Faculty of Pharmacy, Gomal University, DI Khan, KPK, Pakistan.
Faculty of Pharmacy, Gomal University, DI Khan, KPK, Pakistan; Department of Pharmacy, Quaid-i- Azam University, Islamabad, Pakistan.
Int J Pharm. 2015 Dec 30;496(2):759-65. doi: 10.1016/j.ijpharm.2015.10.051. Epub 2015 Nov 3.
Current study was aimed to develop 200mg controlled release matrix tablets of Losartan Potassium using Ethocel 100 Premium and Ethocel 100 FP Premium as rate controlling polymer. In-vitro studies were performed according to USP Method-I in phosphate buffer (PH 6.8) using pharma test dissolution apparatus. The temperature of the dissolution medium was kept constant at 37±0.5°C at 100rpm. Flow properties, physical quality control tests, effect of polymer size and drug-to-polymers ratios were studied using different kinetics models such as 1st-order, zero-order, Hixon Crowell model, Highuchi model and Power law. Difference factor f1 and similarity factor f2 were applied for dissolution profiles against Cardaktin® tablets used as a reference formulation. The matrices with polymer ethocel 100 FP Premiums have prolonged the drug release rate as compared to polymer ethocel 100 Premiums. The n values matrices with polymer ethocel grade 100 ranged from 0.603 to 0.857 indicating that the drug release occurred by anomalous non fickian diffusion kinetics while then value of reference Cardaktin® tablet was measured as 0.125 indicating that these tablets do not follow power law. The dissolution profiles of test formulations were different than that of reference Cardaktin®. This suggests the polymer Ethocel grade 100 can be proficiently incorporated in fabrication and development of once a day controlled release matrix tablets.
本研究旨在开发以 Ethocel 100 Premium 和 Ethocel 100 FP Premium 为控释聚合物的 200mg 控释基质片剂。根据 USP 方法-I，在磷酸盐缓冲液（pH6.8）中进行体外研究，使用 pharma test 溶解装置。溶解介质的温度在 37±0.5°C 下保持恒定，转速为 100rpm。使用不同的动力学模型（如一级、零级、Hixon Crowell 模型、Highuchi 模型和幂律模型）研究了流动特性、物理质量控制试验、聚合物粒径和药物-聚合物比的影响。差异因子 f1 和相似因子 f2 用于评估与用作参考制剂的 Cardaktin®片剂的溶出曲线。与聚合物 Ethocel 100 Premiums 相比，聚合物 Ethocel 100 FP Premiums 的基质延长了药物释放速率。聚合物 Ethocel 等级 100 的 n 值基质范围从 0.603 到 0.857，表明药物释放是通过异常非菲克扩散动力学发生的，而参考 Cardaktin®片剂的值为 0.125，表明这些片剂不遵循幂律。测试制剂的溶出曲线与参考 Cardaktin®片剂不同。这表明聚合物 Ethocel 等级 100 可以有效地纳入每天一次控释基质片剂的制造和开发。
