Aqueous and pH dependent coacervation method for taste masking of paracetamol via amorphous solid dispersion formation

Abstract

AbstractTaste masking of paracetamol was achieved by preparing amorphous solid dispersion (ASD) using modified coacervation method. The method is based on dissolving the drug and polymeric carrier in water adjusted to certain pH level. Then, precipitation of ASD granules is performed by gradually changing pH level. Therefore, the chosen drug and polymer should obtain appropriate acidic or basic groups to enable pH-dependent solvation. Moreover, using solubility enhancing additives such as sodium lauryl sulphate (SLS) and low viscosity polyethylene glycol (PEG 400) found to be essential in aiding drug/polymer aqueous solvation which enhanced amorphization, hence taste masking and drug loading. Solid dispersion between Paracetamol and Eudragit E was formed and that proved by FT-IR, DSC, PXRD and SEM. Also, Paracetamol was released after 2 min in 0.1 N hydrochloric acid medium and the taste of masking forms are accepted from all volunteers. Modified coacervation method does not involve organic solvents, high temperatures, or sophisticated instruments commonly used in taste masking methods. Using PEG 400 resulted in significantly higher drug loading and dissolution rate compared to SLS granules. Moreover, using previously reported scoring system for the evaluation of taste masking methods shows that pH dependent coacervation obtained high scoring over common methods and thus display a robust potential for industrial applications.