Reduced tabletability of roller compacted granules as a result of granule size enlargement
Reduced tabletability of roller compacted granules as a result of granule size enlargement
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DOI：
10.1002/jps.20531
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发表时间：
2006-01-01
影响因子：
3.8
通讯作者：
Himmelspach, MW
中科院分区：
文献类型：
--
作者：
Sun, CQ;Himmelspach, MW
使用微晶纤维素 (MCC) 详细研究了经常观察到的干粒 (DG) 粉末“丧失可再加工性或可压片性”的机制。据推测，颗粒尺寸增大是该现象的主要机制。根据片剂内颗粒间键合的物理模型，可以预测尺寸增大对塑料材料压片性的不利影响。在颗粒/颗粒不存在广泛破裂的情况下，较大颗粒/颗粒表现出可用于粘合的表面积较低，因此在相同条件下压缩时拉伸强度较低。首先使用具有不同粒度分布的不同等级的 MCC 粉末（整体粉末和筛分粉末）证明了尺寸效应。无论等级和筛分，较大的颗粒总是导致较低的可压片性，即在相同压实压力下较低的拉伸强度。随后表明，无论 MCC 的等级如何，颗粒的增大也会降低粉末的压片性。碾压 1 次、2 次和 4 次后的过筛颗粒的压片性随着颗粒尺寸的增加而单调下降，但与碾压总数无关。此外，细颗粒（44-106μm）的压片性高于粗MCC粉末（Avicel PH-200）。这些结果表明，MCC DG 颗粒压片性降低的主要机制是颗粒尺寸增大，而不是“加工硬化”。 (c) 2005 年 Wiley-Liss, Inc.
The mechanism for the frequently observed "loss of reworkability or tabletability" of dry-granulated (DG) powders was investigated in detail using microcrystalline cellulose (MCC). It was hypothesized that granule size enlargement is the primary mechanism to the phenomenon. Detrimental effects of size enlargement on tabletability of plastic materials are predictable based on the physical model of interparticulate bonding within a tablet. In absence of extensive fracture of particles/granules, larger particles/granules exhibit lower surface area available for bonding thus lower tensile strength when compressed under identical conditions. Size effects were first demonstrated using different grades of MCC powders, both whole and sieved, of different particle size distributions. Regardless grade and sieve fraction, larger particles always resulted in lower tabletability, that is, lower tensile strength at the same compaction pressure. It was subsequently shown that enlargement of granules also reduced powder tabletability regardless grade of MCC. Tabletability of sieved granules after roller compacted for one, two, and four times decreased monotonically with increasing granule size but independent of the total number of roller compaction. Moreover, tabletability of fine granules (44-106 mu m) was higher than that of coarse MCC powder (Avicel PH-200). These results suggest that the primary mechanism for reduced tabletabilty of DG granules of MCC is granule size enlargement rather than "work-hardening." (c) 2005 Wiley-Liss, Inc.