Ebel J P, Jay M, Beihn R M
Proctor & Gamble Company, Miami Valley Laboratories, Cincinnati, Ohio 45239-8707.
Pharm Res. 1993 Feb;10(2):233-8. doi: 10.1023/a:1018986827350.
An empirical mass-transfer model for enteric-coating dissolution that uses in vivo dissolution data to characterize the pH-dependent solubility properties of the polymer film and a mass-transfer coefficient determined from in vivo dissolution or disintegration studies is developed. Once the in vivo mass-transfer coefficient has been evaluated, it can be used in conjunction with in vitro dissolution data from other formulations to predict the in vivo time to disintegration and onset of drug release. Results of in vitro dissolution experiments using the USP basket dissolution apparatus and in vivo disintegration experiments using gamma scintigraphy with four enteric-coated pellet formulations are presented. The good agreement among the in vivo mass-transfer coefficients that were determined supports the validity of the model.
建立了一种肠溶包衣溶解的经验传质模型，该模型利用体内溶解数据来表征聚合物膜的pH依赖性溶解特性，并根据体内溶解或崩解研究确定传质系数。一旦评估了体内传质系数，就可以将其与其他制剂的体外溶解数据结合使用，以预测体内崩解时间和药物释放开始时间。给出了使用USP篮式溶解装置进行的体外溶解实验结果，以及使用γ闪烁扫描法对四种肠溶包衣微丸制剂进行的体内崩解实验结果。所确定的体内传质系数之间的良好一致性支持了该模型的有效性。
