Preparation of a Sustained-Release Matrix Tablet of Acetaminophen with Pulverized Low-Substituted Hydroxypropylcellulose via Dry Granulation

Abstract

Pulverized L-HPC (low-substituted hydroxypropylcellulose, LH41) can be used as a sustained-release matrix filler. In previous papers, we had reported that the flowability and packability of LH41 powder with or without acetaminophen was improved by wet granulation for practical uses. In the present report, dry granulation via slugging was employed to avoid the use of an organic solvent (e.g. ethanol). The sustained-releasing functions of the original LH41 were maintained during granulation with lower slugging pressures (≦10 MPa), whereas they were lost with higher slugging pressures (≧ 20 MPa). The sustained-releasing function of the tablet prepared with the granules of LH41 and the drug (acetaminophen) was determined by a function of internal pore size distribution and the swelling property of the tablet. The granules of LH41 and the drug prepared by a roller compactor were applied practically to prepare a controlled-release matrix tablet using a single-punch tabletting machine. It was possible to widely control the drug release of the resultant tablets (i.e. rapid- to sustained-release) by changing the roller compaction pressure. © 1993, The Pharmaceutical Society of Japan. All rights reserved.