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    • 5. 发明申请
    • AZITHROMYCIN DOSAGE FORMS WITH REDUCED SIDE EFFECTS
    • 阿奇霉素剂型减少副作用
    • WO2005053650A1
    • 2005-06-16
    • PCT/IB2004/001654
    • 2004-05-14
    • PFIZER PRODUCTS INC.HAGEN, Timothy, ArthurHERBIG, Scott, MaxLO, Julian, BelknapTHOMBRE, Avinash, GovindAPPEL, Leah, ElizabethCREW, Marshall, DavidFRIESEN, Dwayne, ThomasLYON, David, KeithMCCRAY, Scott, BaldwinWEST, James, Blair
    • HAGEN, Timothy, ArthurHERBIG, Scott, MaxLO, Julian, BelknapTHOMBRE, Avinash, GovindAPPEL, Leah, ElizabethCREW, Marshall, DavidFRIESEN, Dwayne, ThomasLYON, David, KeithMCCRAY, Scott, BaldwinWEST, James, Blair
    • A61K9/16
    • A61K9/1611A61K9/143A61K9/1617A61K9/1623A61K9/1635A61K9/1641A61K9/1694A61K9/2009A61K9/2013A61K9/2031A61K31/7052
    • 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.
    • 口服剂型包含阿奇霉素和有效量的碱化剂。 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,其中所述多颗粒包含阿奇霉素,单山gly酸甘油酯,二山ate酸甘油酯和三山gly酸甘油酯的混合物以及泊洛沙姆。 典型地,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剂,单位剂量小包或小药囊,片剂或胶囊。另外公开的是口服悬浮液,其包含阿奇霉素,有效量的碱化剂和 一辆车。 优选地,阿奇霉素为多颗粒形式,其中所述多颗粒包含阿奇霉素,单山gly酸甘油酯,二山ate酸甘油酯和三山gly酸甘油酯以及泊洛沙姆的混合物。 还公开了用于减少与阿奇霉素给予哺乳动物有关的胃肠副作用的方法,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,其中胃肠副作用的频率低于施用等剂量 进一步公开了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 另外公开的是阿奇霉素多微粒,其包含阿奇霉素,表面活性剂; 和药学上可接受的载体。