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磁共振方法作为预测黄原胶片生物相关性行为的工具。

Magnetic Resonance Methods as a Prognostic Tool for the Biorelevant Behavior of Xanthan Tablets.

机构信息

Jožef Stefan Institute, Jamova 39, 1000 Ljubljana, Slovenia.

Faculty of Pharmacy, University of Ljubljana, Aškerčeva 7, 1000 Ljubljana, Slovenia.

出版信息

Molecules. 2020 Dec 11;25(24):5871. doi: 10.3390/molecules25245871.

Abstract

Hydrophilic matrix tablets with controlled drug release have been used extensively as one of the most successful oral drug delivery systems for optimizing therapeutic efficacy. In this work, magnetic resonance imaging (MRI) is used to study the influence of various pHs and mechanical stresses caused by medium flow (at rest, 80, or 150 mL/min) on swelling and on pentoxifylline release from xanthan (Xan) tablets. Moreover, a bimodal MRI system with simultaneous release testing enables measurements of hydrogel thickness and drug release, both under the same experimental conditions and at the same time. The results show that in water, the hydrogel structure is weaker and less resistant to erosion than the Xan structure in the acid medium. Different hydrogel structures affect drug release with erosion controlled release in water and diffusion controlled release in the acid medium. Mechanical stress simulating gastrointestinal contraction has no effect on the hard hydrogel in the acid medium where the release is independent of the tested stress, while it affects the release from the weak hydrogel in water with faster release under high stress. Our findings suggest that simultaneous MR imaging and drug release from matrix tablets together provide a valuable prognostic tool for prolonged drug delivery design.

摘要

具有控制药物释放的亲水性基质片剂已被广泛用作优化治疗效果的最成功的口服药物递送系统之一。在这项工作中,磁共振成像(MRI)用于研究不同 pH 值和由介质流动引起的机械应力(静止时为 80 或 150 毫升/分钟)对黄原胶(Xan)片剂溶胀和己酮可可碱释放的影响。此外,具有同时释放测试的双模态 MRI 系统能够在相同的实验条件下和同时测量水凝胶厚度和药物释放。结果表明,在水中,水凝胶结构比酸性介质中的 Xan 结构弱且对侵蚀的抵抗力差。不同的水凝胶结构会影响药物释放,在水中以侵蚀控制释放,在酸性介质中以扩散控制释放。模拟胃肠道收缩的机械应力对酸性介质中的硬水凝胶没有影响,其中释放与测试的应力无关,而对水凝胶的释放有影响,在高应力下释放更快。我们的研究结果表明,基质片剂的磁共振成像和药物释放的同时进行,为延长药物递送设计提供了有价值的预测工具。

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