Abstract :
Donepezil Hydrochloride is a reversible inhibitor of the enzyme acetyl cholinesterase and used as an Alzheimer’s
disease, but due to bitterness it has poor patient compliance. Strong and weak cation-exchange resins were used to
block the functional group responsible for causing bitter taste by forming resinates of drug.
An attempt was made to form drug-resin complexes of different ratios with various cation exchange resins like
Indion-234, Indion-234, and Indion 254. Effect of variables was studied on percentage complexation of drug like
type of process, time of complexation, time of swelling, temperature, activation media, pH, and concentration of
loading solution and mode of complexation. Drug-resin complexes were characterized by DSC and FTIR study.
Resinates of different ratios were subjected to sensory evaluation for taste by ranking method. Release of drug from
each complex was studied at the pH of saliva (6.8) and at the gastric pH (1.2) to determine amount of the drug that
would be released during the administration of formulation. Stability of drug-resin complexes was studied by
carrying out AST at elevated temperatures. Amount of drug released from complex was about 5% at salivary pH and
95% at gastric pH.Drug: Indion-234 (1:3 w/w) complex showed good complexation. Drug-resin complex shows
negligible decomplexation of resinate at salivary pH and maximum at gastric pH.
Keywords: Taste Masking, IER, Drug-Resin Complex, SSF, SGF.
Keyword :
Taste Masking, IER, Drug-Resin Complex, SSF, SGF.