Formation and Physico-Chemical Evaluation of Nifedipine-hydroxypropyl-ß-cyclodextrin and Nifedipine-methyl-ß-cyclodextrin: The Development of Orodispersible Tablets.

ABSTRACT

The novelty in this study is the development of new orodispersible tablets containing nifedipine (NIF) as the active ingredient. Initially, the formation of inclusion complexes between nifedipine and two derivatives of beta-cyclodextrin, namely, hydroxypropyl-ß-cyclodextrin (HP-ß-CD) and methyl-ß-cyclodextrin (Me-ß-CD), was established. Inclusion complexes of nifedipine were prepared by different procedures kneading, coprecipitation and lyophilization methods, using a 11 molar ratio among the drug and cyclodextrin compounds. A physical mixture was also developed for comparison, with the same molar ratio. The physicochemical and structural properties of these obtained complexes were subsequently analysed using Fourier-transform infrared spectroscopy, scanning electron microscopy, differential scanning calorimetry and X-ray diffraction techniques. The lyophilization method of preparation leads to obtaining the complete inclusion of nifedipine in the used cyclodextrin cavity, for both the derivative cyclodextrins. After that, preformulation studies and manufacturing of orodispersible tablets containing NIF-HP-ß-CD and NIF-Me-ß-CD, respectively, inclusion complexes were advanced. The obtained findings show that only F3 (which contains NIF-HP-ß-CD) and F6 (which contains NIF-Me-ß-CD) have a suitable flowability for the direct compression materials.