The present disclosure relates to an orally administered pharmaceutical formulation containing an inclusion complex formed as varenicline or a pharmaceutically acceptable salt thereof is included in cyclodextrin. The pharmaceutical formulation can improve convenience of medication by effectively masking the bitter taste of the drug and the irritation during swallowing, can provide the oxidation stability of varenicline and can improve the solubility of the drug.本發明揭露了一種口服藥物製劑，其包括環糊精以及伐尼克蘭或其藥學上可接受的鹽類的一內含錯合物，其中，伐尼克蘭或其藥學上可接受的鹽類係包含於該環糊精內部。該口服藥物製劑可有效的掩蓋藥物的苦味以及吞嚥藥物時的刺激以改善用藥的方便性，並可提供伐尼克蘭的氧化穩定性以即可改善該藥物的溶解度。
