The present study investigates the use of nimodipine-polyethylene glycol solid dispersions for the development of effervescent controlled release floating tablet formulations. The physical state of the dispersed nimodipine in the polymer matrix was characterized by differential scanning calorimetry, powder X-ray diffraction, FT-IR spectroscopy and polarized light microscopy, and the mixture proportions of polyethylene glycol (PEG), polyvinyl-pyrrolidone (PVP), hydroxypropylmethylcellulose (HPMC), effervescent agents (EFF) and nimodipine were optimized in relation to drug release (% release at 60 min, and time at which the 90% of the drug was dissolved) and floating properties (tablet's floating strength and duration), employing a 25-run D-optimal mixture design combined with artificial neural networks (ANNs) and genetic programming (GP). It was found that nimodipine exists as mod I microcrystals in the solid dispersions and is stable for at least a three-month period. The tablets showed good floating properties and controlled release profiles, with drug release proceeding via the concomitant operation of swelling and erosion of the polymer matrix. ANNs and GP both proved to be efficient tools in the optimization of the tablet formulation, and the global optimum formulation suggested by the GP equations consisted of PEG=9%, PVP=30%, HPMC=36%, EFF=11%, nimodipine=14%.

译文

:本研究调查了尼莫地平-聚乙二醇固体分散体在泡腾控释浮动片剂配方开发中的应用。通过差示扫描量热法,粉末X射线衍射,FT-IR光谱和偏振光显微镜以及聚乙二醇(PEG),聚乙烯吡咯烷酮(PVP)的混合比例来表征分散的尼莫地平在聚合物基质中的物理状态。 ,羟丙基甲基纤维素(HPMC),泡腾剂(EFF)和尼莫地平针对药物释放(60分钟时的释放百分比以及90%的药物溶解时间)和漂浮特性(片剂的漂浮强度和持续时间)进行了优化,采用了25次D-最优混合设计,并结合了人工神经网络(ANN)和遗传编程(GP)。已发现尼莫地平以mod I微晶形式存在于固体分散体中,并且稳定至少三个月。片剂表现出良好的漂浮性和控释特性,同时伴随着聚合物基质的溶胀和侵蚀而进行药物释放。人工神经网络和GP均被证明是优化片剂配方的有效工具,GP方程建议的全局最优配方包括PEG = 9%,PVP = 30%,HPMC = 36%,EFF = 11%,尼莫地平= 14%。

+1
+2
100研值 100研值 ¥99课程
检索文献一次
下载文献一次

去下载>

成功解锁2个技能,为你点赞

《SCI写作十大必备语法》
解决你的SCI语法难题!

技能熟练度+1

视频课《玩转文献检索》
让你成为检索达人!

恭喜完成新手挑战

手机微信扫一扫,添加好友领取

免费领《Endnote文献管理工具+教程》

微信扫码, 免费领取

手机登录

获取验证码
登录