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Inclusion complexes of cinnarizine with beta-cyclodextrin in aqueous solution and in the solid state.

Inclusion complex formation of cinnarizine with β-cyclodextrin in aqueous solution and in the solid state was confirmed by the solubility method, powder X-ray diffractometry, differential scanning calorimetry (DSC) and proton nuclear magnetic resonance (1H-NMR) spectroscopy. A solid complex of cinnarizine with β-cyclodextrin in 1 : 2 molar ratio was prepared by a coprecipitation method and a neutralization method, and its dissolution behavior in pH 5.0 buffer solution was examined in comparison with those of several other cinnarizine complexes. The dissolution rate of cinnarizine in the inclusion complex was about 30 times larger than that of intact cinnarizine, being almost the same as that of cinnarizing/PVP K-30 complex (weight ratio 1 : 5). Further, a new and efficient procedure was developed to prepare cinnarizine/β-cyclodextrin inclusion complex on a manufacturing scale.