Development of direct compression entecavir 0.5 mg-loaded tablet exhibiting enhanced content uniformity

Abstract The aim of the present research was to develop direct compression entecavir 0.5 mg-loaded tablet (DCET) providing enhanced content uniformity. Various compositions and preblending methods were tested at lab-scale, and the optimum composition and method were applied to pilot-scale production for further confirmation of the entire process. The content uniformity, physical properties and dissolution behavior of the final film-coated DCET were compared to the commercial product. In lab-scale preparation, the method involving preblending, micronization of API (d 0.5  = 5.13 μm), addition of a larger quantity of colloidal silicon dioxide (1%) and sieving through smaller pores (300 μm) yielded an excellent acceptance value (AV) in the content uniformity criteria compared to a control method and composition (AV 1.0 vs. 9.8). In pilot-scale production, the film-coated DCET provided better content uniformity than the commercial product (AV 1.3 vs. 3.8). Furthermore, both products exhibited similar dissolution profiles in various media. Thus, direct compression entecavir 0.5 mg-loaded tablet developed in this study would be a promising dosage form with excellent content uniformity that may be bioequivalent to the commercial product.