Johnson J R, Wang L H, Gordon M S, Chowhan Z T
Institute of Pharmaceutical Sciences, Syntex, Palo Alto, CA 94304.
J Pharm Sci. 1991 May;80(5):469-71. doi: 10.1002/jps.2600800514.
The effect of tablet formulation solubility and hygroscopicity on the dissolution efficiency of three "super disintegrants" (sodium starch glycolate, crospovidone, and croscarmellose sodium) in tablets prepared by wet granulation was investigated. Lactose, calcium phosphate dibasic, sorbitol, and naproxen sodium, alone or in combination, provided varying degrees of solubility and hygroscopicity in the formulations. To monitor in vitro dissolution, 1% p-aminobenzoic acid was added to the formulation as a tracer. The results indicate that highly soluble and/or hygroscopic ingredients decrease the effectiveness of super disintegrants in promoting in vitro dissolution. The greater the overall hygroscopicity and solubility of the tablet formulation, the larger the decrease in the efficiency of the super disintegrant.
研究了片剂配方的溶解性和吸湿性对三种“超级崩解剂”（羟丙基淀粉甘醇酸钠、交联聚维酮和交联羧甲基纤维素钠）在湿法制粒片剂中溶出效率的影响。乳糖、磷酸氢钙、山梨醇和萘普生钠单独或组合使用，在配方中提供了不同程度的溶解性和吸湿性。为监测体外溶出，向配方中加入1%的对氨基苯甲酸作为示踪剂。结果表明，高溶解性和/或吸湿性成分会降低超级崩解剂促进体外溶出的有效性。片剂配方的总体吸湿性和溶解性越高，超级崩解剂的效率下降幅度越大。
