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通过静电纺丝制备的速溶对乙酰氨基酚/咖啡因纳米纤维。

Fast dissolving paracetamol/caffeine nanofibers prepared by electrospinning.

作者信息

Illangakoon U Eranka, Gill Hardyal, Shearman Gemma C, Parhizkar Maryam, Mahalingam Sunthar, Chatterton Nicholas P, Williams Gareth R

机构信息

UCL School of Pharmacy, University College London, 29-39 Brunswick Square, London WC1N 1AX, United Kingdom.

School of Human Sciences, Faculty of Life Sciences and Computing, London Metropolitan University, 166-220 Holloway Road, London N7 8DB, United Kingdom.

出版信息

Int J Pharm. 2014 Dec 30;477(1-2):369-79. doi: 10.1016/j.ijpharm.2014.10.036. Epub 2014 Oct 17.

Abstract

A series of polyvinylpyrrolidone fibers loaded with paracetamol (PCM) and caffeine (CAF) was fabricated by electrospinning and explored as potential oral fast-dissolving films. The fibers take the form of uniform cylinders with smooth surfaces, and contain the drugs in the amorphous form. Drug-polymer intermolecular interactions were evidenced by infrared spectroscopy and molecular modeling. The properties of the fiber mats were found to be highly appropriate for the preparation of oral fast dissolving films: their thickness is around 120-130 μm, and the pH after dissolution in deionized water lies in the range of 6.7-7.2. Except at the highest drug loading, the folding endurance of the fibers was found to be >20 times. A flavoring agent can easily be incorporated into the formulation. The fiber mats are all seen to disintegrate completely within 0.5s when added to simulated saliva solution. They release their drug cargo within around 150s in a dissolution test, and to undergo much more rapid dissolution than is seen for the pure drugs. The data reported herein clearly demonstrate that electrospun PCM/CAF fibers comprise excellent candidates for oral fast-dissolving films, which could be particularly useful for children and patients with swallowing difficulties.

摘要

通过静电纺丝制备了一系列负载扑热息痛(PCM)和咖啡因(CAF)的聚乙烯吡咯烷酮纤维,并将其作为潜在的口腔速溶膜进行了研究。这些纤维呈表面光滑的均匀圆柱体形状,且药物以无定形形式存在。红外光谱和分子模拟证明了药物与聚合物之间的分子间相互作用。发现纤维毡的性能非常适合制备口腔速溶膜:其厚度约为120 - 130μm,在去离子水中溶解后的pH值在6.7 - 7.2范围内。除了最高载药量情况外,纤维的耐折性大于20次。调味剂可轻松加入到配方中。当将纤维毡加入模拟唾液溶液中时,发现它们在0.5秒内完全崩解。在溶出试验中,它们在约150秒内释放药物,并且比纯药物的溶解速度快得多。本文报道的数据清楚地表明,静电纺丝PCM/CAF纤维是口腔速溶膜的极佳候选材料,这对于儿童和吞咽困难的患者可能特别有用。

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