Diffusion ordered NMR spectroscopy measurements as screening method of potential reactions of API and excipients in drug formulations

Publication date: Available online 8 September 2018Source: Journal of Pharmaceutical and Biomedical AnalysisAuthor(s): Alexander Becht, Curd Schollmayer, Johannes Wiest, Detlef heller, Wolfgang baumann, Helmut Buschmann, Ulrike HolzgrabeAbstractIn the development of new pharmaceutical formulations it is important to consider the possible interactions between the active pharmaceutical ingredient (API) and excipients which is a well-known problem. The object of the work presented here was to investigate such reactions by means of diffusion ordered NMR spectroscopy (DOSY). The known reaction of 5-aminosalicylic acid (5-ASA) and the excipient citric acid was studied. Three reaction products have been verified by DOSY, 1H-NMR and HPLC measurements. Despite a poor separation in the DOSY diagram the reaction products could be assigned, due to the processing of thoughtful selected parts of the signals. The reaction of 5-ASA with formic acid and benzocaine with dibutyl phthalate was also studied by means of DOSY experiments.
Source: Journal of Pharmaceutical and Biomedical Analysis - Category: Drugs & Pharmacology Source Type: research