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A NOVEL APPROACH FOR THE FORMULATION OF GASTRIC ORAL FLOATING DRUG DELIVERY SYSTEM CONTAINING GLIPIZIDE

机译:包含格列吡嗪的口腔漂浮药物递送系统的新方法

摘要

Glipizide is an selective second generation sulphonylurea agent used in the treatment of hyperglycaemia. It is a poorly soluble in the acidic environment. When it is given orally in healthy people, it absorbs rapidly and completely. However, the same cannot be said in people with hyperglycaemia problem, as it delays the absorption of glipizide due to impaired gastric emptying or gastric motility. This delay of absorption may be clinically relevant, since the efficacy of short acting sulphenylureas is dependent upon the absorption rate of the drug. To overcome these draw backs, the present study was undertaken to investigate the gastric retentive dosage form of glipizide particularly a floating controlled drug delivery system. Ten formulations containing retardent material and alkalizing agent were prepared with solubilizing agent in different ratio. It was found that sodiumbicarbonate reacts with HCI and produce C02 which creates pores in tablet and elevates swelling by wetting polymer. So it helps in maintaining the buoyancy. The release rate could be modified by varying the polymer ratio, concentration of alkalizing and solubilizing agent. The prepared tablets were evaluated for general appearance, content uniformity, hardness, friability, buoyancy and in vitro dissolution studies. Formulation FIO containing HPMC K4 and maximum concentration of sodium bicarbonate and PVP showed better release with therapeutic efficacy in comparison to other formulations.
机译:格列吡嗪是用于治疗高血糖症的选择性第二代磺酰脲类药物。它在酸性环境中难溶。在健康人中口服时,它会迅速完全吸收。但是,对于高血糖症患者则不能这样说,因为由于胃排空障碍或胃运动障碍,它会延迟格列吡嗪的吸收。这种吸收延迟可能与临床有关,因为短效亚磺酰脲的功效取决于药物的吸收速率。为了克服这些缺点,进行了本研究以研究格列吡嗪的胃滞留剂型,特别是浮动控制的药物递送系统。用不同比例的增溶剂制备了十种含有阻滞剂​​和碱化剂的制剂。发现碳酸氢钠与HCl反应并产生CO 2,CO 2在片剂中形成孔并通过润湿聚合物而增加溶胀。因此,它有助于保持浮力。释放速率可以通过改变聚合物比例,碱化剂和增溶剂的浓度来改变。评价制备的片剂的总体外观,含量均匀性,硬度,脆性,浮力和体外溶出度研究。与其他制剂相比,包含HPMC K4以及最大浓度的碳酸氢钠和PVP的制剂FIO显示出更好的释放和治疗效果。

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