Author/Authors :
Jelvehgari, Mitra Drug Applied Research Center - Tabriz University of Medical Sciences , Barghi, Leila Faculty of Pharmacy - Tabriz University of Medical Sciences , Barghi, Farhad Student Research committee - Tabriz University of Medical Sciences
Abstract :
Background: Chlorpheniramine maleate (CM) is widely used as an antihistaminic drug but it is very bitter and as yet no mouth dissolving/
disintegrating taste-masked preparation that might be useful for pediatric and geriatric patients is available in the market. Objectives: The purpose of this research was to mask the bitter taste of CM by formulating microspheres of the taste-masked drug. Materials and Methods: This work was done to develop alginate/chitosan particles prepared by ionic gelation (Ca2+ and Al3+) for
the CM release. The effect of different chitosan and Ca2+ concentrations on taste masking and the characteristics of the microspheres
were investigated. Ca2+ and Al3+ alginates microspheres of CM were prepared using cross-linked insoluble complexes that precipitate,
incorporating the drug. Formulations were characterized for particle size and shape, entrapment efficiency, fourier transform
spectroscopy (FTIR), x-ray diffraction (XRD), and differential scanning calorimetry (DSC), bitter taste threshold and in vitro drug release in
simulated gastrointestinal fluids. Results: FTIR, XRD and DSC demonstrated unstable characters of CM in the drug-loaded microspheres and revealed an amorphous form.
Also, the peak of alginate microparticles (Ca2+ and Al3+ ions) in all formulations remained the same, with low intensity of spectrum.
The results of DSC, X-ray diffraction and FTIR showed the presence of several CM chemical interactions with alginate and ions (Ca2+ and
Al3+). The microsphere formulations showed desirable drug entrapment efficiencies (62.2-94.2%). Calcium/aluminum alginate retarded
the release of CM at low pH = 1.2 and released the drug from microspheres slowly at pH = 6.8, simulating intestine pH. The drug release
duration and the release kinetics were dependent on the nature of the polymers, the cation concentrations, and valences (Ca2+ and Al3+).
The drug release rate was decreased by an increase in chitosan and cation concentrations. Conclusions: The results of the present study indicated that oral preparation of CM with an acceptable taste is feasible.
Keywords :
Chlorpheniramine , Calcium , Aluminium , Taste