Formulation and evaluation of taste-masked paracetamol-lipid sachets and chewable tablets

Abstract

The use of lipids as taste-masking excipients in paracetamol sachets and chewable tablets without compromising drug release was investigated. Twelve paracetamol granule formulations were prepared by melt granulation, using Precirol® (glyceryl palmitostearate), cetyl alcohol and stearic acid, at different paracetamol-lipid ratios. Based on efficient taste-masking results coupled with minimum retardation of drug release, paracetamol-Precirol (1:1), paracetamol-cetyl alcohol (1:2) and paracetamol-stearic acid (1:2) granules were selected for preparation of chewable tablets and sachets. Formulations were evaluated for the effect of storage, at 40 °C and 75 % RH for 6 months, on their performance. Results inferred that paracetamol sachets, after reconstitution in 100 ml water, showed efficient taste-masking compared to control sachets (without lipids). The sachets released more than 90 % of their drug content in 30 min, when tested in 900 ml of phosphate buffered saline, pH 5.8. Chewable tablets exhibited comparable taste-masking effect to a reference product, Tylenol® 80 mg chewable tablets, and yielded similar drug dissolution profiles (similarity factor f 2 > 50). Differential scanning calorimetry indicated the absence of interaction between paracetamol and lipids. Scanning electron micrographs supported the obtained results. Upon storage at 40 °C and 75 % RH for 6 months, all the prepared sachets and chewable tablets were found to be stable except cetyl alcohol-based tablets that showed decrease in the efficiency of taste masking with increase in release rate. In conclusion, selected lipids, Precirol®, cetyl alcohol and stearic acid, could be efficiently used in formulation of taste masked paracetamol sachets and chewable tablets without adversely delaying drug release.