Transport approaches to the biopharmaceutical design of oral drug delivery systems: Prediction of intestinal absorption

被引:233
作者
Yu, LX
Lipka, E
Crison, JR
Amidon, GL
机构
[1] UNIV MICHIGAN, COLL PHARM, ANN ARBOR, MI 48109 USA
[2] TSRL INC, ANN ARBOR, MI 48108 USA
关键词
pH-partition hypothesis; absorption potential concept; mass balance approach; mixing tank; dispersion model; compartmental absorption and transit model;
D O I
10.1016/0169-409X(96)00009-9
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
For almost a half century scientists have striven to develop a theoretical model capable: of predicting oral drug absorption in humans. From the pH-partition hypothesis to the compartmental absorption and transit (CAT) model, various qualitative/quantitative approaches have been proposed, revised and extended. In this review, these models are classified into three categories; quasi-equilibrium models, steady-state models and dynamic models. The quasi-equilibrium models include the pH-partition hypothesis and the absorption potential concept, the steady-state models include the film model and the mass balance approaches, and the dynamic models include the dispersion, mixing tank and CAT models. The quasi-equilibrium models generally provide a basic guideline for understanding drug absorption trends. The steady-state models can be used to estimate the fraction of dose absorbed. The dynamic models predict both the fraction of dose absorbed and the rate of drug absorption and can be related to pharmacokinetic models to evaluate plasma concentration profiles.
引用
收藏
页码:359 / 376
页数:18
相关论文
共 59 条
[1]   PREDICTED ABSORPTION RATES WITH SIMULTANEOUS BULK FLUID-FLOW IN THE INTESTINAL-TRACT [J].
AMIDON, GE ;
HO, NFH ;
FRENCH, AB ;
HIGUCHI, WI .
JOURNAL OF THEORETICAL BIOLOGY, 1981, 89 (02) :195-210
[2]   ESTIMATING HUMAN ORAL FRACTION DOSE ABSORBED - A CORRELATION USING RAT INTESTINAL-MEMBRANE PERMEABILITY FOR PASSIVE AND CARRIER-MEDIATED COMPOUNDS [J].
AMIDON, GL ;
SINKO, PJ ;
FLEISHER, D .
PHARMACEUTICAL RESEARCH, 1988, 5 (10) :651-654
[3]   A THEORETICAL BASIS FOR A BIOPHARMACEUTIC DRUG CLASSIFICATION - THE CORRELATION OF IN-VITRO DRUG PRODUCT DISSOLUTION AND IN-VIVO BIOAVAILABILITY [J].
AMIDON, GL ;
LENNERNAS, H ;
SHAH, VP ;
CRISON, JR .
PHARMACEUTICAL RESEARCH, 1995, 12 (03) :413-420
[4]  
ANTONACCIO MJ, 1990, AM J CARDIOL, V65, pA12
[5]   THE VALIDATION OF THE INTESTINAL PERMEABILITY APPROACH TO PREDICT ORAL FRACTION OF DOSE ABSORBED IN HUMANS AND RATS [J].
CHIOU, WL .
BIOPHARMACEUTICS & DRUG DISPOSITION, 1995, 16 (01) :71-75
[6]  
Crison JR, 1992, PHARM RES-DORDR, V10, pS170
[7]  
CRISON JR, 1995, BIOINTERNATIONAL, V2, P301
[8]  
CRISON JR, 1993, THESIS U MICHIGAN
[9]  
DARGENIO DZ, 1992, ADAPT 2 MATH SOFTWAR
[10]   TRANSIT OF PHARMACEUTICAL DOSAGE FORMS THROUGH THE SMALL-INTESTINE [J].
DAVIS, SS ;
HARDY, JG ;
FARA, JW .
GUT, 1986, 27 (08) :886-892