Department of Pharmaceutics, Institute of Pharmaceutical Sciences, Jinnah Sindh Medical University, Karachi, Pakistan.
Department of Pharmaceutics, Faculty of Pharmacy, Dow University of Health Sciences, Karachi, Pakistan.
Pak J Pharm Sci. 2021 Jul;34(4(Supplementary)):1519-1525.
Empagliflozin is a selective inhibitor of sodium glucose co-transporter II, given as mono therapy or an add-on treatment to reduce the glycated hemoglobin levels in type 2 diabetes. This work deals with designing, formulating and optimizing empagliflozin (10mg) immediate release (IR) tablets by direct compression technique using different excipients. Through central composite rotatable design (CCRD), total nine formulations (EF1-EF9) were generated by changing the composition of binder avicel PH 102® (X1) and superdisintegrant acdisol⌖ (X2). Formulation runs with in suitable weight range and powder properties were subjected to compression. The influence of interaction of excipients on friability (Y1), hardness (Y2) and disintegration (Y3) were analyzed by fitting the polynomial quadratic model with response surface methodology (RSM). Trials EF2, EF7, EF8 and EF9 exhibited acceptable tablet attributes upon physico-chemical testing. Different dissolution models were applied to observe the in vitro drug release pattern in phosphate buffer of pH 6.8. The cumulative drug release of IR tablet batches followed the Weibull kinetics with regression coefficient (r2) values of 0.983-0.992. Empagliflozin trials were exposed to accelerated storage conditions (40±2°C/ 75±5% RH) for stability testing. Shelf life period of exposed formulations were computed in range of 22 to 25 months. Keeping in view of the results, it is concluded that the employed technique of preparation and optimization are observed to be excellent for developing immediate release empagliflozin (10mg) tablets.
恩格列净是一种选择性钠-葡萄糖协同转运蛋白 2 抑制剂，可单药治疗或与其他药物联合治疗，降低 2 型糖尿病患者的糖化血红蛋白水平。本工作涉及通过直接压片技术，使用不同的辅料设计、制备和优化恩格列净（10mg）速释片。通过中心组合旋转设计（CCRD），通过改变粘合剂 Avicel PH 102®（X1）和超级崩解剂 acdisol⌖（X2）的组成，生成了 9 种制剂（EF1-EF9）。在合适的重量范围内和粉末特性下进行制剂运行，然后进行压缩。通过响应面法（RSM）拟合多项式二次模型，分析辅料相互作用对脆碎度（Y1）、硬度（Y2）和崩解（Y3）的影响。试验 EF2、EF7、EF8 和 EF9 在物理化学测试中表现出可接受的片剂属性。不同的溶出模型被应用于观察在 pH6.8 的磷酸盐缓冲液中的体外药物释放模式。IR 片剂批次的累积药物释放遵循 Weibull 动力学，回归系数（r2）值为 0.983-0.992。对恩格列净试验进行了加速储存条件（40±2°C/75±5%RH）的稳定性测试。暴露制剂的货架期计算范围为 22 至 25 个月。鉴于这些结果，可以得出结论，所采用的制备和优化技术对于开发恩格列净（10mg）速释片是非常有效的。
