Hanif Muhammad, Shoaib Muhammad Harris, Yousuf Rabia Ismail, Sattar Shahnila, Nadeem Muhammad, Hussain Liaqat, MZia Muhammad Usman, Muhammad Iyad Naeem, Uzair Muhammad, Qadir Imran
Department of Pharmaceutics, Faculty of Pharmacy, University of Karachi, Karachi, Pakistan / Department of Pharmacy, Bahauddin Zakariya University, Multan, Pakistan.
Department of Pharmaceutics, Faculty of Pharmacy, University of Karachi, Karachi, Pakistan.
Pak J Pharm Sci. 2014 Jul;27(4):785-92.
Simple and cost effective study consisting of three steps, comparison of micromeritic properties of different blends i.e. placebo without API and Nimesulide containing, Use of central composite design (CCRD) for intermediate release Nimesulide tablets and stability results of three selected Nimesulide tablet formulations which were calculated by using R Gui. Different concentrations of Avicel, hydroxypropyl methyl cellulose (HPMC) and magnesium stearate were used as variables in central composite design and two types blend i.e., with or without Nimesulide were selected for bulk density, tap density, percentage compressibility; angle of repose and Hausner's ratio. Blending rate constant was performed after applying the different mixing times like 3, 6, 9 and 12 minutes. Twenty intermediate release formulations were designed and three formulations were chosen for compression by direct compression method on the basis of compressibility index. Physicochemical properties and best release pattern in four hours in different dissolution medium were successfully measured. Relative densities, porosity of tablets were compared with tensile strength of tablet and weight variation, hardness, friability and dissolution was performed by simple experiments. Presence of Nimesulide in the bulk increased all micromeratic tests while 9 minutes was best mixing time. The hardness of NM containing tablets increased with the increase of relative density. The release pattern was further analyzed by model dependent i.e. zero order, first order and Higuchi, Korse-meyer and Pappas, Hixson Crowell and model independent kinetic model i.e., f2 value respectively. R Gui explained the F16 formulation shows the best result in stability studies with shelf life 72 months.
比较不同混合物（即不含活性成分的安慰剂和含尼美舒利的混合物）的粉体学性质；使用中心复合设计（CCRD）制备尼美舒利缓释片；利用R Gui计算三种选定的尼美舒利片剂配方的稳定性结果。在中心复合设计中，将不同浓度的微晶纤维素、羟丙基甲基纤维素（HPMC）和硬脂酸镁用作变量，并选择两种类型的混合物（即含或不含尼美舒利）来测定堆密度、振实密度、压缩率百分比、休止角和豪斯纳比率。在施加3、6、9和12分钟等不同混合时间后进行混合速率常数测定。设计了20种缓释配方，并根据压缩指数选择了三种配方通过直接压片法进行压片。成功测定了不同溶出介质中片剂在4小时内的物理化学性质和最佳释放模式。通过简单实验比较了片剂的相对密度、孔隙率与片剂的抗张强度以及重量差异、硬度、脆碎度和溶出度。尼美舒利的存在提高了所有粉体学测试结果，而9分钟是最佳混合时间。含尼美舒利片剂的硬度随相对密度的增加而增加。通过依赖模型的方法（即零级、一级和 Higuchi、Korse - meyer和Pappas、Hixson Crowell模型）以及不依赖模型的动力学模型（即f2值）进一步分析释放模式。R Gui解释说，F16配方在稳定性研究中显示出最佳结果，保质期为72个月。
