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双层释放模型评价可溶胀药物聚电解质基质的溶出度。

Dual Release Model to Evaluate Dissolution Profiles from Swellable Drug Polyelectrolyte Matrices.

机构信息

Instituto de Investigaciones para la Industria Quimica, Consejo Nacional de Investigaciones Científicas y Tecnicas - Universidad Nacional de Salta, Salta, Argentina.

Departamento de Biologia, Bioquimica y Farmacia, Universidad Nacional del Sur, Bahia Blanca, Argentina.

出版信息

Curr Drug Deliv. 2020;17(6):511-522. doi: 10.2174/1567201817666200512093115.

DOI:10.2174/1567201817666200512093115
PMID:32394835
Abstract

BACKGROUND

Mathematical modeling in modified drug release is an important tool that allows predicting the release rate of drugs in their surrounding environment and elucidates the transport mechanisms involved in the process.

OBJECTIVE

The aim of this work was to develop a mathematical model that allows evaluating the release profile of drugs from polymeric carriers in which the swelling phenomenon is present.

METHODS

Swellable matrices based on ionic complexes of alginic acid or carboxymethylcellulose with ciprofloxacin were prepared and the effect of adding the polymer sodium salt on the swelling process and the drug release was evaluated. Experimental data from the ciprofloxacin release profiles were mathematically adjusted, considering the mechanisms involved in each stage of the release process.

RESULTS

A proposed model, named "Dual Release" model, was able to properly fit the experimental data of matrices presenting the swelling phenomenon, characterized by an inflection point in their release profile. This entails applying the extended model of Korsmeyer-Peppas to estimate the percentage of drug released from the first experimental point up to the inflection point and then a model called Lumped until the final time, allowing to adequately represent the complete range of the drug release profile. Different parameters of pharmaceutical relevance were calculated using the proposed model to compare the profiles of the studied matrices.

CONCLUSION

The "Dual Release" model proposed in this article can be used to predict the behavior of complex systems in which different mechanisms are involved in the release process.

摘要

背景

改良药物释放的数学建模是一种重要的工具,它可以预测药物在周围环境中的释放速率,并阐明涉及该过程的传输机制。

目的

本工作的目的是开发一种数学模型,该模型可以评估在存在溶胀现象的聚合物载体中药物的释放曲线。

方法

制备了基于藻酸或羧甲基纤维素与环丙沙星的离子配合物的溶胀基质,并评价了加入聚合物钠盐对溶胀过程和药物释放的影响。通过考虑释放过程各个阶段中涉及的机制,对来自环丙沙星释放曲线的实验数据进行了数学调整。

结果

提出了一种名为“双重释放”模型的模型,该模型能够适当地拟合具有溶胀现象的基质的实验数据,其释放曲线具有拐点。这需要应用扩展的 Korsmeyer-Peppas 模型来估计从第一个实验点到拐点释放的药物百分比,然后使用称为“集中”的模型直到最终时间,从而能够适当地表示药物释放曲线的完整范围。使用所提出的模型计算了不同的药物释放曲线,以比较研究基质的曲线。

结论

本文提出的“双重释放”模型可用于预测涉及不同机制的复杂系统的行为。

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