·实验研究·

基于预混辅料的拉莫三嗪口腔崩解片的制备

查静，王铁杰，王思明，涂家生

(中国药科大学药剂教研室，江苏 南京 210009)

摘要：目的由预混辅料入手，制备拉莫三嗪口腔崩解片。方法以异麦芽酮糖醇、微晶纤维素和交联聚维酮为主要辅料，使用湿法制粒的方法制备预混辅料，并测定了预混辅料产品的粉体学性质。选用拉莫三嗪为主药，与预混辅料及少量崩解剂、润滑剂和矫味剂，通过粉末直压的方法制备拉莫三嗪口腔崩解片，并对拉莫三嗪口腔崩解片进行基本的体外评价。结果通过单因素考察和正交试验，预混辅料的最终处方组成为：异麦芽酮糖醇与微晶纤维素的比例为3∶4，加入8%交联聚维酮。拉莫三嗪口腔崩解片的最优处方组成(按1 000片计)为：25 g 拉莫三嗪，137 g预混辅料，14.4 g低取代羟丙基纤维素，1.8 g硬脂酸镁，1.8 g矫味剂。拉莫三嗪口腔崩解片的崩解时限为35 s，且在5 min内溶出完全。结论根据试验，制备的预混辅料的性质优良，口腔崩解片的崩解时限、口感和溶出度等均符合规定。

关键词：预混辅料；口腔崩解片；拉莫三嗪

基金项目：深圳市战略新兴产业发展专项资金项目(No.JCYJ20130402144215892)

作者简介：查静，女，研究方向：药物新制剂和新技术，E-mail:zj20150501@163.com

通讯作者：涂家生，男，教授，博士生导师，研究方向：药物新制剂和新技术，Tel:13605159819,E-mail:jiashengtu@cpu.edu.cn

中图分类号：R944.4文献标识码：A

Preparation of Lamotrigine Orally Disintegrating Tablets based on the co-processed exicipient

ZHAJing,WANGTie-jie,WANGSi-ming,TUJia-sheng

(DepartmentofPharmaceutics，ChinaPharmaceuticalUniversity,Nanjing210009,China)

Abstract：ObjectiveTo prepare Lamotrigine Orally Disintegrating Tablets (ODTs) based on the co-processed excipients.MethodsFirstly，to prepare the co-processed excipient consisting of isomalt,microcrystalline cellulose and crospovidone by wet granulation method.Afterwards,Lamotrigine ODTs was directly compressed after mixing the co-processed excipient with a small amount of disintegrant，taste-masked agents and magnesium stearate，and the formula optimization was conducted.Finally,the micromeritic properties of co-processed excipient and the disintegration time of Lamotrigine ODTs with the optimal formula were investigated.ResultsThe desirable co-processed excipient composed of isomalt/microcrystalline cellulose at a ratio of 3∶4 and 8% crospovidone.And the components of the optimal formula of Lamotrigine ODTs(in 1 000) included 25 g lamotrigine，137 g co-processed excipient，14.4 g low-substituted hydroxypropyl cellulose，1.8 g magnesium stearate，1.8 g taste-masked agents.From the in-vitro study，the disintegration and dissolution time of Lmotrigine ODTs were within 35 seconds and 5 minutes，respectively.ConclusionAccording to the experiments,the micromeritic properties of co-processed excipients was good and the disintegration time,the dissolution time and the taste of ODTs were eligible.

Key words:Co-processed exicipient;Orally disintegrating tablets;Lamotrigine

口腔崩解片(orally disintegrating tablet，ODT)是近年来发展起来的一种新型速释制剂，其特点是药物置于舌面后，不需用水或只需少量水，也无需咀嚼，就能迅速崩解，借助吞咽动作入胃起效。……