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Co-Amorphization of Kanamycin with Amino Acids Improves Aerosolization.
Pharmaceutics ( IF 4.9 ) Pub Date : 2020-07-30 , DOI: 10.3390/pharmaceutics12080715
Bishal Raj Adhikari 1 , Kārlis Bērziņš 2 , Sara J Fraser-Miller 2 , Keith C Gordon 2 , Shyamal C Das 1
Affiliation  

Different formulation techniques have been investigated to prepare highly aerosolizable dry powders to deliver a high dose of antibiotics to the lung for treating local infections. In this study, we investigated the influence of the co-amorphization of a model drug, kanamycin, with selected amino acids (valine, methionine, phenylalanine, and tryptophan) by co-spray drying on its aerosolization. The co-amorphicity was confirmed by thermal technique. The physical stability was monitored using low-frequency Raman spectroscopy coupled with principal component analysis. Except for the kanamycin-valine formulation, all the formulations offered improved fine particle fraction (FPF) with the highest FPF of 84% achieved for the kanamycin-methionine formulation. All the co-amorphous formulations were physically stable for 28 days at low relative humidity (25 °C/<15% RH) and exhibited stable aerosolization. At higher RH (53%), even though methionine transformed into its crystalline counterpart, the kanamycin-methionine formulation offered the best aerosolization stability without any decrease in FPF. While further studies are warranted to reveal the underlying mechanism, this study reports that the co-amorphization of kanamycin with amino acids, especially with methionine, has the potential to be developed as a high dose kanamycin dry powder formulation.

中文翻译:

卡那霉素与氨基酸的共非晶化可改善雾化作用。

已经研究了不同的配制技术来制备高度可雾化的干粉,以将高剂量的抗生素输送到肺部以治疗局部感染。在这项研究中,我们研究了通过共喷雾干燥将模型药物卡那霉素与选定的氨基酸(缬氨酸,蛋氨酸,苯丙氨酸和色氨酸)共非晶化对其雾化的影响。通过热技术确认了共非晶性。使用低频拉曼光谱结合主成分分析监测物理稳定性。除卡那霉素-缬氨酸制剂外,所有制剂均提供了改进的细颗粒级分(FPF),卡那霉素-蛋氨酸制剂的最高FPF为84%。所有共非晶制剂在低相对湿度(25°C / <15%RH)下物理稳定28天,并表现出稳定的雾化作用。在较高的相对湿度(53%)下,即使将蛋氨酸转化为其结晶对应物,卡那霉素-蛋氨酸制剂仍可提供最佳的雾化稳定性,而FPF不会降低。尽管有必要进行进一步的研究以揭示其潜在机制,但该研究报告指出,卡那霉素与氨基酸(尤其是蛋氨酸)的共非晶化有可能发展为高剂量卡那霉素干粉制剂。
更新日期:2020-07-30
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