Evaluation of Pharmaceutical Compatibility between Acarbose and Common Excipients Used in the Development of Controlled Release Formulations

Background: Excipients are used in the formulation of pharmaceutical dosage forms, but may interact with active pharmaceutical ingredients (APIs). Some of these interactions could alter the physicochemical properties of the APIs which can affect the therapeutic efficacy and safety. Acarbose is an anti-diabetic drug used in this study as an API to investigate its compatibility with common excipients in order to development of pharmaceutical controlled release formulations. Methods: For this purpose, 15 different excipients were selected. Binary mixtures of drug with each of the excipients (1:1 mass ratio) were prepared. Mixtures were analyzed immediately after mixing and also after incubation at stress conditions (adding 20% water and incubated at 40 degrees C for 2 months). The thermal analytical investigation like differential scanning calorimetry (DSC), Fourier transform infra-red spectroscopy (FTIR) and high-performance liquid chromatography (HPLC) were employed for physicochemical evaluations of the possible incompatibility. Photodiode-array (PDA) and mass studies were performed to ensure the peak purity of the HPLC peaks of API in stressed samples. Results: Incompatible excipients with acarbose were determined as EC (ethyl cellulose), Carbopol 934, Hydroxypropyl cellulose, PEG2000 (Polyethylene Glycol 2000), Mg Stearate, Na Alginate and Poloxamer. Conclusion: Results of this study would be used for the development of controlled release formulation of acarbose. It is recommended to avoid the use of incompatible excipients.