An integrated model for determining causes of poor oral drug absorption

被引:141
作者
Yu, LX [1 ]
机构
[1] Glaxo Wellcome Inc, Res Triangle Pk, NC 27709 USA
关键词
small intestinal transit; dissolution; permeation; absorption; modeling;
D O I
10.1023/A:1018911728161
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Purpose. To develop an integrated absorption model for estimating the fraction of dose absorbed and determining the causes of poor oral drug absorption. Methods. Both analytical and numerical methods were used to estimate the fraction of dose absorbed. Results. An integrated absorption model was developed by considering transit flow, dissolution, and permeation processes, simultaneously. A framework was proposed to determine permeability-, dissolution- and solubility-limited absorption. Digoxin, griseofulvin, and panadiplon were employed to illustrate the applications of the integrated model in identifying the causes of poor absorption and guiding formulation development Conclusions. The integrated absorption model was successfully applied to digoxin, griseofulvin, and panadiplon to estimate the fraction dose absorbed and to roughly determine the causes of poor oral drug absorption.
引用
收藏
页码:1883 / 1887
页数:5
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