Provided herein are pharmaceutical formulations comprising
glucokinase activator, or a
prodrug, or a pharmaceutically acceptable salt, an
isotope labeled analogue, a crystalline form, a
hydrate, a solvate, or a diastereomeric or enantiomeric form thereof and the use thereof for treating diseases; the pharmaceutical formulations are in the form of immediate-release formulations, extended-release formulations, or combination of immediate-release formulation and extended-release formulations. The pharmaceutical formulations achieved once-a-day therapy for some diseases, in particular,
type II Diabetes Mellitus with
obesity. The pharmaceutical formulations exhibit sustained 24 hours of glucose-lowering effects. The pharmaceutical formulations also achieved lower Cmax, extended T1 / 2 as well as maintained similar
bioavailability and increased MRT compared with commercial Dorzagliatin tablet, enhanced the
pharmacology effect of restoring the glucose stimulated GLP-1
secretion in diabetes with
obesity.