The present invention provides a method for preparing an entecavir formulation for oral administration comprising the steps of: (A) micronizing entecavir into a particle size of 1 60 µm (B) mixing the micronized entecavir and a pharmaceutical additive to form a pharmaceutical composition and (C) compression molding the pharmaceutical composition by direct compression or dry granulation compression. It is possible to prepare a low dosage entecavir formulation for oral administration with excellent content uniformity and hepatitis B treatment effects through a simple process by the preparation method of the present invention.
