The bioavailability of isoniazid, rifampin, and pyrazinamide in two commercially available combined formulations designed for use in the short-course treatment of tuberculosis

Am Rev Respir Dis. 1986 Jun;133(6):1076-80. doi: 10.1164/arrd.1986.133.6.1076.


The bioavailability of isoniazid, rifampin, and pyrazinamide in 2 combined formulations of the 3 drugs (Rifater) for use primarily in the short-course chemotherapy of tuberculosis has been studied in Chinese patients in Singapore and Hong Kong. One formulation, containing 50 mg isoniazid, 120 mg rifampin, and 300 mg pyrazinamide per tablet is suitable for daily use, whereas the other, containing higher proportions of isoniazid and pyrazinamide, is designed for intermittent treatment, each tablet containing 125 mg isoniazid, 100 mg rifampin, and 375 mg pyrazinamide. Appropriate dosages for the Chinese patients, whose average weight was approximately 50 kg, were 5 and 6 tablets, respectively. Plasma concentrations of the 3 drugs after giving such dosages of the 2 combined formulations were compared in 16 patients, 8 in Singapore and 8 in Hong Kong, by means of a crossover study, with the concentrations obtained when identical doses of the 3 drugs were given using standard separate drug formulations. The concomitant urinary excretions of the drugs and their major metabolites were also estimated. Very similar results were obtained whether the drugs were given as the combined preparations or in their standard separate formulations, demonstrating the excellent bioavailability of all 3 drugs in each of the 2 combined formulations.

MeSH terms

  • Acetylation
  • Adolescent
  • Adult
  • Biological Availability
  • Drug Combinations
  • Humans
  • Isoniazid / blood
  • Isoniazid / metabolism*
  • Isoniazid / therapeutic use
  • Isoniazid / urine
  • Middle Aged
  • Osmolar Concentration
  • Phenotype
  • Pyrazinamide / blood
  • Pyrazinamide / metabolism*
  • Pyrazinamide / therapeutic use
  • Pyrazinamide / urine
  • Rifampin / blood
  • Rifampin / metabolism*
  • Rifampin / therapeutic use
  • Rifampin / urine
  • Time Factors
  • Tuberculosis / blood
  • Tuberculosis / drug therapy*


  • Drug Combinations
  • isoniazid, pyrazinamide, rifampin drug combination
  • Pyrazinamide
  • Isoniazid
  • Rifampin