利格列汀与阿奇霉素的体内外相互作用分析。

Md Didaruzzaman Sohel, Faisal Asif, Tonmoy Kumar Mondal, Md Helal Uddin Sumon, Md Hassan Kawsar
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引用次数: 0

摘要

背景:利格列汀是一种二肽基肽酶-4 (DPP-4)抑制剂。阿奇霉素被指定为一种与第50核糖体亚基的23s rRNA结合,阻碍微生物蛋白合成的抗生素。我们的研究重点是这些药物的药物相互作用。目的:了解利格列汀与阿奇霉素通过络合的强度和性质介导的相互作用的生物利用度和理化途径。方法:采用紫外/可见光谱(UV/VIS)、超高效液相色谱(UPLC)、傅里叶变换红外光谱(FT-IR)和差示扫描量热法(DSC)进行体外相互作用评价,采用口服葡萄糖耐量试验(OGTT)对小鼠模型进行体内相互作用评价。结果:根据Job’s和Ardon’s方程,在特定温度下,不同pH值下的相互作用有轻微变化。在UPLC中,药物混合评价显示利格列汀在50 mg/l时的面积为2013793,阿奇霉素的面积为54631。利格列汀的高度为579234,阿奇霉素的高度为11442。阿奇霉素的波长分别为731.02 cm-1、993.34 cm-1、1379.10 cm-1和1718.58 cm-1。利格列汀的1363.67 cm-1、1473.62 cm-1和1718.58 cm-1的波长也减少。DSC显示,药物混合物的熔化恒温温度为125.55℃,熔化归一化能为-3.0 W/mg,熔化归一化能为-5.5 W/mg的温度为225.75℃。在OGTT试验中,利格列汀的血糖水平分别降低了13.58%和57.25%。结论:利格列汀与阿奇霉素合用可能会降低药物复合物的疗效。
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Analysis between Linagliptin and Azithromycin: In vitro and In vivo Interaction Study.
BACKGROUND Linagliptin is prescribed as a dipeptidyl peptidase-4 (DPP-4) inhibitor. Azithromycin is specified as an antibiotic that binds with 23s rRNA of the 50s ribosomal subunit obstructing the microbial protein synthesis. Our study focuses on the drug-drug interactions of these drugs. OBJECTIVE The purpose of the study is to understand the bioavailability and physicochemical approaches of Linagliptin and Azithromycin interaction mediated through the strength and nature of the complexation. METHODS The assessment drug interaction applying Ultraviolet-visible spectroscopy (UV/VIS), Ultra-Performance Liquid Chromatography (UPLC), Fourier transform infrared spectroscopy (FT-IR), and Differential scanning calorimetry (DSC) for In Vitro assessment. Also, Oral Glucose Tolerance Test (OGTT) in a mice model for In Vivo. RESULTS The mild variation observed at different pH at a specific temperature on Job's and Ardon's equation. On UPLC, the drug mixture is 2013793 and 54631 on 50 mg/l. The height of the drug mixture 579234 and 11442, respectively. The Azithromycin, the wavelength of 731.02 cm-1, 993.34 cm-1, 1379.10 cm-1, and 1718.58 cm-1 diminish from the mixture. Also, from Linagliptin, the wavelength of 1363.67 cm-1, 1473.62 cm-1, 1718.58 cm-1 declines from the drug mixture. The melting endotherm at 125.55°C of melting normalized energy of -3.0 W/mg and 225.75°C with melting normalized energy of -5.5 W/mg of the drug mixture on DSC. In the OGTT test, the blood glucose level decrease Linagliptin and the drug mixture at (13.58 %) and (57.25%). CONCLUSION Hence, the concomitant administration of Linagliptin and Azithromycin at a time might reduce the therapeutic effect of the formation of complexation.
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来源期刊
Drug metabolism letters
Drug metabolism letters Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
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期刊介绍: Drug Metabolism Letters publishes letters and research articles on major advances in all areas of drug metabolism and disposition. The emphasis is on publishing quality papers very rapidly by taking full advantage of the Internet technology both for the submission and review of manuscripts. The journal covers the following areas: In vitro systems including CYP-450; enzyme induction and inhibition; drug-drug interactions and enzyme kinetics; pharmacokinetics, toxicokinetics, species scaling and extrapolations; P-glycoprotein and transport carriers; target organ toxicity and interindividual variability; drug metabolism and disposition studies; extrahepatic metabolism; phase I and phase II metabolism; recent developments for the identification of drug metabolites.
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