Preparation and characterization of isosorbide 5-mononitrate extended-release tablets

Abstract

The objective of this study was to prepare isosorbide 5-mononitrate tablets with an extended-release base using paraffin wax. The goal was to develop a tablet formulation equivalent to the commercially available Imdur® Long Acting Tablet 60 mg. We investigated the effect of paraffin wax on the dissolution rate of isosorbide 5-mononitrate and performed an in vitro dissolution test using the paddle method. The paddle stirring rates were varied from 50 to 150 rpm to mimic pre- and postprandial conditions and determine the effect of food uptake affects on drug absorption. In the dissolution study, isosorbide 5-mononitrate tablets with paraffin wax exhibited extended-release behaviors from 72 to 90 % over an 8-h period, of which the #4 formulation (110-mg paraffin wax) was comparable to the Imdur® Long Acting Tablet 60 mg. From the f 2 factor, the paddle stirring rate did not affect the dissolution both pH 1.2 and 6.8 between the formulation #4 and Imdur® Long Acting Tablet 60 mg for 10 h. The results suggest that the properties of oral extended-release tablet of isosorbide 5-mononitrate containing paraffin wax were comparable to those of the Imdur® Long Acting Tablet 60 mg, and satisfied the guidelines of the Korea Food and Drug Administration.