Chowhan Z T, Amaro A A, Ong J T
Institute of Pharmaceutical Sciences, Syntex Research, Palo Alto, CA 94304.
J Pharm Sci. 1992 Mar;81(3):290-4. doi: 10.1002/jps.2600810320.
The tablet friability resulting from formulation variations was studied under controlled granulation moisture content and tablet crushing strength. Tablets made with lactose were more friable than tablets made with microcrystalline cellulose. Replacement of 0.5% magnesium stearate with 0.5% stearic acid in the formula reduced tablet friability, whereas the combination of 0.5% stearic acid and up to 0.25% magnesium stearate did not increase tablet friability, decrease drug dissolution rate, or increase tablet-to-tablet variability in dissolution. Tablets compressed with extra deep concave punches resulted in lower friability compared with tablets compressed with standard concave or deep concave punches. The friabilities of the standard convex and deep convex tablets were similar, indicating that a critical level of punch tip curvature was important in reducing tablet friability. The dissolution rate was not affected by the punch tip geometry, but the tablet-to-tablet dissolution variability at the 0.5% stearic acid level for the extra deep convex tablets was higher compared with the standard convex tablets.
在控制制粒水分含量和片剂抗压强度的条件下，研究了配方变化导致的片剂脆碎度。用乳糖制成的片剂比用微晶纤维素制成的片剂更脆。在配方中用0.5%的硬脂酸替代0.5%的硬脂酸镁可降低片剂脆碎度，而0.5%硬脂酸与高达0.25%硬脂酸镁的组合不会增加片剂脆碎度、降低药物溶出速率或增加片剂间溶出度的变异性。与用标准凹形或深凹形冲头压制的片剂相比，用超深凹形冲头压制的片剂脆碎度更低。标准凸形和深凸形片剂的脆碎度相似，表明冲头尖端曲率的临界水平对降低片剂脆碎度很重要。溶出速率不受冲头尖端几何形状的影响，但超深凸形片剂在0.5%硬脂酸水平下片剂间溶出度的变异性高于标准凸形片剂。
