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    Azithromycin dosage forms with reduced side effects
    9.
    发明申请
    Azithromycin dosage forms with reduced side effects 有权
    阿奇霉素剂型具有减少的副作用

    公开(公告)号：US20050123627A1

    公开(公告)日：2005-06-09

    申请号：US10763340

    申请日：2004-01-23

    申请人： Timothy Hagen ,  Julian Lo ,  Avinash Thombre ,  Scott Herbig ,  Leah Appel ,  Marshall Crew ,  Dwayne Friesen ,  David Lyon ,  Scott McCray ,  James West

    发明人： Timothy Hagen ,  Julian Lo ,  Avinash Thombre ,  Scott Herbig ,  Leah Appel ,  Marshall Crew ,  Dwayne Friesen ,  David Lyon ,  Scott McCray ,  James West

    IPC分类号： C07H17/00 ,  A61K9/00 ,  A61K9/16 ,  A61K9/20 ,  A61K31/7052 ,  A61K47/02 ,  A61K47/14 ,  A61K47/18 ,  A61K47/44 ,  A61P31/04 ,  A01N59/26 ,  A61K31/198 ,  A61K31/7008 ,  A61K33/10 ,  A61K33/42

    CPC分类号： A61K9/1611 ,  A61K9/143 ,  A61K9/1617 ,  A61K9/1623 ,  A61K9/1635 ,  A61K9/1641 ,  A61K9/1694 ,  A61K9/2009 ,  A61K9/2013 ,  A61K9/2031 ,  A61K31/7052

    摘要： An oral dosage form comprising azithromycin and an effective amount of an alkalizing agent. Preferably, said oral dosage form comprises an effective amount of an alkalizing agent and an azithromycin multiparticulate wherein said multiparticulate comprises azithromycin, a mixture of glyceryl monobehenate, glyceryl dibehenate and glyceryl tribehenate, and a poloxamer. Typically, the oral dosage form includes any suitable oral dosing means such as a powder for oral suspension, a unit dose packet or sachet, a tablet or a capsule. Additionally disclosed is an oral suspension comprising azithromycin, an effective amount of an alkalizing agent and a vehicle. Preferably, the azithromycin is in multiparticulate form wherein said multiparticulate comprises azithromycin, a mixture of glyceryl monobehenate, glyceryl dibehenate and glyceryl tribehenate, and a poloxamer. Also disclosed is a method for reducing gastrointestinal side effects, associated with administering azithromycin to a mammal, comprising contiguously administering azithromycin and an effective amount of alkalizing agent to said mammal wherein the frequency of gastrointestinal side effects is lower than that experienced by administering an equal dose of azithromycin without said alkalizing agent. Further disclosed is a method of treating a bacterial or protozoal infection in a mammal in need thereof comprising contiguously administering to said mammal a single dose of an oral dosage form wherein said oral dosage form comprises azithromycin and an effective amount of an alkalizing agent. Additionally disclosed are azithromycin multiparticulates comprising azithromycin, a surfactant; and a pharmaceutically acceptable carrier.

    摘要翻译： 包含阿奇霉素和有效量的碱化剂的口服剂型。 优选地，所述口服剂型包含有效量的碱化剂和阿奇霉素多颗粒，其中所述多颗粒包括阿奇霉素，单山嵛酸甘油酯，二苯乙酸甘油酯和枸橼酸甘油酯和泊洛沙姆的混合物。 通常，口服剂型包括任何合适的口服给药方式，例如用于口服悬浮液的粉末，单位剂量包或小药囊，片剂或胶囊。 另外公开了包含阿奇霉素，有效量的碱化剂和载体的口服悬浮液。 优选地，阿奇霉素是多颗粒形式，其中所述多颗粒包括阿奇霉素，甘油单山嵛酸甘油酯，二苯甲酸甘油酯和枸橼酸甘油酯和泊洛沙姆的混合物。 还公开了一种减少与向哺乳动物施用阿奇霉素相关的胃肠道副作用的方法，包括向所述哺乳动物连续施用阿奇霉素和有效量的碱化剂，其中胃肠道副作用的频率低于施用相等剂量 的阿奇霉素不含碱化剂。 进一步公开的是一种在有需要的哺乳动物中治疗细菌或原生动物感染的方法，其包括向所述哺乳动物连续施用单剂量的口服剂型，其中所述口服剂型包含阿奇霉素和有效量的碱化剂。 另外公开了包含阿奇霉素，表面活性剂的阿奇霉素多颗粒; 和药学上可接受的载体。

    Controlled release dosage forms of azithromycin
    10.
    发明申请
    Controlled release dosage forms of azithromycin 审中-公开
    阿奇霉素的控释剂型

    公开(公告)号：US20050123615A1

    公开(公告)日：2005-06-09

    申请号：US11003855

    申请日：2004-12-03

    申请人： Roderick Ray ,  Leah Appel ,  Dwayne Friesen ,  Marshall Crew ,  David Newbold

    发明人： Roderick Ray ,  Leah Appel ,  Dwayne Friesen ,  Marshall Crew ,  David Newbold

    IPC分类号： A61K9/16 ,  A61K31/7052 ,  A61K9/52 ,  A61K9/14

    CPC分类号： A61K9/145 ,  A61K9/146 ,  A61K9/1641 ,  A61K31/7052

    摘要： A process for forming multiparticulates of azithromycin and a controlled release dosage form comprising multiparticulates of azithromycin and a pharmaceutically acceptable excipient are disclosed. The dosage form decreases the incidence and/or severity of GI side effects relative to currently available immediate release azithromycin dosage forms that deliver an equivalent dose. The dosage forms operate by effecting azithromycin release at a rate sufficiently slow to ameliorate side effects, yet sufficiently fast to achieve good bioavailability.

    摘要翻译： 公开了形成阿奇霉素的多颗粒和包含阿奇霉素和药学上可接受的赋形剂的多颗粒的控制释放剂型的方法。 相对于递送相当剂量的目前可用的即时释放阿奇霉素剂型，剂型降低了GI副作用的发生率和/或严重性。 剂型通过以足够缓慢的速度实施阿奇霉素释放来改善副作用，但足够快以达到良好的生物利用度。