Tuladhar M D, Carless J E, Summers M P
J Pharm Pharmacol. 1983 May;35(5):269-74. doi: 10.1111/j.2042-7158.1983.tb02932.x.
The dissolution rate of phenylbutazone from tablets after disintegration has been used to determine whether the drug particles underwent crushing or bonding during compression. Two polymorphic forms of the drug were used and the predominant effect for high drug concentration (60%), during compression was dependent upon the original particle size of the drug and its polymorphic form. With a low drug concentration (10%) in the tablet, the diluent protected the drug particles from bonding together. The particle size change of the drug during compression was affected by the nature of the diluent present. Lactose had an abrasive action on Form A phenylbutazone compared with Avicel but had little effect on the more ductile Form B. When the contact time of compression was decreased from 29 to 0.26 s, the 6 microns particles of drug showed less bonding at the shorter time (faster rate of compression) but the effect observed with the larger particles was independent the compression rate.
通过检测保泰松片剂崩解后的溶出速率，来确定药物颗粒在压片过程中是否发生了破碎或粘结。使用了该药物的两种多晶型形式，在压片过程中，高药物浓度（60%）时的主要影响取决于药物的原始粒径及其多晶型形式。片剂中药物浓度较低（10%）时，稀释剂可防止药物颗粒粘结在一起。压片过程中药物的粒径变化受所用稀释剂性质的影响。与微晶纤维素相比，乳糖对A型保泰松有研磨作用，但对更具延展性的B型保泰松影响较小。当压片接触时间从29秒减少到0.26秒时，6微米的药物颗粒在较短时间（更快的压片速度）下显示出较少的粘结，但较大颗粒观察到的效果与压片速度无关。
