溶度增强法制备兰索拉唑快溶片及评价

Arti Choursiya, D. Pandit
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引用次数: 3

摘要

本文对兰唑拉唑速溶片的制备及评价进行了研究。兰索拉唑(LAN)是一种质子泵抑制剂药物,用于治疗胃溃疡。兰索拉唑是一种酸性不稳定的药物,为了避免胃的酸性pH,兰索拉唑被配制成口服快溶片。兰索拉唑是BCS分类的第二类药物,具有低水溶性。因此,为了提高药物的溶解度,我们用聚乙二醇和β环糊精配合物制备了兰索拉唑固体分散体。以乙醇酸淀粉钠、交叉聚维酮、交叉卡蜜糖钠等强力崩解剂为原料,采用直接压缩法制备LAN速溶片。对制备的快溶片进行重量变化、硬度、脆性、崩解时间、药物含量、润湿时间、体外释药及短期稳定性等指标的评价。所有制剂的重量变化率、硬度、脆性和药物含量均匀性均在批准范围内。体外释放实验表明,90秒内可释放99.6%的LAN。总体而言,直接压缩法制备的配方中,含有6% CCS作为超级崩解剂的F3在2 min内释放99% (LAN)的效果最佳。结果表明,LAN快溶片具有增强溶出度的作用,可提高生物利用度,对胃溃疡有较好的治疗效果。关键词:β环糊精,交叉聚维酮,速溶片,胃溃疡,兰唑拉唑,固体分散体
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FORMULATION AND EVALUATION OF FAST DISSOLVING TABLETS OF LANSOPRAZOLE BY SOLUBILITY ENHANCEMENT TECHNIQUE
The present study was focused on preparation and evaluation of Lanzoprazole fast dissolving tablets. Lansoprazole (LAN) is a proton pump inhibitor drug and used for the treatment of gastric ulcer. Lansoprazole is acid labile drug and to avoid the acidic pH of the stomach LAN is formulated as oral fast dissolving tablets. Lansoprazole is the class II drug of the BCS classification and has a low aqueous solubility. Hence, to improve the solubility of the drug we have prepared Lansoprazole solid dispersion with poly ethylene glycol and complex with β cyclodextrin. Fast Dissolving tablets of LAN were formulated using different superdisintegrants like Sodium Starch Glycolate, Cross Povidone, Cross Carmellose Sodium by direct compression method. The prepared fast dissolving tablets were evaluated for various parameters like weight variation, hardness, friability, disintegration time, drug content, wetting time, in-vitro drug release and short term stability studies. Percentage weight variation, hardness, friability and drug content uniformity were found to be within the approved range for all the formulations. The in-vitro release studies showed that 99.6% of LAN within 90 sec. Overall, in the formulations prepared by the direct compression method, F3, which contains 6% CCS as super disintegrants release 99% of (LAN) in 2 min was found to be the best formulation. The results concluded that fast dissolving tablets of LAN showing enhanced dissolution might lead to improved bioavailability and effective therapy for gastric ulcer. KEYWORDS: β cyclodextrin, Cross Povidone, Fast dissolving tablets, Gastric ulcer, Lanzoprazole, Solid dispersion
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