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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.

Journal Title: Drug Metabolism Letters

Price: $95

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