Warren J W, Price J C
J Pharm Sci. 1977 Oct;66(10):1406-9. doi: 10.1002/jps.2600661014.
Migration of a water-soluble drug, propoxyphene hydrochloride, during drying of tablet granulations was studied. Wet granulations of the drug were prepared using lactose as the major diluent and corn starch as a disintegrant. Particle-size fractions of lactose ranging from 53 to 177 micron in diameter were employed in different granulations to examine the effect of particle size of the major diluent on drug migration. Determination of drug concentration at various depths in a dried granulation bed was accomplished by using a drying cell consisting of four layers. A numerical coefficient of migration was developed to compare the extent of drug migration in the various lactose granulations. Migration increased with decreasing particle size of the major diluent, lactose. Two factors that may contribute to increased migration with smaller particles are increased entry suction due to decreased intragranular capillary size and increased intergranular contact area.
研究了水溶性药物盐酸丙氧芬在片剂制粒干燥过程中的迁移情况。以乳糖为主要稀释剂、玉米淀粉为崩解剂制备了该药物的湿颗粒。在不同制粒中使用直径范围为53至177微米的乳糖粒度级分，以研究主要稀释剂粒度对药物迁移的影响。通过使用由四层组成的干燥室来测定干燥颗粒床中不同深度处的药物浓度。开发了一个迁移数值系数来比较各种乳糖颗粒中药物的迁移程度。随着主要稀释剂乳糖粒度的减小，迁移增加。颗粒较小导致迁移增加的两个因素是：由于颗粒内毛细管尺寸减小而增加的进入吸力和增加的颗粒间接触面积。
