Evaluation of the compression properties of co-processed paracetamol, gelatin and microcrystalline cellulose formulation prepared via melt-in agglomeration

Co-processing techniques have been used to modify the properties of dosage forms. The aim of this study is to evaluate the granules and tablet properties of co-processed paracetamol, gelatin and microcrystalline cellulose. Batches of co-processed paracetamol granules (A-E) were prepared by melt-in agglomeration process using paracetamol with varying amounts of gelatin (۱.۰, ۲.۰, ۳.۰ or ۴.۰ % w/w) or starch (۳.۰ % w/w) and microcrystalline cellulose. A control batch (F) of conventional granules was also prepared by wet granulation method with starch mucilage (۴.۰ % w/w). The granules were subjected to micromeritic, compaction and differential scanning calorimetric analyses. The granules were compressed into tablets and their tablet properties evaluated. Granules of batches A-D had higher percent maximum volume reduction of ۱۲.۲۵-۱۶.۱۳ % compared to the percent maximum volume-reduction (۹.۵۲ and ۱۱.۸۱) of granules from batches E and F respectively. Differential scanning result indicates amorphous solidification of co-processed paracetamol. Tablets formulated from batches A-D showed improve tensile strength (۳.۶۳ - ۸.۲۶ Nm-۲) and faster disintegration time (۱.۳۲- ۱.۱۲ min) compared to the tensile strengths (۵.۰۹ & ۵.۰۱ Nm-۲) and disintegration times (۲.۵۴ & ۴.۴۳ min) of tablets from batches E and F respectively. There were no significant difference (P≥۰.۰۵) in their maximum amounts ( >۷۰ %) of drug released after ۴۰ min. Melt-in agglomeration of paracetamol and gelatin with microcrystalline cellulose created amorphous dispersion that improved tabletability parameters of granules and disintegration time and dissolution properties of tablets.

Keywords:

Co-processed , compaction , maximum volume-reduction , amorphous solidification , tabletability