Preparation Of Aceclofenac Enteric-coated Pellets

Aceclofenac is a new kind of nonsteroidal antiinflammatory drugs (NSAIDs), whichis mainly used to treat rheumatoid arthritis (RA) and osteoarthritis (OA). NASIDs havethe irritative effects on the stomach, which may cause stomach bleeding. Theenteric-coated agent can reduce the irritation. This study aims to prepare aceclofenacenteric-coated pellets to reduce the irritation. HPLC method was developed for assayingthe contents of aceclofenac and the methodology was developed. Furthermore, ultravioletspectrophotometry method was developed for assaying the enteric-coated pellets release.Aceclofenac pellets were prepared by the process of centrifugal granulation, in which talcwas the material of spacer layer,and eudragit L30D-55,as enteric coating material,wasapplied in the fluid bed coating system to prepare the enteric-coated pellets.Thepreparation prescription and process parameters were optimized by single factor method.We used New Zealand rabbits to investigate the pharmacokinetics of enteric-coated pelletsand enteric-coated capsules of aceclofenac. The aceclofenac enteric-coated pellets had aparticle size of18~24mesh (0.8~1.0mm). The angle of repose was28.5°less than30°,and the average drug loading was31.25%. The release of the enteric-coated pellets inpH1.0HCL was less than5.00%within2h and that in pH6.8PBS was more than70.00%within45min.The aceclofenac pellets’ yield of Pilot production was88.62%, and the yiledof fluidized bed coating process was73.65%. The pharmacokinetics parameters ofaceclofenac enteric-coated pellets and enteric-coated capsules were: Tmax(6.00±0.50) and(4.00±0.90) h; Cmax(8.40±0.70) and (9.08±0.60) μg·mL-1; AUC(105.11±7.09) and(88.54±15.22)(μg·mL-1)·h. The results indicated that the enteric-coated pellets ofaceclofenac were better than the other two enteric-coated formulations in the acidtolerancel and the reproducibility of prescription,so the study of enteric-coated pellets ofaceclofenac had practical value.