Collett J H, Koo L
J Pharm Sci. 1976 May;65(5):753-4. doi: 10.1002/jps.2600650535.
The in vitro dissolution and partitioning of some 4-substituted benzoic acids from nondisintegrating disks was investigated using a water-octanol system. The rates of appearance of benzoic acids in the aqueous phase differed from the rates of appearance in octanol, probably due to back-transfer from the octanol phase. The suitability of the procedure for investigating the influence of molecular modification on in vitro dissolution and partitioning is considered. Correlations among the rates of appearance in octanol, the rates of appearance in an aqueous phase, and substituent parameters of benzoic acids were investigated. The best statistical fit was obtained using molecular orbital substituent indexes.
使用水 - 辛醇体系研究了一些4 - 取代苯甲酸在非崩解盘上的体外溶解和分配情况。苯甲酸在水相中的出现速率与在辛醇中的出现速率不同，这可能是由于从辛醇相的反向转移所致。考虑了该方法对于研究分子修饰对体外溶解和分配影响的适用性。研究了苯甲酸在辛醇中的出现速率、在水相中的出现速率以及取代基参数之间的相关性。使用分子轨道取代基指数获得了最佳的统计拟合。
