Study of the effect of pvp k30 in the enhancement of solubility of telmisartan by polymer assisted crystal agglomeration using polymer enriched bridging liquid technique

Abstract

Polymer Enriched Bridging liquid is a novel approach for enhancing the flow characteristics, micromeritic properties, solubility and dissolution of poorly water-soluble drugs. Telmisartan is an orally effective Angiotension II receptor antagonist used extensively for the effective management of hypertension. Telmisartan is a poorly water-soluble drug and an ideal candidate for this approach. PVPK30 is used as the hydrophilic polymer. Various formulations were prepared with the addition of PVPK30 in the bridging liquid by Polymer Enriched Bridging Liquid Technique (PEBL). The preparations were subjected to particle size analysis, micromeritic characteristics, FTIR, differential scanning calorimetry (DSC) and Scanning Electron microscopic analysis. The crystal agglomerates were found to be spherical in nature with excellent flow characteristics. The crystallinity of the pure drug was found to be decreased without any drug-polymer interaction. The saturation solubility studies showed that the optimized formulation STP04 showed 30.695 folds increase in solubility in water and 29.462 folds enhancement in pH 7.5 phosphate buffer. The in vitro drug release studies also confirmed the enhancement in dissolution rate. The stability of the prepared aggregates was determined by accelerated stability studies. The addition of polymer in the bridging liquid during crystallization stage improved the effective incorporation of the hydrophilic polymer in the aggregates. Polymer Enriched Bridging Liquid technique can be considered as an ideal technique for solubility and dissolution enhancement.