Que Li, Wu Wei, Cheng Xiaofeng, Hu Tao
Department of Pharmaceutics, School of Pharmacy, Fudan University, Shanghai, PR China.
Pharm Dev Technol. 2006;11(3):295-301. doi: 10.1080/10837450600767649.
A paddle method for measurement of the disintegrating time of orally disintegrating tablets with rizatriptan benzoate as a model drug was evaluated. The paddle method employed a dissolution test assembly with tablets immersed in disintegrating medium through a fastened sinker. Paddle stirring rate, opening of the sinker sieve, and tablet crushing strength influenced disintegrating time greatly. A logarithmic relationship was observed between disintegrating time and paddle revolution speed, while disintegrating time values and tablet crushing strength were fitted to a linear equation. The paddle method values with limited deviation were in good correlation with in vivo results. The paddle method was employed to optimize the disintegrating time of rizatriptan benzoate orally disintegrating tablets using a factorial design. The best-fit quadratic equation with a regression coefficient of 0.996 was highly predictive, which was indicative that the paddle method was precise and applicable in formulation optimization.
以苯甲酸利扎曲普坦为模型药物，对一种用于测量口腔崩解片崩解时间的桨法进行了评估。该桨法采用了一种溶出度测试装置，片剂通过固定的沉降片浸入崩解介质中。桨叶搅拌速率、沉降片筛网孔径和片剂抗压强度对崩解时间有很大影响。观察到崩解时间与桨叶转速之间呈对数关系，而崩解时间值与片剂抗压强度符合线性方程。偏差有限的桨法测定值与体内结果具有良好的相关性。采用桨法通过析因设计优化苯甲酸利扎曲普坦口腔崩解片的崩解时间。回归系数为0.996的最佳拟合二次方程具有高度预测性，这表明桨法精确且适用于制剂优化。
