Formulation and stability study of lipid-based formulations for oral administration of poorly water-soluble drug

Abstract

Rousuvastatin calcium (ROS) is a model of poorly water-soluble drug. The objective of the study was to increase the dissolution rate and stability of ROS through formulation of   basic tablets, contain nanoemulsion of the drug. Full factorial design (2³) was applied for a screening study in which three factors were used at two levels (low and high). The factors were the type of disintegrants (Ac-di-sol, Explotab), the concentration of disintegrant (3%w/w, 5%w/w) and the binder type (Avicel PH101, PEG6000). The tablets are prepared by direct compression. The weight variation, content uniformity, friability, hardness, disintegration time, and in-vitro dissolution of the prepared formulae were evaluated. The stability of tablets was also studied at 40°C & 75% RH for period of 3 months at 40°C. The tablets were prepared by direct compression technique. The formula F6 containing Ac-di-sol (5%w/w) with AvicelPH101 (30%w/w) has the least disintegration time (45.55 ± 4 seconds) and the highest dissolution rate (95±3.6%). The stability of tablets was studied at 40°C & 75 % RH for period of 3 months. The results indicate that ROS tablets may serve as a successful strategy for enhancing the dissolution and stability.