Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, Mercer University, Atlanta, Georgia 30341, USA.
AAPS PharmSciTech. 2010 Dec;11(4):1627-35. doi: 10.1208/s12249-010-9541-6. Epub 2010 Nov 18.
The objective of this work was to apply response surface approach to investigate main and interaction effects of formulation parameters in optimizing novel fast disintegrating tablet formulation using β cyclodextrin as a diluent. The variables studied were diluent (β cyclodextrin, X (1)), superdisintegrant (Croscarmellose sodium, X (2)), and direct compression aid (Spray dried lactose, X (3)). Tablets were prepared by direct compression method on B2 rotary tablet press using flat plain-face punches and characterized for weight variation, thickness, disintegration time (Y (1)), and hardness (Y (2)). Disintegration time was strongly affected by quadratic terms of β cyclodextrin, croscarmellose sodium, and spray-dried lactose. The positive value of regression coefficient for β cyclodextrin suggested that hardness increased with increased amount of β cyclodextrin. In general, disintegration of tablets has been reported to slow down with increase in hardness. However in the present study, higher concentration of β cyclodextrin was found to improve tablet hardness without increasing the disintegration time. Thus, β cyclodextrin is proposed as a suitable diluent to achieve fast disintegrating tablets with sufficient hardness. Good correlation between the predicted values and experimental data of the optimized formulation validated prognostic ability of response surface methodology in optimizing fast disintegrating tablets using β cyclodextrin as a diluent.
本工作旨在应用响应面法考察配方参数对新型速崩片的主效应和交互效应的影响，其中β-环糊精作为稀释剂。研究的变量为稀释剂（β-环糊精，X(1)）、超级崩解剂（交联羧甲基纤维素钠，X(2)）和直接压片赋形剂（喷雾干燥乳糖，X(3)）。采用 B2 旋转压片机，用平直面冲模直接压片，对片剂进行制备并进行重量差异、厚度、崩解时间（Y(1)）和硬度（Y(2)）的特性评价。崩解时间强烈受到β-环糊精、交联羧甲基纤维素钠和喷雾干燥乳糖的二次项的影响。β-环糊精的回归系数为正值，表明随着β-环糊精用量的增加，硬度增加。通常，据报道片剂的崩解速度随着硬度的增加而减慢。然而，在本研究中，发现较高浓度的β-环糊精可在不增加崩解时间的情况下提高片剂的硬度。因此，β-环糊精被提议作为一种合适的稀释剂，以获得具有足够硬度的速崩片。优化配方的预测值与实验数据之间的良好相关性验证了响应面法在优化使用β-环糊精作为稀释剂的速崩片中的预测能力。
