Abstract
Taste 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.
Highlights
Taste masking of paracetamol was achieved by preparing amorphous solid dispersion (ASD) using modified coacervation method
The approach depends on the solubility dependent of the polymeric carrier, the Eudragit E
The drugs to be used must display a proper solubility at certain pH level such as paracetamol
Summary
Taste masking of paracetamol was achieved by preparing amorphous solid dispersion (ASD) using modified coacervation method. There are abundant reported techniques for the preparation of amorphous solid dispersions (ASD) These methods aim to obtain a drug—polymer mixture at the molecular level and include complexation, encapsulation and melt extrusion methods. Each one of these techniques has one or more disadvantages such as using costly and sophisticated instruments, complex or multistep processing, using high temperatures which causes drug degradation issues, and the use of large amounts of organic solvents causing toxicological and environmental issues[8]. The method includes using pH-dependent soluble drug and polymer which can be dissolved in water at selected pH level, solid dispersion is obtained by gradually changing pH where the materials are no longer soluble
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