Masking of Unpleasant Gustatory Sensation by Cross-Linking of Dehydrated Paracetamol Alginate Pellets Produced by Extrusion-Spheronization

Abstract

Alginate paracetamol pellets were prepared by extrusion-spheronization process. The process variables studied were wet mass mixing time, feed rate, die opening diameter, spheronization residence time, feed rate, disk speed, and drying. The formulation variables studied were granulation fluid composition and level and drug-to-excipient ratios. The dried pellets were cross-linked with calcium chloride solution. The cross-linked pellets were evaluated for dissolution test, friability test, sphericity, flow behavior, particle size distribution, aggregation, water uptake, drug entrapment, and yield. Gustatory sensation test exhibited successful taste-masking of paracetamol by present approach.

In Vitro Dissolution Model Can Predict the in Vivo Taste Masking Performance of Coated Multiparticulates

“…There is currently no standardized pharmacopeial dissolution test for taste-masked dosage forms, and as such there is great variation among the methods employed by researchers working in this area . The methods identified differ in terms of the media employed, with phosphate buffer at pH 6.8 being frequently observed, − while some researchers have simply opted for water. − The pH of the media has also been debated with researchers employing phosphate buffers at varied pH values, from 5.6 to 8.0. − In all instances, the volume of media used was 900 mL, in line with conventional dissolution testing and is thus physiologically irrelevant, particularly given that no increase in dose was observed to account for this volume discrepancy. Better attempts have, however, been observed with Guhmann et al, who used simulated salivary fluid (SSF) at pH 7.4 as the dissolution medium and a volume of 50 mL, which is improved compared to the aforementioned but still lacks relevance to the human oral cavity .…”

Formulation and evaluation of immediate release tablets with different types of paracetamol powders prepared by direct compression

“…These materials provide sufficient flowability and compactability. PAR for D.C. is modified with different binders, but it still shows optimal dissolution rate, which is necessary for development of tablets with immediate release profile (Fachaux et al, 1995;Kulkarni and Amin, 2008;Okoye et al, 2009). Despite the increasing interest in controlled release drug delivery systems, the most desired forms of tablets are those intended to be swallowed whole.…”