Department of Pharmaceutical Engineering, School of Pharmaceutical Sciences, University of Shizuoka, Shizuoka, Japan.
Eur J Pharm Biopharm. 2011 Aug;78(3):492-8. doi: 10.1016/j.ejpb.2011.01.014. Epub 2011 Feb 1.
To study the effect of glycerin fatty acid ester (Poem TR-FB) concentrations on the dissolution rate of acetaminophen (APAP), the dissolution and disintegration behaviors of APAP tablets formulated using various lubricants were examined. The change over time in the available surface area of APAP (S(t)), which is in direct contact with solvent, was also analyzed using these dissolution data. In the dissolution tests, a retarded dissolution of APAP was not observed with TR-FB, whereas magnesium stearate (Mg-St), which is widely used as a lubricant, retarded the dissolution. However, no significant difference in the disintegration time between the two lubricants was observed. With regard to the time course of the S(t), Mg-St at 0.1% gave a maximum surface area value at 9.19 min (peak time); however, the profiles for APAP with Mg-St at greater than 0.5% showed downward curvature indicating a gradual decrease in surface area over time. Conversely, with TR-FB, even when its concentration was increased, the S(t) profile for APAP had a maximum value that was more than twice that of APAP with that of 0.5-3.0% of Mg-St. Scanning electron microscopy (SEM) observations showed that the differences in the dissolution rate and S(t) patterns between Mg-St and TR-FB could be explained by differences in extensibility deriving from their morphology. Therefore, it was concluded that TR-FB does not cause retardation of drug dissolution and may prove to be a superior alternative lubricant to Mg-St.
为了研究甘油脂肪酸酯（Poem TR-FB）浓度对乙酰氨基酚（APAP）溶解速率的影响，考察了使用各种润滑剂制备的 APAP 片剂的溶解和崩解行为。还利用这些溶解数据分析了与溶剂直接接触的 APAP 可用表面积（S(t)）随时间的变化。在溶解试验中，TR-FB 没有观察到 APAP 的溶解延迟，而广泛用作润滑剂的硬脂酸镁（Mg-St）则延迟了溶解。然而，两种润滑剂的崩解时间没有显著差异。关于 S(t)的时间过程，0.1%的 Mg-St 在 9.19 分钟（峰值时间）给出最大表面积值；然而，Mg-St 浓度大于 0.5%的 APAP 的曲线显示出向下的曲率，表明表面积随时间逐渐减少。相反，即使 TR-FB 的浓度增加，APAP 的 S(t)曲线也具有最大值，是 Mg-St 浓度为 0.5-3.0%的 APAP 的两倍以上。扫描电子显微镜（SEM）观察表明，Mg-St 和 TR-FB 之间在溶解速率和 S(t)模式上的差异可以用它们形态衍生的延展性差异来解释。因此，结论是 TR-FB 不会导致药物溶解延迟，并且可能是比 Mg-St 更好的替代润滑剂。
