Quality control of anti-tuberculosis fixed-dose combination formulations in the global market: an in vitro study

Int J Tuberc Lung Dis. 2004 Sep;8(9):1081-8.

Abstract

Objective: To determine the quality, and especially the dissolution properties of rifampicin, of fixed-dose combination (FDC) formulations of anti-tuberculosis agents manufactured by major market holders in the anti-tuberculosis sector and supplied for use in national tuberculosis control programmes.

Methods: Dissolution studies were performed for four formulations supplied by four different manufacturers in four dissolution media (0.1N and 0.01N HCl, phosphate buffer [PB] and 20% vegetable oil in PB), at four different agitation rates using USP apparatus II. The formulations were subjected to 4-week accelerated stability studies (40 degrees C / 75% RH) and evaluated for physical, chemical and dissolution stability.

Results: The formulations tested complied with pharmacopeial quality control (QC) tests. The extent of rifampicin release was independent of dissolution medium; however, a slight decrease in the dissolution rate was observed in two products. More than 75% of drug was released in 45 min at all agitation intensities except 30 rpm, and 20% oil in the medium reflected fed state. Formulations were stable in the packaging conditions recommended by the manufacturer for at least 4 weeks.

Conclusions: The formulations tested passed the QC tests and were found to be stable. A decrease in the rate, although not the extent, of dissolution necessitated multiple point dissolution in gastric and intestinal pH conditions to ensure consistency in in vivo bioavailability.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antibiotics, Antitubercular / chemistry
  • Antibiotics, Antitubercular / pharmacokinetics
  • Antibiotics, Antitubercular / standards*
  • Antitubercular Agents / chemistry
  • Antitubercular Agents / pharmacokinetics
  • Antitubercular Agents / standards*
  • Biological Availability
  • Chemistry, Pharmaceutical
  • Drug Industry*
  • Drug Therapy, Combination
  • Global Health
  • Humans
  • Product Packaging*
  • Quality Control
  • Rifampin / chemistry
  • Rifampin / pharmacokinetics
  • Rifampin / standards*
  • Solubility
  • Tuberculosis, Pulmonary / drug therapy

Substances

  • Antibiotics, Antitubercular
  • Antitubercular Agents
  • Rifampin