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Biphasic controlled release delivery system for high solubility pharmaceuticals and method

机译:用于高溶解度药物的双相控释递送系统和方法

摘要

A biphasic controlled release delivery system for pharmaceuticals which have high water solubility, such as the antidiabetic metformin HCl salt, is provided which provides a dosage form that has prolonged gastric residence and includes (1) an inner solid particulate phase formed of substantially uniform granules containing a pharmaceutical having a high water solubility, and one or more hydrophilic polymers, one or more hydrophobic polymers and/or one or more hydrophobic materials such as one or more waxes, fatty alcohols and/or fatty acid esters, and (2) an outer solid continuous phase in which the above granules of inner solid particulate phase are embedded and dispersed troughout, the outer solid continuous phase including one or more hydrophilic polymers, one or more hydrophobic polymers and/or one or more hydrophobic materials such as one or more waxes, fatty alcohols and/or fatty acid esters, which may be compressed into tablets or filled into capsules. Methods for forming the so-described biphasic controlled release delivery system and using such biphasic controlled release delivery system for treating diabetes are also provided.
机译:提供了具有高水溶性的药物的双相控释递送系统,例如抗糖尿病的二甲双胍盐酸盐,其提供了具有延长的胃停留时间的剂型,并且包括(1)由基本上均匀的颗粒形成的内部固体颗粒相,其包含具有高水溶性的药物,以及一种或多种亲水性聚合物,一种或多种疏水性聚合物和/或一种或多种疏水性材料,例如一种或多种蜡,脂肪醇和/或脂肪酸酯,以及(2)外用固体内部连续相,其中上述内部固体颗粒相的颗粒被包埋并分散在槽中,外部固体连续相包括一种或多种亲水性聚合物,一种或多种疏水性聚合物和/或一种或多种疏水性材料,例如一种或多种蜡,脂肪醇和/或脂肪酸酯,它们可以压制成片剂或装入胶囊。还提供了形成所谓的双相控释递送系统并使用这种双相控释递送系统治疗糖尿病的方法。

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