Ferrous ascorbate non-effervescent floating mini-caplets as an oral iron supplement.

ABSTRACT

PURPOSE: This research aimed to develop non-effervescent floating mini-caplets of Ferrous Ascorbate (FA) using low-density polymers to overcome the problems of poor bioavailability associated with immediate-release iron products. Methods: The excipients and method (melt granulation) were selected based on pre-and post-compression parameters in trial batches. The formulation was optimized by a full factorial 32 experimental design. An optimized formulation was evaluated for drug release kinetic, accelerated stability study, and in vivo study in healthy adult New Zealand female rabbits. Results: The optimized formulation F6 mini-caplets (42.5% FA, 45% Glyceryl palmitostearate as Precirol, 10% polyvinyl pyrrolidone K-30, and 2.5% lactose) were found to have instant floating and 12 h floating duration in 0.1N Hydrochloric acid (HCl) dissolution medium. In vitro drug release (diffusion mechanism) at 1 h and 5 h was 30-35% and 65-70%, respectively. It was found stable for three months under an accelerated stability study. In vivo study showed significantly increased serum iron levels and decreased unsaturated iron binding capacity (UIBC) in the test group (optimized formulation) compared to control and standard (immediate-release iron). Conclusion: Based on the in vitro and in vivo results, we conclude that non-effervescent floating FA mini-caplets have higher bioavailability compared to immediate release FA, which may be attributed to prolonged iron release at its absorption site due to their retention in the gastric region. Hence, non-effervescent floating FA mini-caplets may act as a potential approach for iron deficiency.