Department of Pharmaceutics, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences Brno, Palackého 1946/1, Brno, Czech Republic.
Department of Pharmaceutics, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences Brno, Palackého 1946/1, Brno, Czech Republic.
J Pharm Biomed Anal. 2018 Nov 30;161:206-213. doi: 10.1016/j.jpba.2018.08.050. Epub 2018 Aug 25.
The main objective of the presented research was to prepare an innovative carrier as a filler for detection tubes in the form of double-coated pellets with a very significant color transition during the detection of cholinesterase inhibitors such as nerve agents, organophosphorus or carbamate insecticides in liquids that is observable visually and also spectrophotometrically at 412 nm. The pellet cores were prepared by the extrusion/spheronization method. Consecutively, two different coats were applied on the pellet cores in the coating device using the Wurster column method. To increase the color change intensity, the second semipermeable coat based on Eudragit RL was applied on top of the first coat, which was formed by butyrylcholinesterase immobilized in hydroxypropyl methylcellulose. Prepared samples differing in thickness of the second coat were evaluated for their quality parameters, enzymatic activity and inhibition. The detection mechanism was based on the standard Ellman's colorimetric reaction. It was observed that the semipermeable coat prevented leaching of the enzyme into the solution and led to an increased intensity of color transition from white - yellow to white - deep yellow/orange, thus enabling a more accurate visual detection. This system allows easy, rapid and safe identification of cholinesterase inhibitors in liquids, especially chemical warfare agents.
本研究的主要目的是制备一种创新载体,作为检测管中的填充剂,以双涂层颗粒的形式存在,在检测液体中的胆碱酯酶抑制剂(如神经毒剂、有机磷或氨基甲酸酯类杀虫剂)时,具有非常显著的颜色转变,这种颜色转变可以通过肉眼观察到,也可以在 412nm 处通过分光光度法观察到。颗粒核心通过挤出/球形化方法制备。随后,在涂层设备中使用 Wurster 柱方法在颗粒核心上施加两种不同的涂层。为了提高颜色变化强度,在由固定在羟丙基甲基纤维素中的丁酰胆碱酯酶形成的第一层半渗透涂层之上,施加了第二层基于 Eudragit RL 的半渗透涂层。对不同第二层涂层厚度的制备样品进行了质量参数、酶活性和抑制作用的评估。检测机制基于标准的 Ellman 比色反应。结果表明,半渗透涂层阻止了酶向溶液中的浸出,导致颜色从白色-黄色到白色-深黄色/橙色的转变强度增加,从而能够更准确地进行目视检测。该系统允许在液体中轻松、快速和安全地识别胆碱酯酶抑制剂,特别是化学战剂。