Method of evaluation of the bitterness of clarithromycin dry syrup

Chem Pharm Bull (Tokyo). 2002 Feb;50(2):147-52. doi: 10.1248/cpb.50.147.

Abstract

The degree of bitterness of clarithromycin (CAM) dry syrup was evaluated using several methods. Using the inversion method, shaking method, and paddle method, a reasonable correlation between the bitter taste and the amount dissolved was not observed. A mini-column with inner diameter of 0.76 cm and height of 5 cm packed with CAM dry syrup was used for the release test. The release rate of CAM in test solution, which passed through the mini-column, was then measured to evaluate bitterness. The release rate of CAM in the release test using the mini-column correlated well with the results of a sensory test for the bitterness of CAM dry syrup. The dissolution rate constant, defined as the percentage of CAM dissolved from the unit void surface multiplied by the void volume, was inversely proportional to the linear velocity of the test solution. The critical factors affecting evaluation of bitterness were the void volume of the column and linear velocity of the test solution. The optimum linear velocity and void volume were 0.048-0.021 cm/min and 0.27-0.12 cm3, respectively. In addition, the threshold of bitterness of CAM dry syrup was defined as the concentration at which half of the volunteers recognized bitterness in the sensory test. This threshold was found to be 135 microg/ml using the mini-column.

MeSH terms

  • Anti-Bacterial Agents / chemistry*
  • Clarithromycin / chemistry*
  • Hydrogen-Ion Concentration
  • Microscopy, Electron, Scanning
  • Solubility
  • Taste*

Substances

  • Anti-Bacterial Agents
  • Clarithromycin