El-Masry Soha M, Helmy Sally A
Department of Pharmaceutics, Faculty of Pharmacy, Damanhour University, Damanhour, Egypt.
Department of Clinical and Hospital Pharmacy, Faculty of Pharmacy, Taibah University, AL-Madinah AL-Munawarah, Saudi Arabia.
Saudi Pharm J. 2020 Dec;28(12):1704-1718. doi: 10.1016/j.jsps.2020.10.016. Epub 2020 Nov 6.
To design oral controlled release (CR) hydrogel matrix tablets of etamsylate using various hydrophilic polymers. Additionally, to predict plasma concentration-time profiles of etamsylate released from different CR matrices.
Characterization of the release rate was performed by various model dependent and model independent approaches. A simple numerical convolution strategy was adopted to predict the performance of all matrices from their percent released data. The statistical analysis was conducted utilizing a student -test and ANOVA.
The release of etamsylate from all matrices showed a deviation from Fickian transport mechanism except; F2 followed Case II release whereas, F9 and F11 obeyed Fickian diffusion. CR hydrogel based-matrices (F4 and F11) demonstrated the maximum drug retardation and satisfied the USP release limits. Concentration-time profiles of etamsylate were predicted successfully from the release data of all prepared matrices. Pharmacokinetic parameters of etamsylate CR hydrogel matrices were significantly changed with comparison to reference product except F1.
The designed (F2-F11) matrices had the capability to extend the plasma level of etamsylate for an adequate time. However, F4 and F11 were considered the most ideal formulations for once daily application of etamsylate. The prediction of pharmacokinetics of etamsylate was very useful to assess the rationality of the designed matrices for the practical application in humans.
使用多种亲水性聚合物设计酚磺乙胺口服控释（CR）水凝胶基质片。此外，预测从不同CR基质中释放的酚磺乙胺的血药浓度-时间曲线。
通过各种依赖模型和不依赖模型的方法对释放速率进行表征。采用简单的数值卷积策略，根据所有基质的释放百分比数据预测其性能。使用学生t检验和方差分析进行统计分析。
除F2遵循Ⅱ型释放，F9和F11遵循菲克扩散外，所有基质中酚磺乙胺的释放均偏离菲克转运机制。基于CR水凝胶的基质（F4和F11）表现出最大的药物缓释效果，并符合美国药典释放限度。根据所有制备基质的释放数据成功预测了酚磺乙胺的浓度-时间曲线。与参比制剂相比，除F1外，酚磺乙胺CR水凝胶基质的药代动力学参数有显著变化。
所设计的（F2-F11）基质有能力在足够长的时间内延长酚磺乙胺的血药浓度。然而，F4和F11被认为是酚磺乙胺每日一次给药的最理想制剂。酚磺乙胺药代动力学的预测对于评估所设计基质在人体实际应用中的合理性非常有用。
