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Pharmacokinetic and pharmacodynamic aspects of gastroretentive dosage forms

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  • Additional Information
    • Affiliation:
      a Department of Pharmaceutics, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, P.O. Box 12065, Jerusalem 91120, Israel
      b Clinical Sciences Department, The School of Veterinary Medicine, The Hebrew University of Jerusalem, Rehovot 76100, Israel
    • Keywords:
      Gastroretentive dosage forms
      Pharmacokinetics
      Pharmacodynamics
      Controlled release
      Bioavailability
      Metformin
      Levodopa
      Riboflavin
    • Abstract:
      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.
    • ISSN:
      0378-5173
    • Accession Number:
      10.1016/j.ijpharm.2003.09.047
    • Accession Number:
      S037851730400122X
    • Copyright:
      Copyright @ 2004 Elsevier B.V. All rights reserved.
  • Citations
    • ABNT:
      HOFFMAN, A. et al. Pharmacokinetic and pharmacodynamic aspects of gastroretentive dosage forms. International Journal of Pharmaceutics, [s. l.], v. 277, n. 1, p. 141–153, 2004. DOI 10.1016/j.ijpharm.2003.09.047. Disponível em: http://search.ebscohost.com/login.aspx?direct=true&site=eds-live&db=edselp&AN=S037851730400122X&custid=s8280428. Acesso em: 27 fev. 2020.
    • AMA:
      Hoffman A, Stepensky D, Lavy E, Eyal S, Klausner E, Friedman M. Pharmacokinetic and pharmacodynamic aspects of gastroretentive dosage forms. International Journal of Pharmaceutics. 2004;277(1):141-153. doi:10.1016/j.ijpharm.2003.09.047.
    • APA:
      Hoffman, A., Stepensky, D., Lavy, E., Eyal, S., Klausner, E., & Friedman, M. (2004). Pharmacokinetic and pharmacodynamic aspects of gastroretentive dosage forms. International Journal of Pharmaceutics, 277(1), 141–153. https://doi.org/10.1016/j.ijpharm.2003.09.047
    • Chicago/Turabian: Author-Date:
      Hoffman, Amnon, David Stepensky, Eran Lavy, Sara Eyal, Eytan Klausner, and Michael Friedman. 2004. “Pharmacokinetic and Pharmacodynamic Aspects of Gastroretentive Dosage Forms.” International Journal of Pharmaceutics 277 (1): 141–53. doi:10.1016/j.ijpharm.2003.09.047.
    • Harvard:
      Hoffman, A. et al. (2004) ‘Pharmacokinetic and pharmacodynamic aspects of gastroretentive dosage forms’, International Journal of Pharmaceutics, 277(1), pp. 141–153. doi: 10.1016/j.ijpharm.2003.09.047.
    • Harvard: Australian:
      Hoffman, A, Stepensky, D, Lavy, E, Eyal, S, Klausner, E & Friedman, M 2004, ‘Pharmacokinetic and pharmacodynamic aspects of gastroretentive dosage forms’, International Journal of Pharmaceutics, vol. 277, no. 1, pp. 141–153, viewed 27 February 2020, .
    • MLA:
      Hoffman, Amnon, et al. “Pharmacokinetic and Pharmacodynamic Aspects of Gastroretentive Dosage Forms.” International Journal of Pharmaceutics, vol. 277, no. 1, Jan. 2004, pp. 141–153. EBSCOhost, doi:10.1016/j.ijpharm.2003.09.047.
    • Chicago/Turabian: Humanities:
      Hoffman, Amnon, David Stepensky, Eran Lavy, Sara Eyal, Eytan Klausner, and Michael Friedman. “Pharmacokinetic and Pharmacodynamic Aspects of Gastroretentive Dosage Forms.” International Journal of Pharmaceutics 277, no. 1 (January 1, 2004): 141–53. doi:10.1016/j.ijpharm.2003.09.047.
    • Vancouver/ICMJE:
      Hoffman A, Stepensky D, Lavy E, Eyal S, Klausner E, Friedman M. Pharmacokinetic and pharmacodynamic aspects of gastroretentive dosage forms. International Journal of Pharmaceutics [Internet]. 2004 Jan 1 [cited 2020 Feb 27];277(1):141–53. Available from: http://search.ebscohost.com/login.aspx?direct=true&site=eds-live&db=edselp&AN=S037851730400122X&custid=s8280428