Objectives: Tibolone is an estrogen‑like compound used for the treatment of the symptoms associated with the menopausal transition and also for the treatment of osteoporosis. The aim of this study was to evaluate impact of micronization on the dissolution profile so as to improve the release rate of Tibolone drug from tablet dosage form. Materials and Methods: Tibolone oral tablet 2.5 mg is formulated using micronized and unmicronized drug in a preoptimized formula and was evaluated for drug content, dissolution, hardness, thickness, and disintegration time. Particle size reduction of Tibolone drug was achieved by Air Jet Milling and evaluated by using Malvern mastersizer instrument. Results: Micronization of Tibolone enhanced its dissolution rate to a significant extent when compared with unmicronized material. The dissolution profile of formulation with micronized Tibolone was similar to that of European market product (Livial tablet 2.5 mg). Conclusion: Micronization technique has a significant impact on the dissolution of Tibolone. The experimental findings suggest that micronization can be used for the preparation of rapidly dissolving formulations of Tibolone, and could potentially lead to improvement in the in‑vivo bioavailability of Tibolone oral tablets.