Abstract

SPRAY DRIED DISPERSIONS: A VIABLE APPROACH TO IMPROVE BIOAVAILABILITY, TICAGRELOR AS A MODEL DRUG

Dabhi Ajay N.* and Patel Dasharath M.

Abstract

The present study aimed to investigate the processability of APIHydrophilic carrier composite into formulation of solid dispersion and therefore to reveal the benefits of the composite formation in IN-VIVO performance. Spray dried dispersions (SDDs), consisting of active component embedded with hydrophilic polymer, were manufactured by Spray dryer. Release profile as well as IN-VIVO performance of the formulation with reference product was compared. Simple and economical spray drying method based on the solvent evaporation method was developed for the formulation of Ticagrelor solid dispersion. Initial characterization of physical mixtures, pure drug, reference product and solid dispersions were carried out by in vitro dissolution, dissolution efficiency, permeation study, wetting study, solubility study, FT-IR, differential scanning calorimetry (DSC) and IN-VIVO bioavailability study. DSC study showed that Ticagrelor was present in its amorphous form. FT-IR study showed there is no incompatibility between any polymeric systems with drug components. Improvement in the solubility and dissolution rate was observed for all samples. During ageing study, almost no decrease of in vitro drug dissolution was observed as compare with freshly prepared solid dispersions. Solid dispersions showed more than 75% Ticagrelor release after 45 min during dissolution test. IN-VIVO bioavailability study shows more than two fold increase in bioavailability compare to market formulation. The result showed that the spray drying process of a liquid feed is an attractive and promising alternative to obtain enhanced solubility of drug in solid dispersions. Thus, present study demonstrated the high potential of spray drying process technique for obtaining stable free flowing solid dispersions of poorly water-soluble drugs using various solubilizing polymers.

Keywords: Spray dried dispersions, Solubility, Dissolution rate, Spray drying technique, Solubilizing polymers, Anti-static agent, IN-VIVO bioavailability study.