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THE PHARMA REVIEW (OCTOBER 2008)

Molecular Properties and Taste Masking of Indion
234-Mefloquine Resinates

Shridhar J Pandya, Nitin Kadam, Shital J Bidkar, Nilam H Patil, Amit Patel

Abstract: The bitter taste of drugs is an impediment in ensuring patient compliance. The purpose of this research was to formulate tasteless complexes of Mefloquine; an anti malarial drug with ion exchange resins. Optimization of complexation process and evaluation of complexes was also intended. The drug loading process was carried out using different resins and was optimized using different drug: resin ratio and pH. Resinates were characterized by infrared spectroscopy, thermal analysis and XRPD & SEM. Taste evaluation was done using semi quantitative method. Indion 234 gave best loading efficiency at drug resin ratio of 1:1.5. Drug loading was not influenced by pH. XRPD and DSC studies revealed that drug is in amorphous state in complex. The IR studies revealed complexation of secondary amine group of drug with carboxylic functional group of resin. Taste evaluation by using semiquantitative method found resinates as tasteless and agreeable. The drug release from resinates in simulated gastric fluid was complete in 30 min. Ion exchange resinates offer an effective tool for masking of bitterness and improve drug release.

Introduction
Ion exchange resins are solid and suitably insolublilized high molecular weight polyelectrolytes that can exchange their mobile ions of equal charge with the surrounding medium reversibly and stochiometrically. The reaction is an equilibrium reaction. The ion exchange resins are available in different size, cross linkage and functionality making them suitable for different applications. Bitter cationic drugs can get adsorbed on to weak cationic exchange resin of carboxylic acid functionally to form the complex, which is non-bitter. The taste masking applications of ion exchange resins are reported for various cationic drugs eg. Ciprofloxacin, chloroquin phosphate. The ionic binding of the drugs to polymeric materials such as carbopol is emerging as an important mechanism of taste masking. In present study Indion resins were used to mask the taste of bitter drug Mefloquine. Taste masking ability of optimized complex, molecular properties and physical characteristics were evaluated.

 

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