用等温研究预测抗糖尿病阿格列汀的稳定性

IF 0.5 4区 化学 Q4 CHEMISTRY, MULTIDISCIPLINARY
C. Bertol, Gabriel Felimberti, Karini da Rosa, E. Rizzon, R. Pereira, L. Kreutz, Pedro Froelich
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引用次数: 0

摘要

阿格列汀(ALG)苯甲酸酯是一种口服降糖药物,作为DPP-4抑制剂防止肠促胰岛素降解。强制稳定性研究使用高温来分解药物并估计它们在低温下的行为。采用等温热重法(TGA)和液相色谱法(LC-PDA)对ALG的热稳定性进行了评价。在等温热重分析中,ALG分别在150、155、160、165和170°C下进行了高达10%的质量损失。在烘箱中,将药物置于130、140、150、155、160和170°C。采用Arrhenius模型计算动力学参数。ALG遵循零级动力学,其中降解速率不依赖于试剂浓度。活化能范围为31.0 ~ 35.9 kcal mol-1。在细胞毒性试验中,降解药物在CRIB细胞中的毒性低于未降解药物。TGA法比烤炉法和LC-PDA法更快、更实用,且数据具有相关性。在这里,我们描述了ALG降解的动力学参数,提高了对药物的认识,并协助从药物开发新的配方。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
PREDICTION OF ANTI-DIABETIC ALOGLIPTIN STABILITY BY ISOTHERMAL STUDIES
Alogliptin (ALG) benzoate is an oral hypoglycemic drug that works as a DPP-4 inhibitor to prevent incretin degradation. Forced stability studies use high temperatures to decompose drugs and estimate their behavior at low temperatures. We aimed to evaluate the thermal stability of ALG using two techniques: isothermal thermogravimetry (TGA) and degradation in an oven followed by liquid chromatography (LC-PDA) analysis. ALG was subjected to 150, 155, 160, 165, and 170 °C up to 10% of mass loss in isothermal TGA. In the oven, the drug was submitted to 130, 140, 150, 155, 160, and 170 °C. Kinetic parameters were calculated with the Arrhenius model. ALG followed zero-order kinetics, in which the degradation rate did not depend on reagent concentration. Activation energy ranged from 31.0 to 35.9 kcal mol-1. The degraded drug was less toxic in a cytotoxicity assay in CRIB cells than the undegraded drug. The TGA method is faster and more practical than the oven followed by LC-PDA, and the data present a correlation. Here we described the kinetic parameters of ALG degradation, improving the knowledge about the drug and assisting in developing new formulations from the drug.
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来源期刊
Quimica Nova
Quimica Nova 化学-化学综合
CiteScore
1.60
自引率
12.50%
发文量
72
审稿时长
2-4 weeks
期刊介绍: Química Nova publishes in portuguese, spanish and english, original research articles, revisions, technical notes and articles about education in chemistry. All the manuscripts submitted to QN are evaluated by, at least, two reviewers (from Brazil and abroad) of recognized expertise in the field of chemistry involved in the manuscript. The Editorial Council can be eventually asked to review manuscripts. Editors are responsible for the final edition of QN.
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