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Enhanced Pharmacokinetic Properties of Oral and Parenteral Diclofenac-Cyclodextrin Delivery Systems

  • Lawrence J. Penkler
  • Darryl V. Whittaker
  • Luéta A. Glintenkamp
  • M. C. Bosch van Oudtshoorn

Abstract

The application of beta cyclodextrins to enhance the oral and parenteral delivery of the extensively used NSAID diclofenac sodium is described. Tablets containing microcrystalline 1:1 diclofenac sodium/beta-cyclodextrin complex prepared by kneading in a one pot ROTO granulator were formulated with an alkali agent. In a. single dose cross-over study (n=6) the test product yielded mean Tmax after 20 min compared with 40 min for the reference commercial non-enteric coated tablets, and showed more complete absorption. A stable 75mg/3mL aqueous solution of diclofenac sodium/2-hydroxypropyl-beta-cyclodextrin (1:2 mol/mol) was administered via im and iv injection to 6 volunteers. Relative to the commercial im reference product, the test showed significantly enhanced im and interesting iv pharmacokinetics.

Keywords

Reference Product Beta Cyclodextrin Sodium Starch Glycollate Field Proton Magnetic Resonance High Field Proton Magnetic Resonance 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

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Copyright information

© Springer Science+Business Media Dordrecht 1996

Authors and Affiliations

  • Lawrence J. Penkler
    • 1
  • Darryl V. Whittaker
    • 1
  • Luéta A. Glintenkamp
    • 1
  • M. C. Bosch van Oudtshoorn
    • 1
  1. 1.Druggists Group ResearchSouth African Druggists LimitedKorsten 6014, Port ElizabethSouth Africa

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