普拉克索缓释片的制备:体外研究

K. Venkateswarlu, Heerasingh Thakur, Thumati Nagendra Bhaskar Babu
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引用次数: 8

摘要

本研究制备了普拉克索(PMPL)缓释片,并对其进行了评价。采用不同浓度的聚合物和赋形剂配制配方,以获得所需的24 h缓释期。采用湿造粒法制备颗粒,并对其休止角(AR)、堆积密度(BD)、疏通密度(TD)、卡尔指数(CI)和豪斯纳比(HR)进行评价。颗粒具有良好的流动性能。对压缩片的重量变化、硬度、脆度、药物含量、厚度和体外释放度进行评价。配方(F9)含有羧甲基纤维素钠(SCMC10%)和两种等级的微晶纤维素(MCC PH101, MCC PH102)作为稀释剂,每天给药一次,释放效果理想。发现药物释放遵循一级动力学,特别是具有非粘性转运机制的扩散。优化处方F9的药物体外释放模式与上市产品MIRAPEX ER相似(相似因子f2 = 66.43),且释放模式优于上市产品。结果表明,F9制剂可作为每日1次的有效治疗帕金森病的合适候选制剂。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Fabrication of Extended Release Tablets of Pramipexole: In-vitro Studies
In this study, Extended release (ER) tablets of Pramipexole (PMPL) to be taken once daily were prepared and evaluated. Formulations were developed using different polymers and excipients in varying concentrations to get the desired extended release period of 24 h. The granules were prepared by wet granulation method and evaluated for angle of repose (AR), bulk density (BD), tapped density (TD), Carr’s index (CI) and Hausner’s ratio (HR). The granules showed satisfactory flow properties. The compressed tablets were evaluated for weight variation, hardness, friability, drug content, thickness and in-vitro drug release. Formulation (F9) containing Sodium carboxy methyl cellulose (SCMC10%) and both grades of Micro Crystalline Cellulose (MCC PH101, MCC PH102) as diluents gave the desired release for once a day administration. The drug release was found to be followed first order kinetics and particularly diffusion with non-fickian transport mechanism. In-vitro release pattern of drug from the optimized formulation F9 was found to be similar (i.e. the similarity factor f2 was found to be 66.43) with the marketed product MIRAPEX ER and showed better drug release pattern than the marketed product. It was revealed from the results that the formulation F9 could be the suitable candidate for the effective treatment of Parkinson’s disease as once daily formulation.
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