Effect of excipients on tablet properties and dissolution behavior of theophylline-tableted microcapsules under different compression forces

Abstract

Theophylline ethylcellulose microcapsules were tableted by compression with or without excipients [lactose or hydroxypropyl cellulose (HPC-H)]. Tablets without excipients had a crushing strength that was independent of the applied compression force and the particle size of the microcapsules used, but tablet thickness decreased with an increase in the particle size of the microcapsules. The dissolution characteristics of theophylline from tableted microcapsules without excipients were almost independent of the applied compression force, but showed a sustained-release behavior. However, the thickness, crushing strength, and dissolution properties of tablets containing excipients were found to be affected by the type of excipient. Tableted microcapsules containing lactose showed an increase in tablet crushing strength that correlated with an increase in the applied compression pressure, but the tablet thickness did not change. In contrast, tableted microcapsules containing HPC-H showed a decrease in tablet thickness with an increase in the applied compression pressure, but the tablet crushing strength was initially reduced and then increased with an increase in the compression force. There was a rapid release rate for theophylline from tableted microcapsules containing lactose; a zero-order release rate for theophylline was found in tableted microcapsules containing HPC-H. The insoluble compacted matrix formation, disintegration of tablet, rupture of microcapsules, and gel matrix formation may be responsible for the release behavior of theophylline-tableted microcapsules with or without excipients. The reduced surface area and porosity resulted in a prolongation of the release from tableted microcapsules compared with untableted microcapsules.