INCLUSION COMPLEXES OF NICARDIPINE - HCl FOR ORAL ADMINISTRATION

Ghazy, F. S.; Sammour, O. A.; Ghareeb, S. A.; El-Ghamry, H. A.; Issa, M. M.; Atia, G. F.

doi:10.21608/bfsa.2005.65238

INCLUSION COMPLEXES OF NICARDIPINE - HCl FOR ORAL ADMINISTRATION

Document Type : Original Article

Authors

¹ Departments of Pharmaceutics and , Faculty of Pharmacy, Zagazig University, Zagazig, Egypt

² Departments of Pharmaceutics , Faculty of Pharmacy, Zagazig University, Zagazig, Egypt

³ Pharmacology, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt

10.21608/bfsa.2005.65238

Abstract

Inclusion complexes of nicardipine HCl (NIC) with β-cyclodextrin (β-CD) and hydroxypropyl-β-cyclodextrin (HP-β-CD) were prepared using different methods: coevaporation, kneading and co-precipitation. Inclusion complexation in aqueous solution and in solid state was studied by the solubility method, Fourier transform-infrared spectroscopy (FTIR), Differential scanning calorimetry (DSC) and X-ray diffractometry (XRD). The solubility of (NIC) increased as a function of cyclodextrin concentration, showing Bs and AL type diagrams for (β-CD) and (HP-β-CD), respectively. The dissolution rate of (NIC) / cyclodextrin complexes were investigated and compared with those of the physical mixtures and pure drug. The dissolution efficiency of (NIC) increased by complexation with cyclodextrins to 2.8-2.9 fold than (NIC) alone. Oral bioavailability in rabbits increased to ~ 6 fold by complexation with (β-CD).