Pharmacokinetic and pharmacodynamic aspects of gastroretentive dosage forms

Amnon Hoffman*, David Stepensky, Eran Lavy, Sara Eyal, Eytan Klausner, Michael Friedman

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

124 Scopus citations


Controlled release gastroretentive dosage forms (CR-GRDF) enable prolonged and continuous input of the drug to the upper parts of the gastrointestinal (GI) tract and improve the bioavailability of medications that are characterized by a narrow absorption window. CR-GRDF provide a means to utilize all the pharmacokinetic (PK) and pharmacodynamic (PD) advantages of controlled release dosage forms for such drugs. Thus, CR-GRDF may improve therapy with clinically used medications, as well as enable oral administration of drugs, or drug candidates, that hitherto had to be infused parenterally. This manuscript discusses the complexity of the PK and PD factors that influence the treatment benefits of CR-GRDF and summarizes the results of our recent in vivo investigations in animal models (rats and dogs) and in human subjects. We found that a CR-GRDF formulation was superior to the other modes of administration for levodopa and riboflavin, but not for metformin. The PK and PD rationales of GRDFs for the studied drugs are presented and discussed. We conclude that due to the complexity of the PK and PD factors for a certain drug, the rationale for continuous administration obtained by CR-GRDF should be assessed and established in vivo.

Original languageAmerican English
Pages (from-to)141-153
Number of pages13
JournalInternational Journal of Pharmaceutics
Issue number1-2
StatePublished - 11 Jun 2004

Bibliographical note

Funding Information:
The study was supported by the Ministry of Science of Israel and Intec Pharmaceuticals (2000) Ltd. Professor Amnon Hoffman and Professor Michael Friedman are affiliated with the David R. Bloom Center for Pharmacy.


  • Bioavailability
  • Controlled release
  • Gastroretentive dosage forms
  • Levodopa
  • Metformin
  • Pharmacodynamics
  • Pharmacokinetics
  • Riboflavin


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