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. 2021 Apr 26;11(1):8907.
doi: 10.1038/s41598-021-88312-6.

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

Basheer Al-Kasmi  1 , M H D Bashir Alsirawan  2 , Anant Paradkar  3 , Abdul-Hakim Nattouf  1 , Hind El-Zein  1
Affiliations

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

Basheer Al-Kasmi et al. Sci Rep. .

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.

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Conflict of interest statement

The authors declare no competing interests.

Figures

Figure 1
Figure 1
Chemical structures of PCT and EuE.
Figure 2
Figure 2
Images of produced PCT-EuE granules.
Figure 3
Figure 3
PXRD patterns of PCT, EuE, physical mixture, T1, TS, and TP trials.
Figure 4
Figure 4
Thermograms of PCT, EUE, Physical mixture (PM), T1, and TS trials and showing peaks onsets and detected Tg steps.
Figure 5
Figure 5
IR spectra of PCT, EuE, 1:1 PM, T1, and TS trials.
Figure 6
Figure 6
IR spectra of PCT, EuE, 1:1 PM, T1, and TP trials.
Figure 7
Figure 7
SEM images of raw PCT and T1 as a reference formula.
Figure 8
Figure 8
SEM images of TS1, TS4, TP1 and TP4 particles. TS1 and TP1 display smooth surface and no presence of PCT crystal is observed. However, PCT crystals can be observed on the surface of TS4 and TP4 particles.
Figure 9
Figure 9
Dissolution profiles showing the %release of PCT from, pure PCT (blue), TS1 trial (red), TS2 (green), TS3 (purple), and TS4 (yellow).
Figure 10
Figure 10
Dissolution profiles showing the %release of PCT from, pure PCT (blue), TP1 trial (red), TP2 (green), TP3 (purple), and TP4 (yellow).
See this image and copyright information in PMC

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