Based on the potent antioxidant activity, the α-glycosidase and lipase inhibitory effect, and the potent hypoglycemic effect of the fruit extract of Cassia grandis Lf (CgE), in this work it was developed a novel tablet formulation (CgET) using CgE as the active ingredient. The excipients proportion was optimized by using a D-optimal mixture design. The effect of the compaction force (10, 13, 16, 19, and 22 kN) on the technological properties of tablets was evaluated. The optimized granules formulation was compressed at 16 kN, for producing tablets with excellent technological properties. Tablets showed a potent antioxidant effect (IC50 = 1.45 μg/mL), and α-glycosidase inhibitory activity (IC50 = 34.96 μg/mL) more potent than Acarbose (IC50 = 63.25 μg/mL). Tablets exhibited a strong antiglycant effect by the oxidative (IC50 = 22.45 ± 1.80 μg/mL) and non-oxidative (IC50 = 25.49 ± 1.80 μg/mL) pathways, and produced (at 100 mg/kg) a hypoglycemic effect statistically equal to glibenclamide (25 mg/kg). CgET did not show oral acute toxicity (LC50 > 2000 mg/kg), framed as a non-toxic products.