Abstract

DESIGN, EVALUATION AND CHARACTERIZATION OF SPRAY DRIED CYCLODEXTRIN INCLUSION COMPLEXES OF GLIMEPRIDE

Shashikant Devidas Modekar* and Dr. J. S. Patil

ABSTRACT

Glimepiride (GMP) is a Third Generation Sulphonylureas used for treatment of type 2 diabetes. Its poor aqueous solubility and slow dissolution rate lead to a lack of dose proportionality and high inter and intra subject variability. The rationale of this study was to improve the biological performance of the drug by enhancing its solubility and dissolution through complexion with β-CD and HP-β-CD. In the present study attempt has been made to prepare and characterize inclusion complexes of Glimepiride with β-CD and HP-β-CD. The phase solubility diagram with both the complexion agents was classified as AL-type indicating the formation of 1:1 stoichiometric inclusion complex. Apparent stability constant (KC) was 32.95 M-1 and 42.57 M-1 for β-CD and HP-β-CD complexes respectively. The inclusion complexes were prepared by three different methods viz. Kneading, Microwave irradiation and Spray drying method in comparison with physical mixture. The prepared complexes were characterized using FT-IR, Differential Scanning Calorimeter (DSC), Scanning electron microscopy (SEM), XRD and Particle size analysis. The inclusion complex prepared with HP-β-CD by Microwave irradiation method exhibited greatest enhancement in solubility and fastest dissolution of GMP.

Keywords: Glimepiride, ?-CD, HP-?-CD, Phase solubility, Physical mixture, Kneading, Microwave irradiation, Spray drying, Aqueous solubility, Dissolution rate.