Molecular inclusion of rofecoxib with cyclodextrin: pharmacological properties in laboratory animals

Pharmazie. 2004 Mar;59(3):233-4.

Abstract

Rofecoxib is practically insoluble in water and its prolonged use is associated with the incidence of side effects like gastrointestinal perforations, ulcerations and bleeding. Therefore, an attempt has been made to improve the aqueous solubility of the drug by making an inclusion complex using dimethyl-beta-cyclodextrin (DIMEB). The complexes were prepared by kneading and by the spray drying method. The prepared complexes showed better anti-inflammatory activity and decreased ulcerogenic potential than the pure drug.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Carrageenan
  • Cyclodextrins
  • Cyclooxygenase 2
  • Cyclooxygenase 2 Inhibitors
  • Cyclooxygenase Inhibitors / administration & dosage*
  • Cyclooxygenase Inhibitors / chemistry*
  • Cyclooxygenase Inhibitors / pharmacology
  • Drug Compounding
  • Edema / chemically induced
  • Edema / prevention & control
  • Excipients
  • Isoenzymes / metabolism
  • Lactones / administration & dosage*
  • Lactones / chemistry*
  • Lactones / pharmacology
  • Male
  • Prostaglandin-Endoperoxide Synthases / metabolism
  • Rats
  • Rats, Wistar
  • Stomach Ulcer / chemically induced
  • Stomach Ulcer / pathology
  • Sulfones

Substances

  • Cyclodextrins
  • Cyclooxygenase 2 Inhibitors
  • Cyclooxygenase Inhibitors
  • Excipients
  • Isoenzymes
  • Lactones
  • Sulfones
  • rofecoxib
  • Carrageenan
  • Cyclooxygenase 2
  • Prostaglandin-Endoperoxide Synthases