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微波辅助制备交联明胶-扑热息痛基质:采用D-最优设计进行优化

Microwave-assisted Preparation of Cross-linked Gelatin-Paracetamol Matrices: Optimization Using the D-optimal Design.

作者信息

Kuang Tan Kian, Kang Yew-Beng, Segarra Ignacio, Kanwal Ummarah, Ahsan Muhammad, Bukhari Nadeem Irfan

机构信息

International Medical University School of Pharmacy, Department of Pharmaceutical Technology, Kuala Lumpur, Malaysia

International Medical University School of Pharmacy, Department of Pharmaceutical Chemistry, Kuala Lumpur, Malaysia

出版信息

Turk J Pharm Sci. 2021 Apr 20;18(2):167-175. doi: 10.4274/tjps.galenos.2020.48902.

Abstract

OBJECTIVES

This study was conducted to assess the effect of microwave heating on the preparation of paracetamol cross-linked gelatin matrices by using the design of experiment (DoE) approach and explore the influence of the duration of microwave irradiation, the concentrations of crosslinker, and the amount of sodium bicarbonate (salt) on paracetamol release. These parameters were also compared with those of the matrices prepared via conventional heating.

MATERIALS AND METHODS

Twenty gel matrices were prepared with different durations of microwave irradiation, amounts of maize, and concentrations of sodium bicarbonate as suggested by Design Expert (DX). The percentage drug release, the coefficient of variance (CV) in release, and the mean dissolution time (MDT) were the properties explored in the designed experimentation.

RESULTS

Target responses were dependent on microwave irradiation time, cross-linker amount, and salt concentration. Classical and microwave heating did not demonstrate statistically significant difference in modifying the percentage of drug released from the matrices. However, the CVs of microwave-assisted formulations were lower than those of the gel matrices prepared via classical heating. Thus, microwave heating produced lesser variations in drug release. The optimized gel matrices demonstrated that the observed percentage of drug release, CV, and MDT were within the prediction interval generated by DX. The release mechanism of the matrix formulations followed the Peppas-Korsmeyer anomalous transport model.

CONCLUSION

The DoE-supported microwave-assisted approach could be applied to optimize the critical factors of drug release with less variation.

摘要

目的

本研究旨在采用实验设计(DoE)方法评估微波加热对扑热息痛交联明胶基质制备的影响,并探讨微波辐照时间、交联剂浓度和碳酸氢钠(盐)用量对扑热息痛释放的影响。还将这些参数与通过传统加热制备的基质的参数进行比较。

材料与方法

按照Design Expert(DX)软件的建议,制备了20种凝胶基质,其微波辐照时间、玉米用量和碳酸氢钠浓度各不相同。药物释放百分比、释放变异系数(CV)和平均溶解时间(MDT)是设计实验中探索的性质。

结果

目标响应取决于微波辐照时间、交联剂用量和盐浓度。传统加热和微波加热在改变基质中药物释放百分比方面没有显示出统计学上的显著差异。然而,微波辅助制剂的CV低于通过传统加热制备的凝胶基质的CV。因此,微波加热在药物释放方面产生的变化较小。优化后的凝胶基质表明,观察到的药物释放百分比、CV和MDT在DX生成的预测区间内。基质制剂的释放机制遵循Peppas-Korsmeyer异常转运模型。

结论

由DoE支持的微波辅助方法可用于优化药物释放的关键因素,且变化较小。

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