Yasir Karkar
University of Al-Ayen, Iraq
Title: Crystal engineering of a proton pump inhibiting agent to positively modify their physico chemical properties by cocrystal formation
Biography
Biography: Yasir Karkar
Abstract
Cocrystals are multicomponent supramolecular solid forms in which the components are present in stoichiometric ratio. The components that are solid at ambient condition are held together by hydrogen bonds rather than ionic bond which set them apart from salts. Although the first cocrystal dates back to 1844, cocrystallization is only regained interest in the last decade because of their ability to fine-tune the solubility, dissolution rate and other physicochemical properties without altering the chemical structure of the molecule. The aim of this study was to utilize the principles of crystal engineering to improve the physiochemical properties of proton pump inhibitors. Omeprazole was chosen as the subject of this study because it is the first synthesized molecule among proton pump inhibitors and it is to date a blockbuster drug. Before screening attempts, molecular modelling was used to predict cocrystallization possibility and we were able to shortlist the coformers from 9 to 5 potential coformers. Thereafter, we were able to cocrystallize omeprazole with caffeine using liquid assisted grinding in a ball mill. This cocrystal was investigated using thermal analysis, PXRD and FT-IR because single crystal suitable for single crystal X-ray diffraction structure study could not be obtained. Further characterization of this cocrystal indicate it has advantage over omeprazole in terms of solubility, dissolution rate, hygroscopicity and photostability, but offer no advantage in acid stability in solution, however, further testing of the stability with acidic coat need to be carried out