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高剪切湿法制粒过程中含微晶纤维素和聚乙烯吡咯烷酮颗粒的结构与性质演变

Evolution of structure and properties of granules containing microcrystalline cellulose and polyvinylpyrrolidone during high-shear wet granulation.

作者信息

Osei-Yeboah Frederick, Feng Yushi, Sun Changquan Calvin

机构信息

Pharmaceutical Materials Science and Engineering Laboratory, Department of Pharmaceutics, College of Pharmacy, University of Minnesota, Minneapolis, Minnesota, 55455.

出版信息

J Pharm Sci. 2014 Jan;103(1):207-15. doi: 10.1002/jps.23776. Epub 2013 Nov 11.

Abstract

Granulation behavior of microcrystalline cellulose (MCC) in the presence of 2.5% polyvinylpyrrolidone (PVP) was systematically studied. Complex changes in flowability and tabletability of lubricated MCC granules are correlated to changes in intragranular porosity, morphology, surface smoothness, size distribution, and specific surface area (SSA). With 2.5% PVP, the use of 45% granulation water leads to 84% reduction in tablet tensile strength and 76% improvement in powder flow factor. The changes in powder performance are explained by granule densification and surface smoothing. The granulating water level corresponding to the onset of overgranulation, 45%, is significantly lower than the 70% water required for unlubricated MCC granules without PVP. At more than 45% water levels, MCC-PVP granules flow well but cannot be compressed into intact tablets. Such changes in powder performance correspond to the rapid growth into large and dense spheres with smooth surface. Compared with MCC alone, the onset of the phase of fast granule size enlargement occurs at a lower water level when 2.5% PVP is used. Although the use of 2.5% PVP hastens granule nucleation and growth rate, the mechanisms of overgranulation are the same, that is, size enlargement, granule densification, surface smoothing, and particle rounding in both systems.

摘要

系统研究了在2.5%聚乙烯吡咯烷酮(PVP)存在下微晶纤维素(MCC)的造粒行为。润滑后的MCC颗粒的流动性和可压性的复杂变化与颗粒内孔隙率、形态、表面光滑度、尺寸分布和比表面积(SSA)的变化相关。使用2.5%的PVP时,45%的制粒用水量会使片剂抗张强度降低84%,粉末流动因子提高76%。粉末性能的变化可以用颗粒致密化和表面光滑化来解释。对应过造粒起始点的制粒水水平为45%,明显低于无PVP的未润滑MCC颗粒所需的70%的水。当水水平超过45%时,MCC-PVP颗粒流动性良好,但无法压制成完整片剂。粉末性能的这种变化对应于快速生长成表面光滑的大而致密的球体。与单独的MCC相比,使用2.5%的PVP时,快速颗粒尺寸增大阶段的起始点出现在较低的水水平。虽然使用2.5%的PVP会加速颗粒成核和生长速率,但两个体系中的过造粒机制是相同的,即尺寸增大、颗粒致密化、表面光滑化和颗粒圆整化。

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