Controlled release nifedipine delivery device
    95.
    发明授权
    Controlled release nifedipine delivery device 失效
    控释硝苯地平递送装置

    公开(公告)号:US5543154A

    公开(公告)日:1996-08-06

    申请号:US327083

    申请日:1994-10-21

    摘要: A device for the controlled delivery of a beneficial agent as a gelatinous dispersion consisting of (i) a core which contains a beneficial agent, a polymer which forms gelatinous micoroscopic particles upon hydration and if desired an agent to modulate the hydration of the polymer; and (ii) an impermeable, insoluble coating which adheres to and surrounds the core and contains apertures which provide an area for the hydration and release of a disperson comprising gelatinous microscopic particles.

    摘要翻译: 用于作为凝胶状分散体受控输送有益剂的装置,其包含(i)含有有益试剂的核心,在水合时形成凝胶状微观观察颗粒的聚合物,如果需要,调节聚合物水合的试剂; 和(ii)不渗透的不溶性涂层,其粘附并包围芯并且包含孔,其提供用于水合和释放包含凝胶状微观颗粒的分散体的区域。

    Method for preparing aqueous emulsion for coating solid pharmaceutical
preparations
    99.
    发明授权
    Method for preparing aqueous emulsion for coating solid pharmaceutical preparations 失效
    制备用于涂布固体药物制剂的水性乳液的方法

    公开(公告)号:US5512092A

    公开(公告)日:1996-04-30

    申请号:US420569

    申请日:1995-04-12

    摘要: A method for preparing an aqueous emulsion for coating solid pharmaceutical preparations comprises the steps of dissolving a cellulosic polymer in a mixed solvent of water and an organic solvent capable of being admixed with water in any rate to give a polymer solution, self-emulsifying the polymer solution by mixing with water and then concentrating the resulting emulsified stock solution. The concentration is carried out by removing a part of the liquid components while passing it through a membrane for ultrafiltration till the polymer concentration of the resulting emulsion reaches a level of not less than 7% by weight.

    摘要翻译: 制备用于涂布固体药物制剂的水性乳液的方法包括以下步骤:将纤维素聚合物溶解在水和有机溶剂的混合溶剂中,所述混合溶剂能够以任何速率与水混合,得到聚合物溶液,自乳化聚合物 溶液与水混合,然后浓缩得到的乳化原液。 通过除去一部分液体成分,同时使其通过用于超滤的膜直到所得乳液的聚合物浓度达到不小于7重量%的水平来进行浓缩。

    Dosage forms having zero-order dihydropyridine calcium antagonist release
    100.
    发明授权
    Dosage forms having zero-order dihydropyridine calcium antagonist release 失效
    剂型具有零级二氢吡啶钙拮抗剂释放

    公开(公告)号:US5439687A

    公开(公告)日:1995-08-08

    申请号:US14836

    申请日:1993-02-08

    申请人: Sabine Compassi

    发明人: Sabine Compassi

    摘要: Pharmaceutical dosage forms having a linear release rate of the 0.sup.th order for the once-daily oral administration of 20-120 mg of nifedipine or of another calcium antagonist of the dihydropyridine type, characterised by a homogeneous matrix containing 2-50% by weight of hydroxypropylmethylcellulose having an average molecular weight of 20,000-250,000, 5-60% by weight of a calcium antagonist of the dihydropyridine type, as well as customary excipients compatible with the formulation, such as lipophilic or hydrophilic liberation controllers, fillers, flow-regulating agents, lubricants and, optionally, film coatings.

    摘要翻译: 线性释放速率为每日一次口服20-120毫克硝苯吡啶或其他二氢吡啶类钙拮抗剂的线性释放速率,其特征在于含有2-50重量%的羟丙基甲基纤维素 平均分子量为20,000-250,000,5-60重量%的二氢吡啶类型的钙拮抗剂,以及与制剂相容的常规赋形剂,例如亲油或亲水释放控制剂,填充剂,流动调节剂, 润滑剂和任选的膜涂料。