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    • 6. 发明授权
    • Orally administered drug delivery system providing temporal and spatial control
    • 口服给药系统提供时间和空间控制
    • US06960356B1
    • 2005-11-01
    • US09347315
    • 1999-07-02
    • Naresh TalwarHimadri SenJohn N. Staniforth
    • Naresh TalwarHimadri SenJohn N. Staniforth
    • A61K9/00A61K9/22A61K9/26A61K9/28A61K9/46A61K9/52A61K31/496
    • A61K9/0065A61K31/496
    • A pharmaceutical composition in the form of tablets or capsules provides a combination of temporal and spatial control of drug delivery to a patient for effective therapeutic results. The pharmaceutical composition comprises a drug, a gas generating component, a swelling agent, a viscolyzing agent, and optionally a gel forming polymer. The swelling agent belongs to a class of compounds known as superdisintegrants (e.g., cross-linked polyvinylpyrrolidone or sodium carboxymethylcellulose). The viscolyzing agent initially and the gel forming polymer thereafter form a hydrated gel matrix which entraps the gas, causing the tablet or capsule to be retained in the stomach or upper part of the small intestine (spatial control). At the same time, the hydrated gel matrix creates a tortuous diffusion path for the drug resulting in sustained release of the drug (temporal control). A preferred once daily ciprofloxacin formulation comprises 69.9% profloxacin base, 0.34% sodium alginate, 1.103% xanthan gum, 13.7% sodium bicarbonate, 12.1% cross-linked polyvinylpyrrolidone, and optionally other pharmaceutical xcipients, the formulation being in the form of a coated or uncoated tablet or capsule.
    • 片剂或胶囊形式的药物组合物提供药物递送到患者的时间和空间控制的组合以获得有效的治疗结果。 药物组合物包含药物,气体发生组分,溶胀剂,粘稠剂和任选的凝胶形成聚合物。 溶胀剂属于称为超级崩解剂的一类化合物(例如交联聚乙烯吡咯烷酮或羧甲基纤维素钠)。 最初的粘稠溶剂和凝胶形成聚合物之后形成一种水合凝胶基质,其夹带气体,导致片剂或胶囊保留在胃或小肠上部(空间对照)中。 同时,水合凝胶基质为药物产生曲折的扩散途径,导致药物的持续释放(时间控制)。 优选的每日一次环丙沙星制剂包含69.9%的表氟沙星碱,0.34%的藻酸钠,1.103%的黄原胶,13.7%的碳酸氢钠,12.1%的交联的聚乙烯吡咯烷酮,以及任选的其它药物xcipients,该制剂是涂层或 未包衣的片剂或胶囊。
    • 8. 发明授权
    • Orally administered controlled drug delivery system providing temporal and spatial control
    • 口服给药控制药物输送系统提供时间和空间控制
    • US06261601B1
    • 2001-07-17
    • US09152932
    • 1998-09-14
    • Naresh TalwarHimadri SenJohn N. Staniforth
    • Naresh TalwarHimadri SenJohn N. Staniforth
    • A61K946
    • A61K9/0065A61K31/496
    • A pharmaceutical composition in the form of tablets or capsules provides a combination of temporal and spatial control of drug delivery to a patient for effective therapeutic results. The pharmaceutical composition comprises a drug, a gas generating component, a swelling agent, a viscolyzing agent, and optionally a gel forming polymer. The swelling agent belongs to a class of compounds known as superdisintegrants (e.g., cross-linked polyvinylpyrrolidone or sodium carboxymethylcellulose). The viscolyzing agent initially and the gel forming polymer thereafter form a hydrated gel matrix which entraps the gas, causing the tablet or capsule to be retained in the stomach or upper part of the small intestine (spatial control). At the same time, the hydrated gel matrix creates a tortuous diffusion path for the drug, resulting in sustained release of the drug (temporal control). A preferred once daily ciprofloxacin formulation comprises 69.9% ciprofloxacin base, 0.34% sodium alginate, 1.03% xanthan gum, 13.7% sodium bicarbonate, 12.1% cross-linked polyvinylpyrrolidone, and optionally other pharmaceutical excipients, the formulation being in the form of a coated or uncoated tablet or capsule.
    • 片剂或胶囊形式的药物组合物提供药物递送到患者的时间和空间控制的组合以获得有效的治疗结果。 药物组合物包含药物,气体发生组分,溶胀剂,粘稠剂和任选的凝胶形成聚合物。 溶胀剂属于称为超级崩解剂的一类化合物(例如交联聚乙烯吡咯烷酮或羧甲基纤维素钠)。 最初的粘稠溶剂和凝胶形成聚合物之后形成一种水合凝胶基质,其夹带气体,导致片剂或胶囊保留在胃或小肠上部(空间对照)中。 同时,水合凝胶基质为药物产生曲折的扩散途径,导致药物的持续释放(时间控制)。 优选的每日一次环丙沙星制剂包含69.9%环丙沙星碱,0.34%藻酸钠,1.03%黄原胶,13.7%碳酸氢钠,12.1%交联聚乙烯吡咯烷酮和任选的其它药物赋形剂,该制剂呈涂层或 未包衣的片剂或胶囊。