Development of Glimepiride Solid Dispersion using The Coprocessed Excipients of Polyvinylpyrrolidone, Maltodextrin, and Polyethylene Glycol

Abstract

: Objectives: The aim of this work was to produce the solid dispersion of glimepiride (GMP-SD) based on the coprocessed excipient of polyvinylpyrrolidon (PVP), maltodextrin (MD) and polyethylene glycol (PEG). Methods: The PVP-MD-PEG coprocessed excipients were prepared in the ratio of 1:1:1, 1:1:2, 1:2:1, 2:1:1, 2:2:1, 2:1:2, and 1:2:2; as well as characterized. Furthermore, GMP-SD was prepared by spray drying with a ratio of 1:2 for glimepiride and the excipients. The obtained GMP-SD were characterized by fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), X-ray diffraction, and scanning electron microscopy. Dissolution study of GMP-SD was carried out in a phosphate buffer pH 7.4 at ± 37°C for 120 min. Results: The PVP-MD-PEG coprocessed excipients displayed irregular shapes and rough and distributed in a wide range of particle sizes with mostly under 125 μm. The coprocessed excipients exhibited the moisture content of 5-8%, pH of 5-8, and the flow rate of 2.5-4.0 gr/s. The results revealed that there was no chemically interaction between GMP and the coprocessed excipients. Thermal analysis demonstrated that the crystal phase reduction was occurred, thus it was transfomed to amorph form. The dissolution study revealed that GMP-DP proved the dissolution enhancement of GMP compared to the pure GMP. Conclusion: GMP-SD with the PVP-MD-PEG coprocessed excipients has benefit to enhance dissolution rate of glimepiride.Key words: Coprocessed excipient, Glimepiride, Maltodextrin, Polyethylene glycol, Polyvinylpyrrolidone, Solid dispersion.