Crystallinity required in maintaining good chemical stability of orlistat and its related materials is disadvantageous in terms of bioavailability. However, transformation of a crystal form into an amorphous form to increase bioavailability results in damage to chemical stability. An important point of the Technology is to provide solutions to satisfy the contradictory requiremnets. Therefore, the Technology suggests the following solutions: reduction of excessive crystallinity, use of a solubilized composition, improvement of antioxidative ability, use of porous and cellulose type adsorbents to solve instability problems and determination of a pH value suitable to achieve maximum chemical stability.The formulation according to the Technology shows enhanced solubility rate and stability when compared to other orlistat products. The pharmaceutical formulation comprises a pharmacologically active substance, a solvent, a solubilizer, a surfactanct, an antioxidant, and an adsorbent. According to the pharmaceutical formulation and the method, the pharmacologically active substance to obtain an amorphous liquid or semi-solid state, the antioxidant is melted together with the mixture to solve poor chemical stability of the pharmacologically a8ctive substance in an amorphous or liquid state, and the adsorbent is strongly adsorbed to the molten mixture so as to be transformed into a powder form so that the resulting molecules are reconstituted into very tiny crystal forms within the adsorbent to ensure chemical stability.