Delta晶型甘露醇经物理改性后在口服固体制剂中的应用研究

Application of Delta-mannitol in Oral Solid Preparations after Physical Modification

对Delta-甘露醇在湿法制粒过程中发生物理改性的特性进行研究。用纯化水诱导Delta-甘露醇物理性质发生改变,采用XRPD、SEM进行表征;并载药布洛芬,设计不同处方进行压片试验,评价其片剂性能。在液体L/S为20%~30%时,XRPD表明Delta-甘露醇发生晶型转变,同时制备的颗粒紧实、致密;SEM显示Delta-甘露醇发生片状结构到微晶结构的形态学转变;在使用相同量甘露醇的片剂处方中,Delta-片具有更大的孔容积和比表面积;Delta-片的抗张强度明显高于Beta-片,Delta-片在60 min时累积溶出率高,且崩解时间短。Delta-甘露醇经水分诱导发生物理改性,对提高片剂的压缩性能有突出作用,同时也改善了片剂其它性能。

The characteristics of physical modification of delta mannitol in wet granulation were studied.The physical properties of delta mannitol were changed by purified water and characterized by XRPD and SEM;Different formulations of ibuprofen were designed for tablet compression test to evaluate its tablet performance.When the liquid L/S is 20% ~ 30%,XRPD shows that the crystal form of delta mannitol changes,and the prepared particles are compact and compact;SEM showed that the morphology of delta mannitol changed from flake structure to microcrystalline structure;In the tablet formulation using the same amount of mannitol,delta tablets have larger pore volume and specific surface area;The tensile strength of delta tablets was significantly higher than that of beta tablets.Delta tablets had high cumulative dissolution rate and short disintegration time at 60 min.The physical modification of delta mannitol induced by water not only plays a prominent role in improving the compression properties of tablets,but also improves other properties of tablets.