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    • 7. 发明申请
    • Polymeric drug delivery system for hydrophobic drugs
    • 用于疏水药物的聚合物药物递送系统
    • US20050249799A1
    • 2005-11-10
    • US11072098
    • 2005-03-03
    • Jules JacobMichael BassettMarcus SchestopolEdith MathlowitzAvinash NangiaBennett CarterPeyman MoslemyZe'ev ShakedDavid EnscoreCourtney Sikes
    • Jules JacobMichael BassettMarcus SchestopolEdith MathlowitzAvinash NangiaBennett CarterPeyman MoslemyZe'ev ShakedDavid EnscoreCourtney Sikes
    • A61K9/00A61K9/14A61K9/16A61K9/20A61K9/24A61K9/28A61K9/48
    • A61K9/209A61K9/0065A61K9/1635A61K9/1641A61K9/1647A61K9/1652A61K9/1676A61K9/2054A61K9/2077A61K9/2086A61K9/2853
    • An oral delivery system for Class II drugs that have low oral bioavailability due to their insolubility in water and slow dissolution kinetics and method for making such a drug delivery system are disclosed herein. The formulation may be a controlled release or immediate release formulation. The immediate release formulation contains a Class II drug, together with a hydrophobic polymer, preferably a bioadhesive polymer. In one embodiment, the drug and polymer are co-dissolved in a common solvent. The solution is formed into small solid particles by any convenient method, particularly by spray drying. The resulting particles contain drug dispersed as small particles in a polymeric matrix. The particles are stable against aggregation, and can be put into capsules or tableted for administration. The controlled release formulations contain a BCS Class II drug and a bioadhesive polymer. The controlled release formulations may be in the form of a tablet, capsules, mini-tab, microparticulate, or osmotic pump. Enhancement of oral uptake of the drug from use of bioadhesive polymers occurs through (1) increased dissolution kinetics due to stable micronization of the drug, (2) rapid release of the drug from the polymer in the GI tract; and (3) prolonged GI transit due to bioadhesive properties of the polymers. The combination of these effects allows the preparation of a compact, stable dosage form suitable for oral administration of many class II drugs.
    • 本文公开了由于其在水中的不溶性和缓慢的溶解动力学以及制备这种药物递送系统的方法而具有低口服生物利用度的II类药物的口服递送系统。 制剂可以是控释或即时释放制剂。 立即释放制剂含有II类药物,以及疏水性聚合物,优选生物粘附性聚合物。 在一个实施方案中,将药物和聚合物共溶于常用溶剂。 通过任何方便的方法,特别是通过喷雾干燥,将溶液形成小的固体颗粒。 所得到的颗粒含有作为小颗粒分散在聚合物基质中的药物。 颗粒对聚集是稳定的,并且可以放入胶囊或压片以供给药。 控释制剂含有BCS II类药物和生物粘附性聚合物。 控制释放制剂可以是片剂,胶囊,迷你片,微粒或渗透泵的形式。 通过(1)由于药物的稳定的微粉化引起的溶出动力学增加,(2)药物从胃肠道中的聚合物快速释放,增加了使用生物粘附性聚合物对药物的口服摄取。 和(3)由于聚合物的生物粘合性质而延长GI运输。 这些作用的组合允许制备适于口服多种II类药物的紧凑,稳定的剂型。