Provided are a pharmaceutical composition comprising mineralocorticoid receptor antagonist and a use thereof. By orally administrating a pharmaceutical composition to a patient suffering from chronic kidney disease in need of treatment thereof, an effective and safe AUC of the pharmaceutical composition ranges from 188 ng*h/mL to 3173 ng*h/mL, with a bioavailability in mammals ≥ 50%. AUC is controlled in a safe and effective range when the pharmaceutical composition is administered for the treatment of chronic kidney disease in a daily dose of 0.1 mg to 1.0 mg.本發明涉及含鹽皮質激素受體拮抗劑的藥物組合物及其用途，本發明藥物組合物口服給藥於需要其治療的慢性腎病患者，其有效且安全的AUC範圍為188ng*h/mL至3173ng*h/mL，本發明藥物組合物在哺乳動物中的生物利用度50%，以日劑量為0.1mg-1.0mg給藥用於治療慢性腎病，AUC控制在安全有效的範圍內，保證了臨床用藥的安全性和有效性。
