用于高血压治疗的厄贝沙坦快速溶解片剂的配方、改良和评估

Ondieki Kemunto Asenath Susan, Kamal Singh Rathore
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摘要

为了制备血管紧张素受体阻滞剂(ARB)厄贝沙坦的快速溶解片剂,我们采用了直接压片法,其中包括几个步骤。主要重点是改善药物与水接触时的脱嵌时间和溶解速度。乳糖和微晶钠 (MCC) 被用作稀释剂和填充剂,阿斯巴甜和硬脂酸镁被用作润滑剂,而氯磺丙烯酮、氨溶卡麦隆钠 (CCS) 和淀粉乙醇酸钠 (SSG) 则被用作超级脱嵌剂,因为它们在与水接触时会增加水压。研究了片剂的压缩后性能、脱嵌时间、润湿时间和药物释放曲线。制备的制剂与市场上销售的制剂的药物释放情况进行了比较。使用不同比例的辅料制备了 5 种配方,并对优化后的配方进行了表征。片剂的硬度在生产过程中通过压缩进行控制。傅立叶变换红外光谱研究发现,药物与辅料之间不存在相互作用,药物释放取决于配方中辅料的类型。研究发现,直接压片是设计口服快速溶解片剂(FDT)的一种合适、简便和高效的技术。
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Formulation, modification and evaluation of fast dissolving tablet of irbesartan for hypertension management
To prepare fast dissolving tablet of Irbesartan an Angiotensin Receptor Blocker (ARB), direct compression method was utilised, and it comprised several steps. The main focus was to improve the disintergation time as well as the dissolution rate of the drug as it comes into contact with water. Lactose and Microcrystalline sodium (MCC) were used as diluents and fillers, Aspartame and Magnesium Stearate were used as lubricants, Crospovidone, Croscarmellose sodium (CCS), Sodium Starch Glycolate (SSG) were used as superdisintergrants as they increase the hydraulic pressure when the come into contact with water. The post compression properties of the tablet; disintergration time, wetting time and the drug release profile of the prepared table were investigated. The drug release of the prepared formulation was compared to the marketed formulation. 5 formulations were prepared using different ratios of the excipients and the optimized formulations were subjected to characterization. Hardness of the tablet was controlled by compression during the manufacturing process. Following FTIR studies, it was found that there were no interaction between the drug and the excipients and that the drug release depended on the type of the excipients used in the formulation. Direct compression was found to be a suitable, easy and efficient technique for designing fast dissolving tablet (FDT) for oral use.
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