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通过关闭分子内光诱导电子转移增强倍他斯汀荧光:在眼药水和房水中的应用。

Boosting bepotastine fluorescence by switching off intramolecular photoinduced electron transfer: Application to eye drops and aqueous humor.

作者信息

Saad Aya Magdy, Nasr Jenny Jeehan Mohamed, El-Deen Asmaa Kamal

机构信息

Pharmaceutical Analytical Chemistry Department, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt.

Pharmaceutical Analytical Chemistry Department, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt; Department of Pharmaceutical Analytical Chemistry, Faculty of Pharmacy, Mansoura National University, Gamasa 7731168, Egypt.

出版信息

Spectrochim Acta A Mol Biomol Spectrosc. 2025 Feb 15;327:125335. doi: 10.1016/j.saa.2024.125335. Epub 2024 Oct 28.

Abstract

Bepotastine (BPT), a second-generation antihistamine used for treating allergic rhinitis and pruritus, requires precise dosage calculation and accurate measurement in aqueous humor to ensure therapeutic efficacy and avoid adverse effects. This study presents a highly sensitive, cost-effective, readily-implementable, and ecologically sustainable method to detect BPT by enhancing its weak native fluorescence. This has been achieved by switching off the intramolecular photoinduced electron transfer (PET) process through phosphoric acid-induced protonation of the nitrogen in the piperidinyl ring. Further fluorescence enhancement was achieved by incorporating a solution of sodium dodecyl sulfate (SDS) surfactant thus increasing the quantum yield of BPT up to 10 folds. Fluorescence intensity was measured at 425 nm following excitation at 265 nm. The method, validated according to ICH guidelines, demonstrated linearity over the range of 0.70-6.0 µg/mL with a correlation coefficient of 0.9972 and a low detection limit of 0.046 µg/mL. It was successfully applied to measure BPT in aqueous humor and eye drops with % recoveries between 97.59 % and 102.62 %. Finally, sustainability was assessed using various tools, confirming the method's practicality for routine clinical and pharmaceutical quality control analyses.

摘要

贝波他斯汀(BPT)是一种用于治疗过敏性鼻炎和瘙痒症的第二代抗组胺药,在房水中需要精确的剂量计算和准确的测量,以确保治疗效果并避免不良反应。本研究提出了一种高灵敏度、经济高效、易于实施且生态可持续的方法,通过增强其微弱的天然荧光来检测BPT。这是通过磷酸诱导哌啶环中氮的质子化来关闭分子内光诱导电子转移(PET)过程实现的。通过加入十二烷基硫酸钠(SDS)表面活性剂溶液进一步增强荧光,从而使BPT的量子产率提高了10倍。在265nm激发后,于425nm处测量荧光强度。该方法根据ICH指南进行了验证,在0.70 - 6.0µg/mL范围内呈线性,相关系数为0.9972,检测限低至0.046µg/mL。它成功应用于测量房水和滴眼液中的BPT,回收率在97.59%至102.62%之间。最后,使用各种工具评估了可持续性,证实了该方法在常规临床和药物质量控制分析中的实用性。

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