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Development,pharmacological and toxicological evaluation of a new tablet formulation based on Cassia grandis fruit extract
Authors:Ariadna Lafourcade Prada  Leonard Domingo Rosales Achod  Hady Keita  Jose Carlos Tavares Carvalho  Tatiane Pereira de Souza  Jesús Rafael Rodríguez Amado
Abstract:The treatment of Diabetes mellitus (DM) involves drugs for controlling the blood glucose level, and for treating concomitant disorders such as obesity. 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. Fruits of the Cassia grandis L f, an underutilized species from the Cuban’ eastern region; allow developing a novel tablet formulation that could be used for the treatment of diabetic patients.
Keywords:Mixture design  Antioxidant  α-glycosidase  Antiglycant  Diabetes  Acute toxicity
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