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 pcnt . 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.
