Controlled release pharmaceutical compositions containing tiagabine
    8.
    发明授权
    Controlled release pharmaceutical compositions containing tiagabine 失效
    包含噻加滨的控释药物组合物

    公开(公告)号:US06399100B1

    公开(公告)日:2002-06-04

    申请号:US09127210

    申请日:1998-07-31

    IPC分类号: A61K922

    摘要: Controlled release oral pharmaceutical preparations are provided which comprise a therapeutically effective amount of tiagabine or a pharmaceutically acceptable salt thereof dispersed in a rate controlling polymeric matrix comprising at least one rate controlling polymer. The preparation can be formulated into oral dosage forms such as tablets or multiparticulates which provide therapeutically effective plasma levels of tiagabine for a period of at least 12 hours, preferably 24 hours or more. The preparation can provide tiagabine mean plasma concentrations equal to or greater than 50% of the maximum plasma concentration for at least 10 hours, preferably 14 hours, most preferably 16 hours or more.

    摘要翻译: 提供了控制释放的口服药物制剂,其包含分散在包含至少一种速率控制聚合物的速率控制聚合物基质中的治疗有效量的噻加滨或其药学上可接受的盐。 该制剂可以配制成口服剂型,例如片剂或多颗粒,其提供治疗有效的噻加滨的血浆水平至少12小时,优选24小时或更长时间。 该制剂可以提供等于或大于最大血浆浓度的50%的替加滨平均血浆浓度至少10小时,优选14小时,最优选16小时或更长。

    Cisapride mini-tablet formulations
    9.
    发明授权
    Cisapride mini-tablet formulations 失效
    西沙必利微片剂

    公开(公告)号:US6110494A

    公开(公告)日:2000-08-29

    申请号:US995583

    申请日:1997-12-22

    摘要: A sustained release cisapride oral dosage formulation suitable for once-daily administration comprises a plurality of mini-tablets containing cisapride or a salt thereof with an organic acid and capable of releasing cisapride at different sites along the gastrointestinal tract. The mini-tablets include a proportion of immediate release tablets and a proportion of tablets which release cisapride in response to the pH environment at a given site in the distal regions of the gastrointestinal tract and which include cisapride or a salt thereof embedded in a matrix of hydrophilic polymer, said matrix being coated with a pH dependent polymer, the formulation having a Cmax/Cmin ratio under steady state conditions of 2:1 or less as evidenced by a substantially flat plasma profile in vivo.

    摘要翻译: 适用于每日一次给药的持续释放西沙必利口服剂量制剂包含多种含有西沙必利或其盐与有机酸并能够沿胃肠道不同部位释放西沙必利的微型片剂。 微型片剂包括一定比例的速释片剂和一定比例的片剂,其释放西沙必利,以响应于胃肠道远端区域中给定部位的pH环境,并且包括西沙必利或其嵌入基质中的盐 亲水性聚合物,所述基质涂覆有pH依赖性聚合物,所述制剂在2:1或更低的稳定状态条件下具有Cmax / Cmin比例,这通过体内基本上平坦的血浆曲线证明。

    Taste-masked formulations
    10.
    发明授权
    Taste-masked formulations 失效
    口味掩饰的配方

    公开(公告)号:US6153220A

    公开(公告)日:2000-11-28

    申请号:US163731

    申请日:1998-09-30

    摘要: A taste-masked micromatrix powder in which the ratio of a cationic copolymer synthesized form dimethylaminoethyl methacrylate and neutral methacrylic acid esters compared to a drug having poor organoleptic properties is greater than 2 to 1, preferably 4 to 1, most preferably 6 to 1 (wt/wt). Taste masked immediate release micromatrix powders can be formed by spray drying the drug and cationic copolymer whereas sustained release micromatrix powders can be formed by granulating controlled release powders, which can be made by spray drying the drug with a retarding polymer, with the cationic copolymer. The immediate release or sustained release taste-masked powders of this invention can be incorporated into conventional oral dosage forms such as sprinkles, suspension, fast melt tablets, chewable tablets or effervescent tablets.

    摘要翻译: 合成的甲基丙烯酸二甲基氨基乙酯和中性甲基丙烯酸酯的阳离子共聚物与具有不良感官特性的药物相比的比例大于2比1,优选4比1,最优选6比1(重量比)的掩味微米矩阵粉末 / wt)。 可以通过喷雾干燥药物和阳离子共聚物来形成口味掩蔽的立即释放微阵列粉末,而通过使用阳离子共聚物通过用延迟聚合物喷雾干燥药物来制备控释粉末,可以形成持续释放微阵列粉末。 本发明的立即释放或持续释放的掩味粉末可以掺入常规的口服剂型如洒剂,悬浮液,快速熔融片剂,咀嚼片剂或泡腾片剂中。