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Development, pharmacological and toxicological evaluation of a new tablet formulation based on Cassia grandis fruit extract
Sustainable Chemistry and Pharmacy ( IF 6 ) Pub Date : 2020-03-12 , DOI: 10.1016/j.scp.2020.100244
Ariadna Lafourcade Prada , Leonard Domingo Rosales Achod , Hady Keita , Jose Carlos Tavares Carvalho , Tatiane Pereira de Souza , Jesús Rafael Rodríguez Amado

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.



中文翻译:

一种基于决明子果提取物的新型片剂的研制,药理和毒理学评估

糖尿病(DM)的治疗涉及控制血糖水平和治疗合并症(例如肥胖症)的药物。鉴于决明子果实提取物(CgE)的强抗氧化活性,α-糖苷酶和脂肪酶的抑制作用以及强降血糖作用,本工作开发了一种以CgE作为抗氧化剂的新型片剂(CgET)。有效成分。通过使用D-最佳优化赋形剂比例混合设计。评估了压实力(10、13、16、19和22 kN)对片剂技术性能的影响。将优化的颗粒剂压缩至16 kN,以生产具有出色技术性能的片剂。片剂显示出强大的抗氧化作用(IC 50  = 1.45μg/ mL),并且α-糖苷酶抑制活性(IC 50  = 34.96μg/ mL)比阿卡波糖(IC 50  = 63.25μg / mL)更有效。片剂通过氧化性(IC 50  = 22.45±1.80μg/ mL)和非氧化性(IC 50)表现出强大的抗血糖作用 = 25.49±1.80μg/ mL)途径,并产生(100 mg / kg)的降血糖作用在统计学上等同于格列本脲(25 mg / kg)。CgET没有口服毒性(LC 50  > 2000 mg / kg),被认为是无毒产品。决明子L f的果实,古巴东部地区未充分利用的物种;允许开发可用于治疗糖尿病患者的新型片剂。

更新日期:2020-03-12
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