儿童用尼美舒利口腔崩解片制备及质量检查.doc

儿童用尼美舒利口腔崩解片制备及质量检查[摘要] 目的:制备儿童用尼美舒利口腔崩解片并考察其质量。方法:采用直接压片法制备,以有关物质、片剂硬度、崩解时间、外观、溶出度为指标进行质量检查。通过均匀设计实验,优选了崩解剂和填充剂。结果:制备的尼美舒利口腔崩解片崩解迅速,口感好,剂量小,适合儿童应用。结论:本文所得的处方和工艺可以制备优良的儿童用尼美舒利口腔崩解片。 [关键词] 尼美舒利;口腔崩解片;质量检查;稳定性研究 [中图分类号]R92 [文献标识码] A[文章编号] 1673-7210(2009)08(c)-045-03 Preparation for Pediatric Nimesulide Orally Disintegrating Tablets and quality evaluation WANG Yusong1, LI Li2, WANG Jingkun1 (1.Fuhehuaxing Pharmaceutical Group Co. Ltd of Heilongjiang, Zhaodong 151100, China;2.The First Hospital of Zhaodong,Zhaodong 151100, China) [Abstract] Objective: To study the formulation and preparation of pediatric Nimesulide orally disintegrating tablet and evaluate its quality. Methods: The tablets were prepared by direct powder compression technique. The properties of tablets,such as related substance, tablet hardness, disintegrating time, appearance, dissolution were determined.The formulation of orally disintegrating tablets was optimized by equal experiment design according to disintegrating agent and bulking agent. Results: The tablets that were prepared by the optimal formula were disintegrated quickly in mouth. It was delectable flavour and suitable for children taking. Conclusion: The preparation and formulation descried here appears promising in pediatric Nimesulide orally disintegrating tablets with good quality. [Key words] Nimesulide; Orally Disintegrating Tablets; Quality evaluation; Stability study 尼美舒利[1](Nimesulide)是德国BOEHRINGER MANHEIM公司开发的非甾体抗炎镇痛药。在芬兰、爱尔兰等国相继报道使用尼美舒利发生了肝脏严重不良反应,被相应药监部门叫停销售。因此,儿童应用尼美舒利的剂量一度引起关注。2007年9月22日,欧洲药品管理局(EMEA)要求口服尼美舒利的说明书[2]修改为,用于12岁以上人群,最大剂量不超过100 mg;2008年6月11日,中国食品药品监督管理局(SFDA)要求口服尼美舒利说明书[3]修改为:用于1岁以上儿童,剂量为5 mg/(kg?d),分2~3次服用,最大剂量不超过100 mg,2次/d。因此,儿童用的尼美舒利应该为小于50 mg的小剂量。 口腔崩解片[4]是指不需用水或只需用少量水,无需咀嚼,遇唾液迅速溶解或崩解后借吞咽动力,药物即可入胃起效的片剂。其适用于小儿吞咽困难的患者,如果在制备时采用一定的方法改善制剂的口感,可大大提高儿童患者的服药依从性,解决婴幼儿服药难的问题。 印度PANACEA公司在2002年5月2日获准上市了商品名为NIMULID-MD-KID的儿童用尼美舒利口腔崩解片,剂量为50 mg。 本文提供了一种儿童用尼美舒利口腔崩解片的制备方法,填补了国内无儿童型尼美舒利口腔崩解片的空白。