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

Abstract

AIM:

We did a prospective study to investigate pharmacokinetics of a single intramuscularly (i.m.) administered Valdecoxib (VC) polymeric microparticles in New Zealand white rabbits.

METHOD:

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.

RESULTS:

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.

CONCLUSIONS:

Injectable poly[lac(glc-leu)] microparticles hold promise for increasing drug bioavailability and reducing dosing frequency for better management of rheumatoid arthritis.

• Authors: Sagar M Agnihotri, Pradeep R Vavia
• Journal: Drug development and industrial pharmacy (Drug Dev Ind Pharm) Vol. 35 Issue 9 Pg. 1043-7 (Sep 2009) ISSN: 1520-5762 [Electronic] England
• PMID: 19365783 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Cyclooxygenase 2 Inhibitors
• Delayed-Action Preparations
• Excipients
• Isoxazoles
• Sulfonamides
• valdecoxib

Topics

• 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)