盐酸阿米替林微孔的渗透泵控释片的制备及体外释放度的考察.doc

盐酸阿米替林微孔渗透泵控释片的制备及体外释放度的考察 冯晶1，周苏1，郭斌2 本文档由【中文word文档库】提供，转载分发敬请保留本信息； 中文word文档库免费提供海量范文、教育、学习、政策、报告和经济类word文档。 （1.辽宁医学院，锦州，121000；2.辽宁医学院附属第一医院，锦州，121000）190mg,包衣液中PEG400为10％4%；该制剂体外释放行为符合零级释放规律，24h累积释放度＞90%。结论 体外释药速度缓慢、平稳。可进一步进行体内释药行为考察。 关键词：盐酸阿米替林；微孔渗透泵控释片；释放；正交设计 Preparation and drug release in vitro of the Amitriptyline Hydrochloride Controlled porosity osmotic pump tablets FENG Jing1,ZHOU Su1,GUO Bin2 (1.Liaoning Medical College，Jinzhou ,121001;2.The First Affiliated Hospital of Liaoning Medical College , Jinzhou,121000) ABSTRACT OBJECTIVE:To investigate formula of Amitriptyline Hydrochloride Controlled porosity osmotic pump tablets and influencing factor of the in vitro release . Methods: the cumulative percent release was used as the evaluation stantard for the drug release profile in vitro. According to investigate of the univariate and the orthogonal design of Amitriptyline Hydrochloride Controlled porosity osmotic pump tablets to selected optimal formula .Results: the best formula of self-made Amitriptyline Hydrochloride Controlled porosity osmotic pump tablets is lactose:190mg,PEG400:10%,and coating increases 4% on weight.It complies to the character of zero-order release.And the release of it in 24h were greater than 90%.Conclusion:the drug release profile of self-made Amitriptyline Hydrochloride Controlled porosity osmotic pump tablets in vitro is slower and steadier . It can be further investigated by the in vitro release. Key words:Amitriptyline Hydrochloride;Controlled porosity osmotic pump tablets;Release;Orthogonal design 盐酸阿米替林临床上用于治疗抑郁症已有多年历史，最近美国埃默里大学科研人员研究发现，该药能直接促进大脑中“神经生长因子”的发展，维持神经细胞中的含氧量和葡萄糖含量，从而激发神经细胞向外伸展神经突，以连结其他神经细胞，促进大脑发育。另外，盐酸阿米替林还能抑制神经毒素红藻氨酸的产生。这显示了它不同于很多抗抑郁药物的药效机制。这项研究结果将发表在最新一期美国《化学与生物学》杂志上。由于盐酸阿米替林是抗抑郁的常用药，而患有抑郁症的病人在没有看护的情况下有时不能保证每天2-3次自行服用药物。根据药理学研究表明[1]，阿米替林口服后，在整个胃肠道内都有吸收易于把给药时间设计为每24小时服用一次的控释制剂。一般认为，缓控释制剂适用于半衰期短的药物（T1/2为2-8h1h或大于12h的不宜制成缓控释制剂。但由于制剂技术的进步，对口服缓控释制剂药物的选择已发生了一些观念性的变化，许多限制已被打破。如地西泮半衰期长达32h，《美国药典》也收载其缓释制剂的产品[2]。笔