Cocrystal Screening of Ibuprofen with Oxalic Acid and Citric Acid via Grinding Method

3rd International Conference on Global Sustainability and Chemical Engineering

工业技术;化学工业

Othman, M.F.^1 ; Anuar, N.^1 ; Ad Rahman, S.^2 ; Ahmad Taifuddin, N.A.^1

Faculty of Chemical Engineering, Universiti Teknologi MARA (UiTM), Malaysia^1

Faculty of Chemical and Natural Resources Engineering, Universiti Malaysia Pahang (UMP), Malaysia^2

关键词: Biological safety;    Co-crystal formation;    Co-crystallizations;    Cocrystallization;    High permeability;    Physicochemical property;    Powder X-ray diffraction (pXRD);    Therapeutic effects;   

Others  :  https://iopscience.iop.org/article/10.1088/1757-899X/358/1/012065/pdf
DOI  :  10.1088/1757-899X/358/1/012065

学科分类：工业工程学

来源: IOP

【 摘 要 】

Ibuprofen is a Class II Biological Safety Class (BSC) drugs used for relief of arthritis, as an analgesic and possesses the effect of antiplatelet. The major problem involves in ibuprofen is it has a low solubility and high permeability thus causes an unsatisfactory therapeutic effect to humans. Thus, in this work, alteration of ibuprofen's physicochemical properties is conducted by means of cocrystallization technique. Co-crystallizations of ibuprofen were prepared with selected coformers using dry grinding and liquid assisted grinding (LAG) techniques in different molar ratios while ethanol and propanol were used as a solvent. The new crystalline forms were identified and characterized by differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and fourier transform infrared spectroscopy (FTIR). Analysis for Ibuprofen-Citric acid (IBP-CA) system, co-crystal was successfully formed in 1:2, 1:3, 2:1 and 3:1 molar ratios for neat grinding method although the co-crystal produced is unstable. Meanwhile, for Ibuprofen-Oxalic acid (IBP-OA) system, the co-crystal formation was identified only in 1:1, 1:2 and 1:3 molar ratios for the neat grinding method. LAG method shows that co-crystal formation was unsuccessful in both solvents for IBP-CA, while IBP-OA co-crystal was formed in the molar ratio 1:1, 2:1 and 3:1 in ethanol, and 2:1 and 3:1 in propanol.