关键词: Anticancer drug Erlotinib hydrochloride Particle size Pharmaceutical particles RESS-C method

Mesh : Erlotinib Hydrochloride / chemistry Nanoparticles / chemistry Particle Size Antineoplastic Agents / chemistry Temperature Chromatography, Supercritical Fluid / methods Drug Compounding / methods Pressure

来  源:   DOI:10.1038/s41598-024-64477-8   PDF(Pubmed)

Abstract:
The size of the drug particles is one of the essential factors for the proper absorption of the drug compared to the dose of the drug. When particle size is decreased, drug uptake into the body increases. Recent studies have revealed that the rapid expansion of supercritical solution with cosolvent plays a significant role in preparing micron and submicron particles. This paper examines the preparation of Erlotinib hydrochloride nanoparticles using a supercritical solution through the cosolvent method for the first time. An examination of the parameters of temperature (318-338 K), pressures (15-25 MPa) and nozzle diameter (300-700 μm) was investigated by Box-Behnken design, and their respective effects on particle size revealed that the nozzle diameter has a more significant impact on particle size than the other parameters. The smallest particles were produced at temperature 338 K, pressure 20 MPa, and nozzle diameter 700 μm. Besides, the ERL nanoparticles were characterized using SEM, DLS, XRD, FTIR, and DSC analyses. Finally, the results showed that the average size of the ERL particles decreased from 31.6 μm to 200-1100 nm.
摘要:
与药物剂量相比,药物颗粒的大小是药物适当吸收的重要因素之一。当颗粒尺寸减小时,进入体内的药物吸收增加。最近的研究表明,超临界溶液与共溶剂的快速膨胀在制备微米和亚微米颗粒中起着重要作用。本文首次考察了通过共溶剂法利用超临界溶液制备盐酸厄洛替尼纳米粒。检查温度参数(318-338K),压力(15-25MPa)和喷嘴直径(300-700μm)通过Box-Behnken设计进行了研究,以及它们各自对颗粒尺寸的影响表明,喷嘴直径对颗粒尺寸的影响比其他参数更显著。最小的颗粒是在338K的温度下产生的,压力20MPa,和喷嘴直径700μm。此外,使用SEM对ERL纳米粒子进行了表征,DLS,XRD,FTIR,和DSC分析。最后,结果表明,ERL颗粒的平均尺寸从31.6μm减小到200-1100nm。
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