Effect of time-dependent polymer on the dissolution rate of flurbiprofen: Formulation and evaluation of colon-specific matrix tablets

Abstract

An effort was made in the present study to prepare flurbiprofen matrix tablets to improve the therapeutic efficacy by increasing therapeutic drug concentrations in lower intestine i.e., site-specific release to colon. The current experiment was aimed to formulate matrix tablets using sodium alginate and HPMC K15M by direct compression method to study the effect of polymer on colon-specific drug release. The prepared matrix tablets were characterized for physical evaluations to indicate tablet uniformity and mechanical integrity. From the evaluations, HPMC matrices were found to be superior in tablet integrity and mechanical strength in comparison to sodium alginate matrices. In vitro drug release studies were performed by using USP XXIV Type II dissolution apparatus filled with simulated gastrointestinal fluids. From the in vitro dissolution studies, formulation F5 containing 50 mg of HPMC K 15M showed 11.62±0.78% drug release in 5 h and it was gradually increased to 98.83±1.02% in 24 h that indicates retardation of drug release in upper gastrointestinal tract and significant amount of drug release was observed in the colon. The accelerated stability studies proved the stability of drug in HPMC matrices. Hence, the development of HPMC K15M matrix tablets was suitable to achieve the colon-specific release of flurbiprofen. Further the efficacy of prepared matrix tablets has to be assessed by pharmacokinetic studies.