TY - JOUR
T1 - Evolution of structure and properties of granules containing microcrystalline cellulose and polyvinylpyrrolidone during high-shear wet granulation
AU - Osei-Yeboah, Frederick
AU - Feng, Yushi
AU - Sun, Changquan Calvin
PY - 2014/1
Y1 - 2014/1
N2 - 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.
AB - 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.
KW - compaction
KW - excipients
KW - formulation
KW - granulation
KW - mechanical properties
KW - oral drug delivery
KW - particle engineering
KW - powder flow
KW - powder technology
KW - tableting
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U2 - 10.1002/jps.23776
DO - 10.1002/jps.23776
M3 - Article
C2 - 24218097
AN - SCOPUS:84890558496
SN - 0022-3549
VL - 103
SP - 207
EP - 215
JO - Journal of Pharmaceutical Sciences
JF - Journal of Pharmaceutical Sciences
IS - 1
ER -