Orally Disintegration Tablet (ODT) Formulation of Candesartan Cilexetil With Croscarmellose Sodium and Crospovidone as Superdisintegrant

Nurista Dida Ayuningtyas, Yahya Febrianto, Tutut Lutfi
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Abstract

Candesartan cilexetil is a group of selective AT1 hypertension drugs (angiotensin II receptor antagonist 1). The drawback of candesartan cilexetil in conventional tablets is that it cannot be used for geriatric patients who have difficulty swallowing tablets, patients with developmental disorders of the muscle and nervous system (tremors), and in schizophrenic patients that lead to poor patient compliance, so to overcome this problem alternative dosage forms are made new namely ODT candesartan cilexetil. This study aims to determine the effect of the combination of superdesintegrant croscarmellose sodium and crospovidone on the quality test of the physical properties of tablets. Candesartan cilexetil ODT tablets bolted by direct compression method with variations in levels of superdesintegrant croscarmellose sodium and crospovidone 2: 3,5%, 2,75: 2,75%, 5: 0,5%, 4,25: 1,25 %, 3,5: 2%. Tests conducted to determine the physical quality of candesartan cilexetil ODT, namely organoleptic, weight uniformity, size uniformity, hardness, brittleness, disintegration time, wetting time and water absorption ratio. Showed an increase in the use of crospovidone (5%) and a decrease in croscarmellose sodium (0.5%) had a greater effect on the disintegration time because it could make the tablet porous when in contact with water so that it would accelerate the disintegration time of 29.167 seconds and increase the speed of wetting the tablets 25.33 seconds. The combination of superdisintegrant croscarmellose sodium and crospovidone (0.5: 5%) in formula 3 can provide physical properties that meet the best quality ODT requirements for candesartan cilexetil.
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以交联棉糖钠和交联维酮为超崩解剂的坎地沙坦西莱西酯口服崩解片的研制
坎地沙坦西列地酯是一组选择性AT1高血压药物(血管紧张素II受体拮抗剂1)。坎地沙坦西列地酯常规片剂的缺点是不能用于吞咽片剂有困难的老年患者、有肌肉和神经系统发育障碍(震颤)的患者以及导致患者依从性差的精神分裂症患者。因此,为了克服这个问题,替代剂型是新的,即ODT坎地沙坦西莱西酯。本研究旨在确定超崩解剂交联棉糖钠与交联维酮配用对片剂物性质量检验的影响。坎地沙坦西莱西酯ODT片采用直接压缩法固定,超崩解剂交叉淀粉糖钠和交叉维酮的含量分别为2:3、5%、2,75:2,75%、5:0、5%、4,25:1,25%、3,5:2%。测定坎地沙坦西莱西酯ODT的物理质量,即感官、重量均匀性、尺寸均匀性、硬度、脆性、崩解时间、润湿时间和吸水率。结果表明,增加交联维酮用量(5%)和减少交联维酮钠用量(0.5%)对崩解时间的影响较大,交联维酮可使片剂与水接触时呈多孔状,崩解时间可加快29.167秒,润湿速度可加快25.33秒。配方3中超崩解剂交联棉糖钠与交联维酮(0.5:5%)的组合可提供满足坎地沙坦西列酯最佳质量ODT要求的物理性能。
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