Abstract：
One of the most common forms of controlled release technology for oral drug delivery comprises an active ingredient dispersed in a hydrophilic matrix forming polymer such as hydroxypropyl methylcellulose (HPMC), which is tableted via direct compression. However, HPMC may pose problems in direct compression due to its poor flowability. Hence, mannitol syrup was spray-coated over fluidized HPMC particles to produce co-processed HPMC-mannitol at ratios of 20:80, 50:50, and 70:30. Particles of pure HPMC, co-processed HPMC-mannitol, and their respective physical mixtures were evaluated for powder flowability, compression profiles, and controlled release performance. It was found that co-processed HPMC-mannitol consisted of particles with improved flow compared to pure HPMC particles. Sufficiently strong tablets of >2 MPa could be produced at moderate to high compression forces of 150-200 MPa. The dissolution profile could be tuned to obtain desired release profiles by altering HPMC-mannitol ratios. Co-processed HPMC-mannitol offers an interesting addition to the formulator\'s toolbox in the design of controlled release formulations for direct compression.
摘要：
用于口服药物递送的控释技术的最常见形式之一包括分散在亲水性基质形成聚合物如羟丙基甲基纤维素(HPMC)中的活性成分。这是通过直接压缩制表。然而,HPMC由于其差的流动性而可能在直接压缩中造成问题。因此，将甘露醇糖浆喷涂在流化HPMC颗粒上,以20:80、50:50和70:30的比率产生共处理的HPMC-甘露醇。纯HPMC颗粒，共处理HPMC-甘露醇，并对各自的物理混合物进行粉末流动性评价，压缩轮廓，和控制释放性能。发现与纯HPMC颗粒相比,共处理的HPMC-甘露醇由具有改善的流动性的颗粒组成。在150-200MPa的中等至高压缩力下,可以生产>2MPa的足够强的片剂。可以通过改变HPMC-甘露醇比率来调节溶出曲线以获得期望的释放曲线。共加工HPMC-甘露醇在设计用于直接压缩的控释制剂时，为配方设计师的工具箱提供了有趣的补充。
