DEVELOPMENT AND EVALUATION OF TAPENTADOL HYDROCHLORIDE EXTENDED RELEASE TABLET

Extended release tablets of Tapentadol hydrochloride were prepared by wet granulation method using microcrystalline cellulose PH101, sodium carboxy methyl cellulose, polyvinyl pyrrolidine (K-90), methocel K 200M and plasdone. The drug and excipients compatibility was studied by FT-IR which showed no physico-chemical interaction. The polymer used Hydroxy propyl ethyl cellulose was granular blend. Also it was concluded that it improves the drug release at 12th hour. The kinetic treatment of the drug release data of the prepared formulations followed zero order drug release the prepared formulations followed Higuchi profile. It indicated that the drug release from the tablets involves anomalous diffusion mechanism or diffusion coupled with erosion, and directly proportional to square root of time as indicated by the n value of 0.66 in Korsmeyer's plot. On comparing equation of straight line and regression coefficient (R2) with Innovator, formulation F8 shows similarity of results with innovator. Hence F8 was considered as formulation with extended release profile as indicated by 95.2% of drug released at the end of 12hrs. The stability studies were carried out for a period of 3 months as per ICH guidelines. There were no significant changes in dissolution profile and other parameters of the optimized formulation F8. To conclude, formulation F8 containing higher concentration of polymer (HPMC) and optimum concentration of super disintegrant showed drug release of 95.2% at the end of 12h, and this optimized formulation can be selected for further studies. Key words: Tapentadol hydrochloride , microcrystalline cellulose , Extended release tablets, stability