Studies On Prescription, Preparation Technology And Quality Control Standards Of Nabumetone Dispersible Tablets

Nabumetone (4-[6-methoxy-2-naphthyl]-butan-2-one) is a newly developednonacidic prodrug that after oral dosing is metabolized chiefly to an activenonsteroidal anti-inflammatory moiety-6-methoxy-2-naphtlyl-acetic acid (6-MNA),6-MNA inhibits prostaglandin synthesis in vitro, and exhibits analgesic, antipyretic,and anti-inflammatory activity. Nabumetone is recommended 1g once daily for thesymptomatic treatment of rheumatoid arthritis, osteoarthritis and soft-tissue injuries.Nabumetone was well tolerated in man.In this paper, nabumetone dispersible tablets were prepared. Firstly, theformulation and preparation technology have been explored and studied. Formulationswere screened according to disintegration time, dispersible uniformity and dissolutiondegree, combined with the properties of nabumetone physical chemistry. Based on theabove results and the studies of determination methods and conditions, thenabumetone dispersible tablets quality control standards have been set up. Thedissolution rate and the disintegration time of nabumetone dispersiblle tablets weresignificantly faster than that of nabumetone tablets.Secondly, the stability of nabumetone dispersible tablets was investigated indetail. By the tests of strong light shinning, high temperature and heavy humidity, itwas proved that nabumetone dispersible tablets were insensitive to the above factors.Meanwhile, Further high stability of the product was certified by the acceleration testand room temperature long term storage test (18 months).Finally, Three sale-up experiments for industrial nabumetone dispersible tabletswere carried out. The result showed that its appearance, weigh difference,disintegration ,dispersible uniformity and dissolution reached the standards of Chinesepharmacopoeia, It indicated that the preparative technology in this study had a highrecurrence and the product quality was easily controlled, so it could be industriallyproduced. The bioavailability of the industrial nabumetone dispersible tablets havebeen compared with that of marketing nabumetone tablets, the result indicated that thetwo formulations are bioequivalences. In conclusion, established reliable academic foundation and industrial basis fornext optimizing nabumetone dispersible tables prescription have importantsignificance in theoretical guide and practical application value for developing thedispersible tablets.