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在生理眼液泪流量下,每日一次性治疗性隐形眼镜中抗炎药物的体外控制释放。

In vitro controlled release of an anti-inflammatory from daily disposable therapeutic contact lenses under physiological ocular tear flow.

机构信息

Biomimetic and Biohybrid Materials, Biomedical Devices, and Drug Delivery Laboratories, Department of Chemical Engineering, Auburn University, Auburn, AL 36849, USA.

出版信息

Eur J Pharm Biopharm. 2012 May;81(1):170-7. doi: 10.1016/j.ejpb.2012.01.015. Epub 2012 Feb 7.

DOI:10.1016/j.ejpb.2012.01.015
PMID:22333489
Abstract

Novel molecularly imprinted, therapeutic contact lenses capable of controlled release of the non-steroidal anti-inflammatory (NSAID) diclofenac sodium were synthesized, exploiting ionic non-covalent interactions. Poly(HEMA-co-DEAEM-co-PEG200DMA) soft contact lenses were prepared (105±5 μm thickness, diameter 15.0±0.2mm, base curve of 8.6±0.2mm) with different monomer to template ratios and dynamic release studies were conducted in artificial lacrimal solution using two different in vitro methods. Under infinite sink conditions, imprinted contact lenses demonstrated concentration dependent release kinetics. Under physiological flow rates, by increasing the M/T ratio from 1 to 10.5, the release rate decreased from 11.72 μg/h to 6.75 μg/h during the first 48 h. The release rate was more constant, moving toward zero-order release. To use these lenses as daily disposable lenses, the first 24h of release was studied and found to be linear with a rate of 17.27, 11.99, and 8.74 μg/h for M/T ratios of 1, 3.5, and 10.5, respectively. Furthermore, the lenses prepared with a M/T ratio of 10.5 released diclofenac at a rate close to the maximum dose delivered by commercial eye drops, making them ideal for use as daily disposable lenses, and potentially leading to better patient benefit with substantially increased efficacy.

摘要

利用离子非共价相互作用,合成了具有新型分子印迹、治疗作用的隐形眼镜,可控制释放非甾体抗炎药(NSAID)双氯芬酸钠。制备了不同单体与模板比的聚(HEMA-co-DEAEM-co-PEG200DMA)软性隐形眼镜(厚度 105±5μm,直径 15.0±0.2mm,基弧 8.6±0.2mm),并采用两种不同的体外方法在人工泪液中进行了动态释放研究。在无限吸收条件下,印迹隐形眼镜表现出浓度依赖性释放动力学。在生理流速下,通过将 M/T 比从 1 增加到 10.5,在前 48 小时内,释放速率从 11.72μg/h 降低到 6.75μg/h。释放速率更加稳定,趋近于零级释放。为了将这些隐形眼镜用作日抛隐形眼镜,研究了前 24 小时的释放情况,发现对于 M/T 比为 1、3.5 和 10.5 的隐形眼镜,释放速率分别为 17.27、11.99 和 8.74μg/h,呈线性关系。此外,M/T 比为 10.5 的隐形眼镜以接近商业眼药水的最大剂量释放双氯芬酸钠,使其成为日抛隐形眼镜的理想选择,并可能带来更好的患者获益,提高疗效。

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