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Preparation, pharmacokinetic and pharmacodynamic evaluation of carbamazepine inclusion complexes with cyclodextrins

In an attempt to improve the solubility, bioavailability and anti-convulsion activity of carbamazepine (CBZ), inclusion complexes of CBZ were prepared with α-CD, β-CD and di-O-methyl-β-cyclodextrin (DM-β-CD). This report investigates the study of CBZ's phase diagram, preparation of the inclusion complexes and characterization of the physicochemical properties of the complexes. The bioavailability and and-convulsion activity of CBZ were determined in animals following oral administration of the prepared complexes, and compared with the sole drug, as well as physical and ground mixtures with different types of cyclodextrins. The solubility curves of CBZ with α-CD, β-CD and DM-β-CD were typical AL type curves, and apparent stability constants, K c , were calculated from the slope and intercept of the solubility diagrams as 1000, 2400 and 4333 M -1 , respectively. The inclusion complexation, in aqueous solution and in solid phases, was confirmed by the solubility method, X-ray diffractometry, infrared spectroscopy (IR) and differential scanning calorimetry (DSC). The dissolution rate of CBZ in ground mixtures and inclusion complexes was much more rapid than that of CBZ alone or the corresponding physical mixtures. The bioavailability studies indicated faster absorption of CBZ from its complex and ground mixtures with DM-β-CD, compared to α-CD and β-CD, or the corresponding physical mixtures as indicated by the t and the C values. Administration of the CBZ-DM-β-CD complex produced the highest protection percentage for mice from death (66%) by maximum electroshock- induced convulsion (MES). The onset of convulsion was markedly delayed in mice pretreated with the CBZ-DM-β-CD complex. Based on the obtained results, preparation of CBZ complexes with DM-β-CD should markedly improve the solubility, bioavailability and anticonvulsion activity of CBZ.