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Drug Investigation

, Volume 2, Supplement 4, pp 29–36 | Cite as

Biopharmaceutical Optimisation of β-Cyclodextrin Inclusion Compounds

  • D. Acerbi
  • G. Bovis
  • F. Carli
  • M. Pasini
  • L. Pavesi
  • T. Peveri
Article

Summary

To improve the biopharmaceutical performance of the nonsteroidal anti-inflammatory drug piroxicam, inclusion compounds with β-cyclodextrin carrier have been prepared and studied for a wide range of chemical, physical and pharmaceutical properties.

Three bulk products were obtained, 2 by a process of freeze-drying (preparation A/1 and preparation A/2) and changing process parameters, and 1 by spray-drying (preparation B). The objective was to obtain tablets which provide a rapid-release dosage form of piroxicam.

Studies were conducted in vitro and in humans and compared tablets of the inclusion complex of piroxicam and β-cyclodextrin with marketed oral and parenteral dosage forms of piroxicam. Significant differences were found in plasma levels, maximum plasma concentration (Cmax) and area under the plasma concentration-time curve (AUC), confirming that biopharmaceutical optimisation of the complexes can be achieved, leading to an overall pattern of absorption which is better than those presented by standard, non-complexed formulations of piroxicam (capsules, and ampoules for intramuscular use).

Evidence for a correlation between the 2 main physicopharmaceutical variables (solubilisation kinetics of the complex and dissolution rate of the tablet) and biopharmaceutical performances support the development of the product.

Keywords

Dissolution Rate Inclusion Complex Piroxicam Water Contact Angle Physical Mixture 
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

© Adis International Limited 1990

Authors and Affiliations

  • D. Acerbi
    • 1
  • G. Bovis
    • 1
  • F. Carli
    • 2
  • M. Pasini
    • 1
  • L. Pavesi
    • 1
  • T. Peveri
    • 2
  1. 1.Chemical and Biopharmaceutical Research LaboratoriesChiesi Farmaceutici SpAParmaItaly
  2. 2.Vectorpharma SpATriesteItaly

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