Pharmacokinetics of intramuscular microparticle depot of valdecoxib in an experimental model.
OBJECTIVE
We did a prospective study to investigate pharmacokinetics of a single intramuscularly (i.m.) administered Valdecoxib (VC) polymeric microparticles in New Zealand white rabbits.


METHODS
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.
Agnihotri
Sagar M
SM
Pharmaceutical Division, Institute of Chemical Technology, University of Mumbai, Matunga, Mumbai, India. agnihotrisagar@hotmail.com
Vavia
Pradeep R
PR
D000818:Animals; D019540:Area Under Curve; D001682:Biological Availability; D002851:Chromatography, High Pressure Liquid; D052246:Cyclooxygenase 2 Inhibitors / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D003627:Data Interpretation, Statistical; D003692:Delayed-Action Preparations; D004305:Dose-Response Relationship, Drug; D005079:Excipients; D006207:Half-Life; D007273:Injections, Intramuscular; D007555:Isoxazoles / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D008855:Microscopy, Electron, Scanning; D053758:Nanoparticles; D010316:Particle Size; D011817:Rabbits; D013449:Sulfonamides / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D000096926:Benzenesulfonamides
D052246:Cyclooxygenase 2 Inhibitors; D003692:Delayed-Action Preparations; D005079:Excipients; D007555:Isoxazoles; D013449:Sulfonamides; C406224:valdecoxib; D000096926:Benzenesulfonamides