Bushra Rabia, Rehman Attaur, Ghayas Sana, Zafar Farya, Ali Huma, Shafiq Yousra, Khalid Farah, Khan Maqsood Ahmed, Hanif Anas, Mustapha Omer
Department of Pharmaceutics, Faculty of Pharmacy, Dow University of Health Sciences, Karachi, Pakistan.
Department of Pharmaceutics, Faculty of Pharmacy, Ziauddin University, Karachi, Pakistan.
Pak J Pharm Sci. 2018 Nov;31(6 (Supplementary):2725-2731.
Cinitapride hydrogen tartarate is relatively a new prokinetic agent that widely prescribed for GERD and epigastric pain. Present study was aimed to develop and optimize cinitapride (1 mg) immediate release (IR) tablet formulation(s) by direct compression using central composite rotatable technique. Overall nine formulations (FC1-FC9) were generated by varying the composition of binder avicel PH 102 (X1) and superdisintegrant crospovidone (X2). The effect of interaction of excipients on hardness (Y1), friability (Y2), disintegration (Y3) and dissolution at 15 min (Y4) were analyzed by RSM plotting. On the basis of physico-chemical evaluation FC3, FC4 and FC6 were found to be the optimized formulations however; FC3 was selected to be the best trial owing to excellent drug release (100.17%) with least friability (0.14%). These IR tablets showed the release pattern similar to the Weibull model with r2 value of 0.978-0.998. The dissimilarity (f1) and similarity indexes (f2) of FC3, FC4, FC6 with the marketed product were estimated to be 2.57 and 76.51, 4.51 and 64.46, 4.32 and 66.78 respectively. Trial optimized formulations were highly stable with the shelf lives of 58-64 months. So, keeping in view the results of present investigation, it is concluded that the technique of manufacturing and optimization is found to be excellent for developing immediate release cinitapride tablets.
酒石酸西尼必利是一种相对较新的促动力药物，广泛用于治疗胃食管反流病和上腹部疼痛。本研究旨在采用中心复合旋转技术通过直接压片法开发并优化西尼必利（1毫克）速释片制剂。通过改变粘合剂微晶纤维素PH 102（X1）和超级崩解剂交联聚维酮（X2）的组成，总共制备了九种制剂（FC1 - FC9）。通过响应曲面法绘图分析了辅料相互作用对硬度（Y1）、脆碎度（Y2）、崩解度（Y3）和15分钟时溶出度（Y4）的影响。基于理化评价，发现FC3、FC4和FC6是优化后的制剂；然而，由于药物释放优异（100.17%）且脆碎度最低（0.14%），FC3被选为最佳试验制剂。这些速释片显示出与威布尔模型相似的释放模式，r2值为0.978 - 0.998。FC3、FC4、FC6与市售产品的差异度（f1）和相似度指数（f2）分别估计为2.57和76.51、4.51和64.46、4.32和66.78。试验优化后的制剂具有高度稳定性，货架期为58 - 64个月。因此，鉴于本研究结果，得出结论：所采用的制造和优化技术对于开发西尼必利速释片非常出色。
