Enhancing Dissolution Rate and Antibacterial Efficiency of Azithromycin through Drug-Drug Cocrystals with Paracetamol

• Main Authors: Noor Ul Islam, Ezzat Khan, Muhammad Naveed Umar, Attaullah Shah, Muhammad Zahoor, Riaz Ullah, Ahmed Bari
• Format: Article
• Language: English
• Published: MDPI AG 2021-08-01
• Series: Antibiotics
• Subjects: antibacterial agents; azithromycin; cocrystallization; dissolution studies; paracetamol
• Online Access: https://www.mdpi.com/2079-6382/10/8/939

Cocrystallization is a promising approach to alter physicochemical properties of active pharmaceutical ingredients (hereafter abbreviated as APIs) bearing poor profile. Nowadays pharmaceutical industries are focused on preparing drug-drug cocrystals of APIs that are often prescribed in combination therapies by physicians. Physicians normally prescribe antibiotic with an analgesic/antipyretic drug to combat several ailments in a better and more efficient way. In this work, azithromycin (AZT) and paracetamol (PCM) cocrystals were prepared in 1:1 molar ratio using slow solvent evaporation method. The cocrystals were characterized by Fourier transform infrared (FTIR), Raman spectroscopy, powder X-ray diffraction (PXRD), differential scanning calorimeter (DSC), thermo gravimetric analysis (TGA) and high-performance liquid chromatography (HPLC). Vibrational spectroscopy and DSC confirmed that both APIs interact physically and showed chemical compatibility, while PXRD pattern of the starting material and products revealed that cocrystal have in a unique crystalline phase. The degree of hydration was confirmed by TGA analysis and result indicates monohydrate cocrystal formation. The HPLC analysis confirmed equimolar ratio of AZT:PCM in the cocrystal. The in vitro dissolution rate, saturation solubility, and antimicrobial activity were evaluated for AZT dihydrate and the resulting cocrystals. The cocrystals exhibited better dissolution rate, solubility and enhanced biological activities.