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Tannate complexes of antihistaminic drug: Sustained release and taste masking approaches
Faculty
Pharmacy
Year:
2012
Type of Publication:
Article
Pages:
91-100
Authors:
Zidan, Ahmed S, Khan, Mansoor A, Rahman, Ziyaur, Berendt, Robert T
DOI:
10.1016/j.ijpharm.2011.10.033
Journal:
INTERNATIONAL JOURNAL OF PHARMACEUTICS ELSEVIER SCIENCE BV
Volume:
422
Research Area:
Pharmacology \& Pharmacy
ISSN
ISI:000302398700013
Keywords :
Brompheniramine maleate, Tannic acid, Complex, Solid-state NMR, Electronic tongue, Bitter taste
Abstract:
The aim of this investigation was to evaluate the complexation potential of brompheniramine maleate (BPM) and tannic acid (TA) for sustained release and taste masking effects. The complexes (1:1-1:7 TA to BPM ratio) were prepared by the solvent evaporation method using methanol, phosphate buffer pH 6.8 or 0.1 N HCl as common solvents. The complexes were characterized microscopically by scanning electron microscopy (SEM), chemically by Fourier transform infrared (FTIR) and solid-state NMR (SSNMR), thermally by differential scanning calorimetry (DSC), for crystallinity by powder X-ray powder diffraction (PXRD), for organoleptic evaluation by electronic tongue (e-tongue), and for solubility in 0.1 N HCl and phosphate buffer pH 6.8. The dissolution studies were carried out using the USP II method at 50 rpm in 500 ml of dissolution media (0.1 N HCl or phosphate buffer pH 6.8). SEM images revealed that the morphology of complexes were completely different from the individual components, and all complexes had the same morphological characteristics, irrespective of the solvent used for their preparation, pH or ratio of BPM and TA. The FTIR spectra showed the presence of chemical interactions between the TA and BPM. DSC, PXRD and SSNMR indicated that the drug lost its crystalline nature by formation of the complex. Complexation has significantly reduced the solubility of BPM and sustained the drug release up to 24 h in phosphate buffer pH 6.8 media. The bitter taste of the BPM was completely masked which was indicated by Euclidean distance values which was far from the drug but near to its placebo in the complexes in all ratios studied. The taste masked complexes can be potentially developed as suitable dosage forms for pediatric use. In summary, complexation of BPM and TA effectively sustained the dissolution and masked the bitter taste of drug for the development of suitable dosage forms for pediatric use. Published by Elsevier B.V.
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