PREPERATION AND CHARACTERIZATION OF Β-Cyclodextrin INCLUSION COMPLEXES ORAL TABLETS CONTAINING POORLY WATER SOLUBLE GLIMIPIRIDE USING FREEZE DRYING METHOD

Abstract

Glimepiride is an oral antidiabetic drugs which is practically insoluble in water. The formation of β-cyclodextrin inclusion complex was able to increase the solubility of glimepiride. This study aim to prepare, characterize and formulation of inclusion complex tablets in order to meet the requirement in Pharmacopeia. The inclusion complex were prepared in a molar ratio of 1:1 and 1:2 by freeze drying method, after that characterized include FTIR spectroscopy and scanning electro microscope (SEM). Further, it was formulated into tablets by direct compression technique using primogel and crospovidone as super disintegrants. The tablets were evaluated include weight uniformity, hardness, friability, disintegration, and dissolution. The dissolution studies of inclusion complex were performed by using USP II apparatus. The result of FTIR and SEM provided evidence of the formation of complexes after utilizing freeze-drying methods. The tablet evaluation containing inclusion complex glimepiride-β cyclodextrin with primogel and cropovidone as disintegrant showed that increased concentration of disintegrant will increase disintegration time of the tablets. All of formulas meet the requirements in the Pharmacopoeia. The inclusion complex of glimepiride-β cyclodextrin successfully used for enhancing the solubility of glimepiride and the tablets meet the requirement in Pharmacopeia.

Characterization, formulation and evaluation of glibenclamide with β-cyclodextrin inclusion complexes tablets

“…4 Recent publications reported that cyclodextrins improved solubility and dissolution of itraconazole, curcumin, repaglanid, mirisetin, and glimepiride. [5][6][7][8][9] Spray drying method is one method that has been widely used to evaporate solvent for the formation of complex inclusion of poorly water-soluble drugs with β-cyclodextrin. The results of aripiprazole-β-cyclodextrin inclusion complex prepared by spray drying technique showed that this techniques could increase solubility and dissolution rate of aripiprazole.…”

Design of Cyclodextrin-Based Functional Systems for Biomedical Applications

“…Among them, CDs and their derivatives show the ability to increase the solubility, stability, dissolution rate, and bioavailability of poorly soluble drugs through the formation of inclusion complexes and thereby are widely used for pharmaceutical applications. In addition, the advantages of CDs as a carrier also include (1) chemical derivatization by site-specific substitution; (2) the tunable cavity sizes; and (3) low toxicity and immunogenicity ( Kurkov and Loftsson, 2013 ; Syukri et al, 2015 ). The drug molecules can be partially or entirely inserted into the hydrophobic CD cavity under the driving forces of hydrophobic, electrostatic, van der Waals, charge-transfer interactions, etc.…”

Physicochemical Characterization, Molecular Docking, and In Vitro Dissolution of Glimepiride–Captisol Inclusion Complexes

“…The images of the samples were taken at an excitation voltage of 10 kV. 39 Fourier Transform Infrared Spectroscopy. The analysis was performed on a Fourier transform infrared spectrophotometer (Bruker) to determine functional groups of glimepiride, Captisol, physical mixture, and inclusion complexes.…”