Pharmacokinetics of intramuscular microparticle depot of valdecoxib in an experimental model.

We did a prospective study to investigate pharmacokinetics of a single intramuscularly (i.m.) administered Valdecoxib (VC) polymeric microparticles in New Zealand white rabbits.
Poly[lac(glc-leu)] microparticles encapsulating a potent cyclooxygenase-2- selective inhibitor, VC, were prepared by emulsion and solvent evaporation technique and administered i.m. to rabbits for pharmacokinetic study.
A single i.m. dose of drug-loaded poly[lac(glc-leu)] microparticles resulted in sustained therapeutic drug levels in the plasma for 49 days. The relative bioavailability was increased severalfold as compared with unencapsulated drug.
Injectable poly[lac(glc-leu)] microparticles hold promise for increasing drug bioavailability and reducing dosing frequency for better management of rheumatoid arthritis.
AuthorsSagar M Agnihotri, Pradeep R Vavia
JournalDrug development and industrial pharmacy (Drug Dev Ind Pharm) Vol. 35 Issue 9 Pg. 1043-7 (Sep 2009) ISSN: 1520-5762 [Electronic] England
PMID19365783 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Cyclooxygenase 2 Inhibitors
  • Delayed-Action Preparations
  • Excipients
  • Isoxazoles
  • Sulfonamides
  • valdecoxib
  • Animals
  • Area Under Curve
  • Biological Availability
  • Chromatography, High Pressure Liquid
  • Cyclooxygenase 2 Inhibitors (administration & dosage, pharmacokinetics)
  • Data Interpretation, Statistical
  • Delayed-Action Preparations
  • Dose-Response Relationship, Drug
  • Excipients
  • Half-Life
  • Injections, Intramuscular
  • Isoxazoles (administration & dosage, pharmacokinetics)
  • Microscopy, Electron, Scanning
  • Nanoparticles
  • Particle Size
  • Rabbits
  • Sulfonamides (administration & dosage, pharmacokinetics)

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