Gordon M S, Rudraraju V S, Dani K, Chowhan Z T
Institute of Pharmaceutical Sciences, Syntex, Inc., Palo Alto, CA 94304.
J Pharm Sci. 1993 Feb;82(2):220-6. doi: 10.1002/jps.2600820222.
The effect of the mode of super disintegrant incorporation in wet granulated tablets was investigated with three super disintegrants: sodium starch glycolate, crospovidone, and croscarmellose sodium. The disintegrants were incorporated extragranularly or intragranularly or distributed equally between the two phases. Lactose, naproxen, or dibasic calcium phosphate was used as the principal tablet component to provide various degrees of solubility to the formulations. The formulations were dried to three different levels of moisture content. The results indicated that, for the formulations studied, extragranular incorporation resulted in faster dissolution than did equal distribution intragranularly and extragranularly, which in turn was superior to intragranular incorporation. Granulation moisture content was found to have a formulation-specific impact on tablet dissolution, with each main tablet component behaving in a different fashion. When all other factors were kept constant, there was a tendency for croscarmellose sodium to produce faster tablet dissolution than sodium starch glycolate or crospovidone. The super disintegrants tended to promote faster dissolution in a neutral pH medium than in an acidic medium.
采用三种超级崩解剂（羟丙基甲基纤维素、交联聚维酮和交联羧甲基纤维素钠）研究了其在湿法制粒片剂中的加入方式的影响。崩解剂以颗粒外加入、颗粒内加入或在两相之间均匀分布的方式加入。乳糖、萘普生或磷酸氢钙用作主要片剂成分，以使制剂具有不同程度的溶解性。将制剂干燥至三种不同的水分含量水平。结果表明，对于所研究的制剂，颗粒外加入会比颗粒内和颗粒外均匀分布导致更快的溶出，而颗粒内和颗粒外均匀分布又优于颗粒内加入。发现制粒水分含量对片剂溶出具有制剂特异性影响，每种主要片剂成分的表现方式不同。当所有其他因素保持恒定时，交联羧甲基纤维素钠比羟丙基甲基纤维素或交联聚维酮有使片剂溶出更快的趋势。超级崩解剂在中性pH介质中比在酸性介质中倾向于促进更快的溶出。
