テオフィリン徐放性ドライシロップ剤の先発品と後発品の品質比較評価に関する研究

Abstract

To evaluate the quality of the original theophylline sustained-release dry-syrup product and 4 generic versions on the market, we conducted a content uniformity test, dissolution test, bioavailability test, and bitter taste test on these products. Serum theophylline concentrations of the original product were investigated in 3 rats according to a test that was divided into 2 different particle sizes with the following results. For the whole preparations, the mean content was about 20% and changing the pH did affect the dissolution rate for any preparation. However, when the preparations were divided into 2 different particle size ranges, there was a large variation in content for the different particle size categories for all preparations. For preparation A, particles of less than 75μm in particle size had the highest content, for preparation B particles from 150 to 300μm had the highest content, preparation C had the highest content in the 75-150μm particle size range and the highest content for preparations D and E was in particles of over 300μm in size. For preparation A, the ratio of the content of particles of less than 75μm in size to that of particles of 150 to 300μm was about 1.7 and the ratio of the area under the concentration time curve for these 2 particle size ranges was about 2.1. In the taste test, all preparations were found to be masked sufficiently against bitterness just after administration, but 2 preparations were not sufficiently masked at 15 seconds after administration. These results suggest that some of the generic products are superior in quality to the original one and some are inferior.