Formulation and Evaluation of Taste-Masked Orally Disintegrating Tablets of Nicergoline based on β-cyclodextrin Inclusion Complexation

Amira Hosny Hassan, Ahmed Mahmoud Abdel Haleem Ali, Mohamed Ahmed El-Nabarawy, Ahmed Abd-Elbary

Abstract


Complexation of nicergoline with β-cyclodextrin (β-CD) into an inclusion complex has been used successfully to improve the drug’s solubility, dissolution rate and hence per oral absorption. In addition, masking of the bitter taste was also achieved. The preparation of inclusion complexes was performed using two different techniques, namely; physical mixing and kneading. The apparent stability constant (Kc) of the complex was calculated from the phase solubility analysis. Compatibility of nicergoline and β-CD complex with disintegrants and superdisintegrants were evaluated using powder x-ray diffractometry (PXRD), differential scanning calorimetry (DSC), and fourier transform infrared spectroscopy (FTIR). The morphology of complex particles was studied using scanning electron microscopy. Pharmaceutical characterization confirmed that all additives were compatible with the drug and no signs of physical or chemical interaction were detected. Orodispersible tablets (ODTs) of nicergoline complexed with β-CD and containing 7-9 % camphor had rapid disintegration time (7-12 seconds) and fast drug release profiles (90-100 % in 10 minutes). Therefore, nicergoline ODTs are considered a valuable choice dosage form with improved per oral absorption and taste acceptability.

Keywords


β-cyclodextrin; Inclusion Complex; Nicergoline; Orodispersible; Sublimation

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References


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