Assessment of Structural Compatibility of Saxagliptin in Physical Mixtures with some excipient by Using HPLC

Abstract

Saxagliptin hydrochloride is an oral hypoglycemic agent used for treatment of type 2 diabetes mellitus. Saxagliptin is unstable because it undergoes an intra-molecular cyclisation reaction to form a cyclicamidine in both solution and solid states. In pharmaceutical development of saxagliptin it’s important to select the excipients which are compatible and help to minimize the formation of cyclicamidine. In excipient compatibility study for saxagliptin it’s essential to identify the formation of cyclicamidine and other related substances. In current work method for quantification of saxagliptin, cyclicamidine and its related substances by high performance liquid chromatographic was developed and validated. This method was used as screening technique for assessing the compatibility of saxagliptin with some pharmaceutical excipients. These were evaluated by analyzing the pure saxagliptin and saxagliptin-excipient in physical mixture, which were stored under different conditions at 40°C/75% relative humidity (RH) for one month. The method was successfully validated as per ICH guidelines. The results of compatibility study demonstrate the suitability of saxagliptin with Methocel, Polyethylene glycol (PEG), Opadry Red, Opadry pink, Opadry white, and Opadry Pink.