在液体射流通道反应器中激光破碎合成亚微米级活性药物的研究

IF 2.7 4区 材料科学 Q3 CHEMISTRY, PHYSICAL
Tina Friedenauer, Kim Buck, Maike Eberwein, Anna‐Lena Bünte, Christoph Rehbock, Stephan Barcikowski
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引用次数: 0

摘要

开发新药制剂的一个挑战是克服其在相关水介质中的低溶解度。将药物粉末的粒度减小到几百纳米是一种众所周知的方法,由于提高了总表面积,导致溶解度增加。然而,最先进的粉碎技术,如低温碾磨,受到药物降解和污染的影响,特别是当直径为亚微米时,需要较长的处理时间。在这项工作中,皮秒脉冲激光在液体喷射通道反应器中粉碎分散的药物颗粒,作为一种无磨损的粉碎技术,使用疏水口服模型药物萘普生、强的松龙、酮康唑和醋酸甲地孕酮。使用扫描电子显微镜(SEM)表征药物颗粒的粒径和形态,并使用分析离心机量化辐照后粒径分布的变化。通过衰减全反射-傅里叶变换红外光谱(ATR - FTIR)、高效液相色谱(HPLC)和X射线衍射(XRD),研究结果突出了液体喷射通道反应器设置的优越破碎效率,与批处理相比,药物的亚微米颗粒(SMP)的比例高100倍,这提高了溶解度,并且化学降解最小(<1%)。此外,本文还讨论了主要由光机械诱导的有机微粒(MP)激光破碎机制。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Efficient Synthesis of Submicrometer‐Sized Active Pharmaceuticals by Laser Fragmentation in a Liquid‐Jet Passage Reactor with Minimum Degradation
Abstract One challenge in the development of new drug formulations is overcoming their low solubility in relevant aqueous media. Reducing the particle size of drug powders to a few hundred nanometers is a well‐known method that leads to an increase in solubility due to an elevated total surface area. However, state‐of‐the‐art comminution techniques like cryo‐milling suffer from degradation and contamination of the drugs, particularly when sub‐micrometer diameters are aspired that require long processing times. In this work, picosecond‐pulsed laser fragmentation in liquids (LFL) of dispersed drug particles in a liquid‐jet passage reactor is used as a wear‐free comminution technique using the hydrophobic oral model drugs naproxen, prednisolone, ketoconazole, and megestrol acetate. Particle size and morphology of the drug particles are characterized using scanning electron microscopy (SEM) and changes in particle size distributions upon irradiation are quantified using an analytical centrifuge. The findings highlight the superior fragmentation efficiency of the liquid‐jet passage reactor setup, with a 100 times higher fraction of submicrometer particles (SMP) of the drugs compared to the batch control, which enhances solubility and goes along with minimal chemical degradation (<1%), determined by attenuated total reflection‐Fourier transform infrared spectroscopy (ATR‐FTIR), high‐performance liquid chromatography (HPLC), and X‐ray diffraction (XRD). Moreover, the underlying predominantly photo‐mechanically induced laser fragmentation mechanisms of organic microparticles (MP) are discussed.
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来源期刊
Particle & Particle Systems Characterization
Particle & Particle Systems Characterization 工程技术-材料科学:表征与测试
CiteScore
5.50
自引率
0.00%
发文量
114
审稿时长
3.0 months
期刊介绍: Particle & Particle Systems Characterization is an international, peer-reviewed, interdisciplinary journal focusing on all aspects of particle research. The journal joined the Advanced Materials family of journals in 2013. Particle has an impact factor of 4.194 (2018 Journal Impact Factor, Journal Citation Reports (Clarivate Analytics, 2019)). Topics covered include the synthesis, characterization, and application of particles in a variety of systems and devices. Particle covers nanotubes, fullerenes, micelles and alloy clusters, organic and inorganic materials, polymers, quantum dots, 2D materials, proteins, and other molecular biological systems. Particle Systems include those in biomedicine, catalysis, energy-storage materials, environmental science, micro/nano-electromechanical systems, micro/nano-fluidics, molecular electronics, photonics, sensing, and others. Characterization methods include microscopy, spectroscopy, electrochemical, diffraction, magnetic, and scattering techniques.
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