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Formulation and Evaluation of fast dissolving films of Granisetron Hydrochloride

机译:盐酸格拉司琼快速溶解膜的研制与评价

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Granisetron hydrochloride is a novel serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy. It is well absorbed from the gastrointestinal tract, but its oral bioavailability is low (60%) due to extensive first-pass metabolism which makes it an ideal candidate for rapid release drug delivery system. In the present work we have prepared and evaluated fast dissolving oral films of Granisetron hydrochloride by solvent casting method using different concentrations polymers HPMC, PVA and their combinations. Mannitol was used as a disintegrating agent and Propylene glycol as a plasticizer. The prepared oral films were evaluated for Physical appearance, texture, Weight uniformity, thickness uniformity, percentage moisture absorption, disintegration time, drug content uniformity, folding endurance, tensile strength, in-vitro drug release, and stability studies. In-vitro release rate of Granisetron hydrochloride was studied in phosphate buffer pH 6.8. F1, F5 and F7 showed maximum release rate about 94.95%, 95.98% and 96.29% in 180 seconds respectively, whereas F3 showed 60.98%. Short term stability studies of selected films indicated that there is no significant change with respect to physical appearance, disintegration time, drug content and in-vitro drug release.
机译:盐酸Granisetron是一种新型的5羟色胺5-HT3受体拮抗剂,可作为止吐药来治疗化疗后的恶心和呕吐。它从胃肠道吸收良好,但是由于广泛的首过代谢,其口服生物利用度低(60%),这使其成为快速释放药物递送系统的理想候选者。在目前的工作中,我们已经使用不同浓度的聚合物HPMC,PVA及其组合,通过溶剂流延法制备和评估了盐酸Granisetron的速溶口腔膜。甘露醇用作崩解剂,丙二醇用作增塑剂。评价制备的口腔膜的物理外观,质地,重量均匀性,厚度均匀性,吸湿百分数,崩解时间,药物含量均匀性,耐折性,抗张强度,体外药物释放和稳定性研究。在pH 6.8的磷酸盐缓冲液中研究了Granisetron盐酸盐的体外释放速率。 F1,F5和F7在180秒内显示最大释放率分别为94.95%,95.98%和96.29%,而F3显示为60.98%。选定膜的短期稳定性研究表明,其物理外观,崩解时间,药物含量和体外药物释放没有明显变化。

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