Hydrogel-based matrices for controlled drug delivery of etamsylate: Prediction of in-vivo plasma profiles,Saudi Pharmaceutical Journal

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Hydrogel-based matrices for controlled drug delivery of etamsylate: Prediction of in-vivo plasma profiles
Saudi Pharmaceutical Journal ( IF 3.0 ) Pub Date : 2020-11-06 , DOI: 10.1016/j.jsps.2020.10.016
Soha M El-Masry ₁ , Sally A Helmy _{1,

2}

Affiliation

Objectives

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.

Methods

Characterization of the in-vitro release rate was performed by various model dependent and model independent approaches. A simple numerical convolution strategy was adopted to predict the in-vivo performance of all matrices from their in-vitro percent released data. The statistical analysis was conducted utilizing a student t-test and ANOVA.

Results

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 in-vitro release data of all prepared matrices. Pharmacokinetic parameters of etamsylate CR hydrogel matrices were significantly changed with comparison to reference product except F1.

Conclusion

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 in-vivo pharmacokinetics of etamsylate was very useful to assess the rationality of the designed matrices for the practical application in humans.

中文翻译：

用于控制依坦磺酸盐给药的基于水凝胶的基质：体内血浆曲线的预测

目标

使用各种亲水性聚合物设计口服控制释放 (CR) 乙醇酸水凝胶骨架片。此外，预测从不同 CR 基质释放的依他苯磺酸的血浆浓度-时间曲线。

方法

体外释放速率的表征通过各种模型相关和模型无关的方法进行。采用简单的数值卷积策略从所有矩阵的体外释放百分比数据中预测其体内性能。使用学生t检验和 ANOVA 进行统计分析。

结果

所有基质中依氨磺酸盐的释放都显示出与 Fickian 转运机制的偏差，除了：F2 遵循案例 II 发布，而 F9 和 F11 遵循 Fickian 扩散。基于 CR 水凝胶的基质（F4 和 F11）表现出最大的药物延迟并满足 USP 释放限制。从所有制备的基质的体外释放数据中成功预测了依坦磺酸盐的浓度-时间曲线。与除 F1 外的参考产品相比，依他苯磺酸盐 CR 水凝胶基质的药代动力学参数发生了显着变化。