A new tablet brittleness index
A new tablet brittleness index
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DOI：
10.1016/j.ejpb.2015.04.007
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发表时间：
2015-06-01
影响因子：
4.9
通讯作者：
Sun, Changquan Calvin
中科院分区：
文献类型：
--
作者：
Gong, Xingchu;Sun, Changquan Calvin
脆性是影响粉末成形成败的重要材料性能之一。我们已经发现，在断裂处的径向弹性应变的倒数是最合适的片剂脆性指数（TBI）用于定量的药物片剂的脆性。基于新菌株的TBI得到理论考虑和脆碎度数据的系统统计分析的支持。它对片剂组成和压实参数的变化都足够敏感。对于所有测试材料，其正确地表明，对于相同粉末，片剂脆性随着片剂孔隙率的增加而增加。此外，TBI随着脆性赋形剂乳糖一水合物在与塑性赋形剂微晶纤维素的混合物中的含量增加而增加。构建了在片剂拉伸强度和TBI的各种组合下实现小于1%片剂脆碎度的概率图。来自市售片剂的数据验证了该概率图，推荐TBI值150作为药用片剂的上限。该TBI可根据片剂直径断裂试验期间常规获得的数据计算，该试验通常用于评估片剂机械强度。因此，由于其不需要额外的实验工作，因此可用于定量片剂脆性以指导片剂处方开发。(C)2015爱思唯尔B.V.保留所有权利。
Brittleness is one of the important material properties that influences the success or failure of powder compaction. We have discovered that the reciprocal of diametrical elastic strain at fracture is the most suitable tablet brittleness indices (TBIs) for quantifying brittleness of pharmaceutical tablets. The new strain based TBI is supported by both theoretical considerations and a systematic statistical analysis of friability data. It is sufficiently sensitive to changes in both tablet compositions and compaction parameters. For all tested materials, it correctly shows that tablet brittleness increases with increasing tablet porosity for the same powder. In addition, TBI increases with increasing content of a brittle excipient, lactose monohydrate, in the mixtures with a plastic excipient, microcrystalline cellulose. A probability map for achieving less than 1% tablet friability at various combinations of tablet tensile strength and TBI was constructed. Data from marketed tablets validate this probability map and a TBI value of 150 is recommended as the upper limit for pharmaceutical tablets. This TBI can be calculated from the data routinely obtained during tablet diametrical breaking test, which is commonly performed for assessing tablet mechanical strength. Therefore, it is ready for adoption for quantifying tablet brittleness to guide tablet formulation development since it does not require additional experimental work. (C) 2015 Elsevier B.V. All rights reserved.