Application of statistical design on the early development of sustained-release tablet containing ivy leaf extract

摘要

The aim of this study was to develop a sustained-release (SR) tablet of ivy leaf extract (ILE) that exhibits robust dissolution profiles unaffected by pH and mechanical stress in the gastrointestinal (GI) tract using statistical design. The response surface design was used to study the effect of type and amount of sustaining polymer on the drug release over time. The type and amount of sustaining polymers were set as factors. The percentages of dissolved hederacoside C, as an indicator substance of ILE, at 6, 12, and 24 h were set as the responses. The highest desirability value was obtained when 26.09% of HPMC K15 M (hydroxypropyl methylcellulose, 15,000 mPa s) was used among the various polymers tested. The granules and tablets prepared with this composition showed acceptable physical properties (bulk density, tapped density, angle of repose, thickness, hardness, and friability). The drug release profiles of the SR tablet exhibited non-Fickian mechanism close to zero-order release based on the Korsmeyer-Peppas model regardless of the pH of dissolution media and the paddle speed of the dissolution tester. Overall, the present study suggested a new statistical approach to the development of SR tablets containing herbal medicine and successfully developed the tablets.