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    • 2. 发明授权
    • Stabilized compositions containing alkaline labile drugs
    • 含有碱性不稳定药物的稳定组合物
    • US08173152B2
    • 2012-05-08
    • US12294367
    • 2007-03-22
    • Michael W. CrowleyJustin M. KeenJohn J. KolengFeng Zhang
    • Michael W. CrowleyJustin M. KeenJohn J. KolengFeng Zhang
    • A61F13/02
    • A61K9/70A61K9/0024A61K9/006A61K9/7023A61K9/703A61K9/7069A61K9/7084A61K9/7092A61K31/4468A61K31/568A61K45/06A61K47/10A61L15/44A61L27/54A61L31/16A61L2300/602
    • A stabilized bioadhesive composition containing an alkaline labile drug and a method for its preparation are provided. In one aspect, the composition is a hot-melt extruded (HME) composition comprising a preformed excipient mixture comprising an acidic component and an alkaline thermoplastic matrix-forming material, e.g. polymer. The excipient mixture is formed before blending with an alkaline labile drug. The blend is then hot-melt extruded to form the HME composition. By so doing, the acidic component is able to neutralize or render moderately acidic the excipient mixture. This particular process has been shown to substantially reduce the degradation of an alkaline labile drug during hot-melt extrusion. The excipient mixture softens or melts during hot-melt extrusion. It can dissolve or not dissolve drug-containing particles during extrusion. Various functional excipients can be included in the carrier system to improve process performance and/or improve the chemical or physical properties of the HME composition.
    • 提供了含有碱性不稳定药物的稳定的生物粘合剂组合物及其制备方法。 在一个方面,组合物是热熔挤出(HME)组合物,其包含预先形成的赋形剂混合物,其包含酸性组分和碱性热塑性基质形成材料,例如, 聚合物。 赋形剂混合物在与碱性不稳定药物共混之前形成。 然后将共混物热熔融挤出以形成HME组合物。 通过这样做,酸性成分能够中和或赋予赋形剂混合物中度酸性。 已经显示了该特定方法,以显着降低热熔融挤出期间碱性不稳定药物的降解。 赋形剂混合物在热熔挤出过程中软化或熔化。 在挤出过程中可溶解或不溶解含药颗粒。 可以在载体体系中包括各种功能赋形剂以改善工艺性能和/或改善HME组合物的化学或物理性能。
    • 8. 发明授权
    • Stabilized compositions containing alkaline labile drugs
    • 含有碱性不稳定药物的稳定组合物
    • US08883187B2
    • 2014-11-11
    • US13463375
    • 2012-05-03
    • Michael M. CrowleyJustin M. KeenJohn J. KolengFeng Zhang
    • Michael M. CrowleyJustin M. KeenJohn J. KolengFeng Zhang
    • A61F2/02A61K9/00A61K31/568A61K9/70
    • A61K9/70A61K9/0024A61K9/006A61K9/7023A61K9/703A61K9/7069A61K9/7084A61K9/7092A61K31/4468A61K31/568A61K45/06A61K47/10A61L15/44A61L27/54A61L31/16A61L2300/602
    • A stabilized bioadhesive composition containing an alkaline labile drug and a method for its preparation are provided. In one aspect, the composition is a hot-melt extruded (HME) composition comprising a preformed excipient mixture comprising an acidic component and an alkaline thermoplastic matrix-forming material, e.g. polymer. The excipient mixture is formed before blending with an alkaline labile drug. The blend is then hot-melt extruded to form the HME composition. By so doing, the acidic component is able to neutralize or render moderately acidic the excipient mixture. This particular process has been shown to substantially reduce the degradation of an alkaline labile drug during hot-melt extrusion. The excipient mixture softens or melts during hot-melt extrusion. It can dissolve or not dissolve drug-containing particles during extrusion. Various functional excipients can be included in the carrier system to improve process performance and/or improve the chemical or physical properties of the HME composition.
    • 提供了含有碱性不稳定药物的稳定的生物粘合剂组合物及其制备方法。 在一个方面,组合物是热熔挤出(HME)组合物,其包含预先形成的赋形剂混合物,其包含酸性组分和碱性热塑性基质形成材料,例如, 聚合物。 赋形剂混合物在与碱性不稳定药物共混之前形成。 然后将共混物热熔融挤出以形成HME组合物。 通过这样做,酸性成分能够中和或赋予赋形剂混合物中度酸性。 已经显示了该特定方法,以显着降低热熔融挤出期间碱性不稳定药物的降解。 赋形剂混合物在热熔挤出过程中软化或熔化。 在挤出过程中可溶解或不溶解含药颗粒。 可以在载体体系中包括各种功能赋形剂以改善工艺性能和/或改善HME组合物的化学或物理性能。