Development of multi-layered gastric floating tablets based on konjac glucomannan: a modified calcium supplement with enhanced bioavailability

Abstract

This study developed a gastric-floating delivery system of calcium based on konjac glucomannan (KGM). The developed calcium tablets, consisting of one core layer coated with two barrier layers, were fabricated with a facile method. The role of KGM within the tablets was evaluated from characteristics including swelling behavior, hydrated gel properties, floating ability and release profiles of calcium (Ca). The results indicated that upregulating the KGM fraction accelerated the formation of a more compact gel network in gastric conditions, which prolonged both the floating lag time and floating duration, which resulted in a more sustained swelling behavior and a slower release of calcium. Among all the formulations, a core tablet containing 20% KGM (K20) was selected as the optimized one as it could quickly float up in 7.21 s, exhibited an almost linear release and obtained a release amount of 87.73% within 12 h. Finally, a comparison of in vivo calcium bioavailability between a KGM-based calcium tablet and a commercial calcium tablet (Caltrate®) was carried out by monitoring the serum calcium concentration after administration in rabbits. The results suggested that, after having the KGM-based calcium tablet, the changes of serum calcium levels were gentler due to a sustained-release property. The difference integral value between profile K20 and the baseline was 1.4358, larger than that of Caltrate® (1.1808), suggesting the higher absorption efficiency of KGM-based calcium tablets.