INCLUSION COMPLEXES OF NICARDIPINE - HCl FOR ORAL ADMINISTRATION | ||
Bulletin of Pharmaceutical Sciences Assiut University | ||
Article 13, Volume 28, Issue 1, June 2005, Pages 119-129 PDF (788.1 K) | ||
Document Type: Original Article | ||
DOI: 10.21608/bfsa.2005.65238 | ||
Authors | ||
F. S. Ghazy1; O. A. Sammour* 2; S. A. Ghareeb3; H. A. El-Ghamry2; M. M. Issa4; G. F. Atia4 | ||
1Departments of Pharmaceutics and , Faculty of Pharmacy, Zagazig University, Zagazig, Egypt | ||
2Departments of Pharmaceutics , Faculty of Pharmacy, Zagazig University, Zagazig, Egypt | ||
3Pharmacology, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt | ||
4Departments of Pharmaceutics , Faculty of Pharmacy, Zagazig University, Zagazig, Egypt | ||
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). | ||
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