Aryl semicarbazones can be considered a novel class of compounds presenting anticonvulsant activity. In order to improve the efficiency and bioavailability of benzaldehyde semicarbazone (BS) we used the host–guest strategy and -cyclodextrin (-CD) to prepare a BS/-CD 1:1 inclusion compound, which was characterized by thermal analyses (TG, DTG, DSC), XRD powder pattern diffraction analyses, infrared data and 1H, 13C, 2D-ROESY NMR and 1H relaxation times. The BS/-CD inclusion compound was tested in rats using the maximum electroshock (MES) screen. The minimum dose necessary to produce anticonvulsant activity decreased from 100 mg/Kg (ip or vo) for the free semicarbazone to 25 mg/Kg/vo (75%) and 15 mg/Kg/ip (85%), indicating that the host–guest strategy that uses -CD and BS is very effective and could be successfully employed in the preparation of pharmaceutical formulationof anticonvulsants.