Optimization and Evaluation of Orodispersible Solid Dispersion Tablet of Ketotifen Fumarate

Abstract

The present study was aimed to integrate the developed and optimized ketotifen fumarate dispersion into Orodispersible tablets formulations, to enhance the dissolution rate and bioavailability aspects of the drug. Ketotifen fumarate solid dispersion was prepared using different concentrations of poloxamer 407via solvent evaporation and fusion method. Solubility study, x-ray diffraction (XRD), scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FTIR) and other investigations were done. Ten formulations of the optimum dispersed ketotifen fumarate Orodispersible tablets were prepared with various superdisintegrants, the results of in vitro - in vivo tests revealed that, the dispersion of the drug in the polymer considerably enhanced the solubility, the batch (Fsd 3) prepared by fusion method showed increased the solubility as ~2-fold compared with a pure drug. FTIR spectra, SEM and XRD data, showed amorphrization of ketotifen fumarate, which explains the better dissolution rate of the drug from its solid dispersions. Formulation F1 containing 15%w/w of crospovidone was showed in vitro- in vivo disintegration time (17 sec., 15 sec. respectively) and percent of drug dissolved in 2 min. was 90.04%, proved to be the optimum formulation, which is required for obtaining rapidly disintegrating tablets. The solubility of the drug had increased, and the resultant orodispersible tablets can be considered as a promising dosage form to achieve better patient compliance.

Natural polymer Effect on gelation and rheology of ketotifen-loaded pH-sensitive in situ ocular gel (Carbapol) ‎

“…Polyelectrolyte is a polymer containing either alkaline or acidic functional group which release or accept the protons in responsive to pH environmental changes so that when the change of pH occurred leading to gelling of the polymer solution [4]. Ketotifen fumarate belongs to the histamine H1 receptor antagonists, Ketotifen fumarate is used in the treatment of allergic conditions like conjunctivitis, rhinitis, and the prophylactic management of asthma [5]. It is found in white or light yellowish-white crystallize powders and it was sparingly soluble in acetic acid and methanol, slightly soluble in ethanol, water, and acetic anhydride with pKa: 8.75 and Log P 4.99 [6,7].…”