The effect of ultrasound on the crystallization-precipitation process of transforming sodium amoxicillin into amoxicillin trihydrate.

IF 9.7 1区 化学 Q1 ACOUSTICS
Aicha Ladaidi, Loïc Hallez, Isabelle Pochard, Nicolas Rouge, Jean-Yves Hihn
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Abstract

Crystallization is a process used in many industrial fields. However, in the pharmaceutical industry it plays a crucial role as the quality of the drug (finished product) in terms of therapeutic efficacy and stability is strongly related to the physical properties of the active ingredient, as well as other excipients determined and controlled through this process. This paper deals with the feasibility of the transformation of amoxicillin sodium salt into amoxicillin trihydrate. It will also be the opportunity of studying the physical properties of the crystals obtained (size and size distribution, shape, purity, morphology) as a result from the interaction of the crystallization-precipitation process with or without ultrasound and the selected antibiotic amoxicillin. The limiting factor for sonocrystallization is pH, the optimum pH being 4.5. Indeed, for a pH below 2, the crystallization yield does not exceed 10 %. Ultrasound has a synergistic effect on crystallization by improving the yield and the fineness of the powder, as well as on the kinetics of the reaction in relation to the nucleation time, even if it is not necessarily possible to attribute this phenomenon to solubility or de-supersaturation. For 30 min experiments, the best yield of 95 % was obtained using a low frequency (20 kHz), compared to the yield obtained without ultrasound (69 %) or with higher frequencies (581 kHz - 72 % and 864 kHz - 65 %). In addition to the ultrasound frequency used, temperature, pH and sonication time also have a profound effect on the product's crystal morphology and size. In the case of low frequency, particle size ranged from 0.4 to 60 μm, and from 0.7 to 250 μm under silent conditions.

超声对阿莫西林钠转化为三水合阿莫西林结晶沉淀过程的影响。
结晶是一种应用于许多工业领域的工艺。然而,在制药工业中,它起着至关重要的作用,因为药物(成品)的质量在治疗效果和稳定性方面与活性成分的物理性质以及通过该过程确定和控制的其他赋形剂密切相关。探讨了阿莫西林钠盐转化为三水合阿莫西林的可行性。这也将是研究晶体的物理性质(大小和大小分布,形状,纯度,形态)的机会,这是结晶沉淀过程与超声或不超声和所选抗生素阿莫西林相互作用的结果。超声结晶的限制因素是pH,最佳pH值为4.5。事实上,当pH值低于2时,结晶率不超过10%。超声波通过提高粉末的产率和细度,以及与成核时间有关的反应动力学,对结晶具有协同作用,即使不一定可以将这种现象归因于溶解度或去过饱和。在30分钟的实验中,与不使用超声波(69%)或更高频率(581 kHz - 72%和864 kHz - 65%)的产率相比,使用低频(20 kHz)获得的产率最高为95%。除了使用的超声频率外,温度、pH值和超声时间对产品的晶体形态和尺寸也有深远的影响。在低频条件下,颗粒尺寸范围为0.4 ~ 60 μm,在静音条件下为0.7 ~ 250 μm。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
Ultrasonics Sonochemistry
Ultrasonics Sonochemistry 化学-化学综合
CiteScore
15.80
自引率
11.90%
发文量
361
审稿时长
59 days
期刊介绍: Ultrasonics Sonochemistry stands as a premier international journal dedicated to the publication of high-quality research articles primarily focusing on chemical reactions and reactors induced by ultrasonic waves, known as sonochemistry. Beyond chemical reactions, the journal also welcomes contributions related to cavitation-induced events and processing, including sonoluminescence, and the transformation of materials on chemical, physical, and biological levels. Since its inception in 1994, Ultrasonics Sonochemistry has consistently maintained a top ranking in the "Acoustics" category, reflecting its esteemed reputation in the field. The journal publishes exceptional papers covering various areas of ultrasonics and sonochemistry. Its contributions are highly regarded by both academia and industry stakeholders, demonstrating its relevance and impact in advancing research and innovation.
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