Formulation, evaluation and pharmacokinetics of colon targeted pulsatile system of flurbiprofen

Abstract

Objective: The intent of the present investigation is to develop colon targeted compression coated flurbiprofen pulsatile release tablets that retard the drug release in the upper gastro intestinal system but progressively release in the colon.Materials and methods: Flurbiprofen core tablets were prepared by direct compression method and were compression coated with hydroxypropyl methylcellulose and Eudragit S100. The formulation is optimized based on the in vitro drug release study and further evaluated by X-ray imaging and pharmacokinetic studies in healthy humans for colonic delivery.Results and discussions: The optimized formulation showed negligible drug release (7.26 ± 0.05%) in the initial lag period followed by progressive release (99.27 ± 0.46%) for 24 h. The X-ray imaging study in human volunteers showed that the tablets reached the colon without disintegrating in the upper gastrointestinal tract. The Cmax of colon targeted tablets was 10792.62 ng/mL at Tmax 10 h where as in case of immediate release tablets the Cmax was 15684.79 ng/mL at Tmax 3 h signifies the ability of compression coated tablets to target the colon.Conclusion: Development of pulsatile release compression coated tablets using combination of time dependent and pH sensitive approaches was suitable to target the flurbiprofen to colon.