Pharmacological screening of glibenclamide solid dispersion in fructose-fed diabetic rats

Mst Mahfuza Rahman, R. Barman, Md. Rafiqul Islam Khan, Md. Ashraf Ali, Md. Shah Alam Sarker, M. I. I. Wahed
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Abstract

In this study, our main objective was to estimate the therapeutic effectiveness of the formulated solid dispersion of glibenclamide (GSD) with improved dissolution profiles in comparison with pure GLB by means of fructose-fed diabetic rat model. To evaluate the pharmacological effectiveness of the formulated GSD, fructose-fed diabetic rat model was evolved, and the obtained consequences were compared with the conventional GLB treatment. GSD exhibited improved glucose and lipid-lowering efficacy of GSD in contrast to pure GLB after 15 days of treatment. Low dose (0.5mg/kg) and high dose (5mg/kg) of GSD showed significant lowering of blood glucose which is 6±0.2 mmol/L and 5.6±0.3 mmol/L respectively after 15 days of treatment that is much better than that of pure GLB (6.2±0.4 mmol/L). Furthermore, low dose of GSD presented approximately comparable beneficiary effects in regard to triglycerides (72.00±7.23mg/dL) total cholesterol (110.33±5.78 mg/dL), and low-density lipoprotein (67.60±5.21mg/dL) and high-density lipoprotein (28.33±1.53 mg/dL) as pure GLB after 15 days. Additionally, histological studies as well confirmed no fatty infiltration from liver by GSD as compared with GLB which was consistent with the biochemical parameters. For treating diabetes and hyperlipidaemia, the formulated GSD might be a potential substitute for traditional GLB.
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格列本脲固体分散体在果糖喂养糖尿病大鼠体内的药理学筛选
在本研究中,我们的主要目的是通过果糖喂养的糖尿病大鼠模型,评估与纯GLB相比,具有改善溶解特性的格列本脲固体分散体(GSD)的治疗效果。为了评估配方GSD的药理学有效性,建立了果糖喂养的糖尿病大鼠模型,并将获得的结果与传统的GLB治疗进行了比较。治疗15天后,与纯GLB相比,GSD表现出改善的GSD的葡萄糖和降脂功效。低剂量(0.5mg/kg)和高剂量(5mg/kg)GSD治疗15天后血糖显著下降,分别为6±0.2mmol/L和5.6±0.3mmol/L,明显优于纯GLB(6.2±0.4mmol/L)。此外,15天后,低剂量GSD对甘油三酯(72.00±7.23mg/dL)、总胆固醇(110.33±5.78mg/dL。此外,组织学研究也证实,与GLB相比,GSD没有脂肪从肝脏浸润,这与生化参数一致。对于治疗糖尿病和高脂血症,所配制的GSD可能是传统GLB的潜在替代品。
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