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    • 9. 发明授权
    • Extending the duration of drug release within the stomach during the fed mode
    • 在喂食模式期间延长胃内药物释放的持续时间
    • US06340475B2
    • 2002-01-22
    • US09282233
    • 1999-03-29
    • John W. ShellJenny Louie-HelmMicheline Markey
    • John W. ShellJenny Louie-HelmMicheline Markey
    • A61K926
    • A61K9/0065A61K9/2013A61K9/2031A61K9/205A61K9/2054
    • Drugs are formulated as unit oral dosage forms by incorporating them into polymeric matrices comprised of hydrophilic polymers that swell upon imbibition of water to a size that is large enough to promote retention of the dosage form in the stomach during the fed mode. The oral formulation is designed for gastric retention and controlled delivery of an incorporated drug into the gastric cavity, and thus administered, the drug is released from the matrix into the gastric fluid by solution diffusion. The swollen polymeric matrix, having achieved sufficient size, remains in the gastric cavity for several hours if administered while the patient is in the fed mode, and remains intact long enough for substantially all of the drug to be released before substantial dissolution of the matrix occurs. The swelling matrix lowers the accessibility of the gastric fluid to the drug and thereby reduces the drug release rate. This process, together with diffusion retardation by selection of specific polymers, polymer molecular weights, and other variables, results in a sustained and controlled delivery rate of the drug to the gastric cavity.
    • 将药物配制成单位口服剂型,通过将它们并入由亲水性聚合物组成的聚合物基质中,所述亲水性聚合物在吸水时膨胀至足够大以在给药模式期间促进剂型在胃中的保留。 口服制剂设计用于胃内保留和控制递送并入药物进入胃腔,并因此施用,通过溶液扩散将药物从基质释放到胃液中。 已经达到足够大小的溶胀的聚合物基质在患者处于喂养模式的同时在胃腔内保留数小时,并保持完整的时间足以使基本上所有的药物在基质溶解之前被释放出来 。 溶胀基质降低胃液对药物的可及性,从而降低药物释放速率。 该方法与通过选择特定聚合物,聚合物分子量和其他变量的扩散阻滞一起导致药物持续且受控制的胃腔输送速率。