Comparative bioequivalence study of rifampicin and isoniazid combinations in healthy volunteers

Int J Tuberc Lung Dis. 1999 Jul;3(7):627-31.

Abstract

Objective: To assess the bioavailability of rifampicin (RMP) in three brands of combination formulations of anti-tuberculosis drugs.

Design: A three-way double-blind, cross-over bioavailability study of RMP and isoniazid (INH), consisting of a comparison of a two-drug combination of tablets of RMP and INH each separately (reference brand R) and a tablet of RMP + INH (brand N), and a capsule of RMP + INH (brand L) was carried out in 12 healthy male volunteers. Coded plasma samples were analysed for levels of RMP as well as INH and acetylisoniazid (ACINH) by two high performance liquid chromatography (HPLC) methods.

Results: The mean values of RMP in brand N (Cmax 6.49+/-0.52 microg/mL, Tmax 2.33+/-0.18 h, AUC(0-24h) 39.83+/-3.44 microg/mL.h) were comparable with those obtained with brand R (Cmax 5.22+/-0.59 microg/mL, Tmax 2.50+/-0.12 h, AUC(0-24h) 33.33+/-3.47 microg/mL.h). The mean values of RMP in brand L (Cmax 3.05+/-0.52 microg/ mL, Tmax 3.79+/-0.57 h and AUC(0-24h) 21.78+/-3.67 microg/ mL.h) were significantly different from those in brand R. Nevertheless, all of the pharmacokinetic parameters obtained for INH and ACINH in all three brands were comparable.

Conclusion: Using brand R as a comparison, brand N was bioequivalent and brand L was not bioequivalent.

Publication types

  • Clinical Trial
  • Comparative Study
  • Randomized Controlled Trial

MeSH terms

  • Adolescent
  • Adult
  • Antibiotics, Antitubercular / administration & dosage
  • Antibiotics, Antitubercular / blood
  • Antibiotics, Antitubercular / pharmacokinetics*
  • Antitubercular Agents / administration & dosage
  • Antitubercular Agents / blood
  • Antitubercular Agents / pharmacokinetics*
  • Area Under Curve
  • Biological Availability
  • Chromatography, High Pressure Liquid
  • Cross-Over Studies
  • Double-Blind Method
  • Drug Administration Schedule
  • Drug Combinations
  • Drug Therapy, Combination
  • Humans
  • Isoniazid / administration & dosage
  • Isoniazid / blood
  • Isoniazid / pharmacokinetics*
  • Male
  • Reference Values
  • Rifampin / administration & dosage
  • Rifampin / blood
  • Rifampin / pharmacokinetics*
  • Therapeutic Equivalency

Substances

  • Antibiotics, Antitubercular
  • Antitubercular Agents
  • Drug Combinations
  • Isoniazid
  • Rifampin