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首页> 外文期刊>Current Science: A Fortnightly Journal of Research >Delivery of repaglinide-cholestyramine complex loaded ethylcellulose
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Delivery of repaglinide-cholestyramine complex loaded ethylcellulose

机译：递送瑞格列奈-胆固醇胺复合物乙基纤维素

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摘要

The main aim of this work is to develop and thoroughly evaluate resin-based multiparticles of repaglinide for effective management of type-2 diabetes mellitus. Repaglinide was complexed with cholestyramine resin; later the resin complexed drug was encapsulated in ethylcellulose microspheres. The microspheres were characterized for micromeritic properties, SEM analysis, entrapment efficiency, percentage yield, IR spectroscopy, buoyancy behaviour and in vitro drug release in simulated gastric fluid. Microparticles showed regular shape and spherical morphology with entrapment efficiency in the range 51-69%. Differential scanning calorimetry confirmed that there was no chemical interaction between the polymer and the drug. Resin-based microspheres showed good buoyancy behaviour (P < 0.0 5) due to the presence of bicarbonate ions and sustained release compared to plain drug microspheres (P < 0.05). Finally, the effectiveness of the formulations was evaluated in vivo for blood glucose lowering effect in both normal and streptozotocin-induced diabetic rats. Blood glucose lowering effect induced in diabetic rats by the repaglinide-loaded microspheres was significantly greater (P < 0.0 5) and prolonged (similar to 8 h) compared to plain drug microspheres. In a nutshell, floating microspheres containing drug resin complex were able to sustain the drug release in an effective manner for prolonged periods of time and proven in vivo effectiveness by reducing blood glucose level for a longer duration
机译：这项工作的主要目的是开发和彻底评估瑞格列奈的树脂基多颗粒药物，以有效治疗2型糖尿病。将瑞格列奈与胆甾醇胺树脂复合;之后，将树脂复合药物封装在乙基纤维素微球中。表征了微球的微胶束性质，SEM分析，包封效率，百分收率，IR光谱，浮力行为和在模拟胃液中的体外药物释放。微粒表现出规则的形状和球形形态，截留效率在51-69％的范围内。差示扫描量热法证实聚合物与药物之间没有化学相互作用。与普通药物微球相比，基于树脂的微球由于存在碳酸氢根离子并具有持续释放作用，因此具有良好的浮力性能（P <0.0 5）。最后，在正常和链脲佐菌素诱导的糖尿病大鼠中，评估了体内制剂对降低血糖的效果。与普通药物微球相比，负载瑞格列奈的微球在糖尿病大鼠中引起的血糖降低作用明显更大（P <0.0 5），并且延长了（类似于8小时）。简而言之，含有药物树脂复合物的漂浮微球能够长时间有效地维持药物释放，并通过降低血糖水平更长的时间证明了体内有效性

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