NDLI: Time-Dependent Oral Absorption Models

Content Provider	Springer Nature Link
Author	Higaki, Kazutaka Yamashita, Shinji Amidon, Gordon L.
Copyright Year	2001
Abstract	The plasma concentration–time profiles following oral administration of drugs are often irregular and cannot be interpreted easily with conventional models based on first- or zero-order absorption kinetics and lag time. Six new models were developed using a time-dependent absorption rate coefficient, k$_{a}$(t), wherein the time dependency was varied to account for the dynamic processes such as changes in fluid absorption or secretion, in absorption surface area, and in motility with time, in the gastrointestinal tract. In the present study, the plasma concentration profiles of propranolol obtained in human subjects following oral dosing were analyzed using the newly derived models based on mass balance and compared with the conventional models. Nonlinear regression analysis indicated that the conventional compartment model including lag time (CLAG model) could not predict the rapid initial increase in plasma concentration after dosing and the predicted C$_{max}$ values were much lower than that observed. On the other hand, all models with the time-dependent absorption rate coefficient, k$_{a}$(t), were superior to the CLAG model in predicting plasma concentration profiles. Based on Akaike's Information Criterion (AIC), the fluid absorption model without lag time (FA model) exhibited the best overall fit to the data. The two-phase model including lag time, TPLAG model was also found to be a good model judging from the values of sum of squares. This model also described the irregular profiles of plasma concentration with time and frequently predicted C$_{max}$ values satisfactorily. A comparison of the absorption rate profiles also suggested that the TPLAG model is better at prediction of irregular absorption kinetics than the FA model. In conclusion, the incorporation of a time-dependent absorption rate coefficient k$_{a}$(t) allows the prediction of nonlinear absorption characteristics in a more reliable manner.
Starting Page	109
Ending Page	128
Page Count	20
File Format	PDF
ISSN	1567567X
Journal	Journal of Pharmacokinetics and Pharmacodynamics
Volume Number	28
Issue Number	2
e-ISSN	15738744
Language	English
Publisher	Kluwer Academic Publishers-Plenum Publishers
Publisher Date	2001-01-01
Publisher Place	New York
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	Pharmacology/Toxicology Pharmacy Veterinary Medicine Biochemistry Biomedical Engineering
Content Type	Text
Resource Type	Article
Subject	Pharmacology

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