两种多形性纤维素修饰软压实制成包被微球的多单元微球体系(MUPS): MUPS中多形性修饰对崩解时间和药物释放的影响

V. Balzano, G. Betz, H. Leuenberger
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引用次数: 0

摘要

将UICEL-A/102和MCC - 102包覆颗粒压实成多单元颗粒系统(MUPS)。将MCC 102和UICEL-A/102分别与双氯芬酸钠混合,制成颗粒,然后用kolliccoat®SR 30d的水悬浮液包被,将30%-50%的包被颗粒包被在40%-60%的MCC 102粉末(缓冲液)和10%的STA-RX®1500或UICEL-A/102(崩解剂)中。最后,使用PressterTM压实模拟器将压片混合物压实成MUPS。与未压缩的亚基相比,uel - a /102和MCC 102 MUPS具有机械坚固性(破碎强度为70-100 N),在水中分解速度快,并保持相同的释放曲线和相似的表面和内部形态。UICEL-A/102被证明更适合作为立即释放微丸和MUPS的填充剂,而MCC 102被证实是MUPS控释微丸的有利填充剂。
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Multiple unit pellet systems (MUPS) obtained by soft compaction of two polymorphic cellulose modifications as coated pellets: influence of the polymorphic modification in MUPS on disintegration time and drug release
The compaction of UICEL-A/102 and MCC 102 coated pellets into multiple unit pellet systems (MUPS) is presented in this work. MCC 102 and UICEL-A/102 were separately mixed with sodium diclofenac, pelletised and afterwards coated with a water suspension of Kollicoat® SR 30 D. 30%-50% of the so produced coated pellets were embedded in 40%-60% of MCC 102 powder (cushioning) and 10% of either STA-RX® 1500 or UICEL-A/102 (disintegrant). Finally, the tabletting mixtures were compacted into MUPS using a PressterTM Compaction Simulator. Both UICEL-A/102 and MCC 102 MUPS resulted to be mechanically robust (crushing strength of 70-100 N), fast disintegrating in water and maintained the same release profile and similar superficial and inner morphology compared to the uncompressed subunits. UICEL-A/102 proved to be more appropriate as filler for immediate release pellets and MUPS, whereas MCC 102 confirmed to be advantageous filler for controlled release pellets in MUPS.
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