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一种用于左旋多巴口服给药的新型pH响应性聚电解质水凝胶复合物。第二部分:基于IPEC的片剂基质的表征与配方

A novel pH-responsive interpolyelectrolyte hydrogel complex for the oral delivery of levodopa. Part II: characterization and formulation of an IPEC-based tablet matrix.

作者信息

Ngwuluka Ndidi C, Choonara Yahya E, Kumar Pradeep, du Toit Lisa C, Khan Riaz A, Pillay Viness

机构信息

Wits Advanced Drug Delivery Platform Research Unit, Department of Pharmacy and Pharmacology, School of Therapeutic Sciences, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg, 7 York Road, Parktown, 2193, South Africa.

出版信息

J Biomed Mater Res A. 2015 Mar;103(3):1085-94. doi: 10.1002/jbm.a.35258. Epub 2014 Jun 17.

Abstract

This study was undertaken in order to apply a synthesized interpolyelectrolyte complex (IPEC) of polymethacrylate and carboxymethylcellulose as a controlled release oral tablet matrix for the delivery of the model neuroactive drug levodopa. The IPEC (synthesized in Part I of this work) was characterized by techniques such as Fourier Transform Infra-Red (FTIR) spectroscopy, Differential Scanning Calorimetry (DSC), Advanced DSC (ADSC), and Scanning Electron Microscopy (SEM). The tablet matrices were formulated and characterized for their drug delivery properties and in vitro drug release. FTIR confirmed the interaction between the two polymers. The IPEC composite generated tablet matrices with a hardness ranging from 19.152-27.590 N/mm and a matrix resilience ranging between 42 and 46%. An IPEC of polymethacrylate and carboxymethylcellulose was indeed an improvement on the inherent properties of the native polymers providing a biomaterial with the ability to release poorly soluble drugs such as levodopa at a constant rate over a prolonged period of time.

摘要

本研究旨在应用聚甲基丙烯酸酯与羧甲基纤维素的合成聚电解质复合物(IPEC)作为控释口服片剂基质,用于递送模型神经活性药物左旋多巴。通过傅里叶变换红外(FTIR)光谱、差示扫描量热法(DSC)、高级DSC(ADSC)和扫描电子显微镜(SEM)等技术对IPEC(在本工作的第一部分合成)进行了表征。对片剂基质进行了配方设计,并对其药物递送特性和体外药物释放进行了表征。FTIR证实了两种聚合物之间的相互作用。IPEC复合材料制成的片剂基质硬度范围为19.152 - 27.590 N/mm,基质弹性恢复率在42%至46%之间。聚甲基丙烯酸酯与羧甲基纤维素的IPEC确实改善了天然聚合物的固有性能,提供了一种能够在长时间内以恒定速率释放左旋多巴等难溶性药物的生物材料。

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