| 摘要 |
Disclosed are oral immediate release solid pharmaceutical formulations comprising a quinazolinone as an active ingredient and (i) from about 10% w/w to about 85% w/w of microcrystalline cellulose; (ii) about 4% w/w of sodium starch glycolate as a disintegrant; (iii) about 0.5% w/w of magnesium stearate; and (iv) about 2.5% w/w of colloidal silicon dioxide as a glidant. The pharmaceutical formulations are useful for regulating the expression of apolipoprotein A-I (ApoA-I) and as BET inhibitors, for the treatment and prevention of cardiovascular disease, and cholesterol- or lipid-related disorders, including, for example, metabolic syndrome, inflammatory disease, Alzheimer’s disease, atherosclerosis, diabetes, and cancer. The pharmaceutical active ingredient is selected from: 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)quinazolin-4(3H)-one; 2-(3-chloro-4-(2-hydroxyethoxy)phenyl)-5, 7 -dimethoxyquinazolin-4(3H)-one; 2-(4-(2-hydroxyethoxy)-3-methoxyphenyl)-5,7-dimethoxyquinazolin-4(3H)-one; 2-(4-hydroxy-3-(2-hydroxyethyl)phenyl)-5,7-dimethoxyquinazolin-4(3H)-one; 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethylquinazolin-4(3H)-one; 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5-methoxyquinazolin-4(3H)-one; 2-(4-(2-hydroxyethoxy)-3-methylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one; 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one; |
