Abstract:
The study is aimed at evaluating the physical properties, quality control parameters and the dissolution profiles of commercial samples of artemether-lumefantrine tablets. The physiochemical parameters and assay of six brands of the products were assessed through the evaluation of uniformity of tablet weight, friability, hardness, disintegration and assay of active pharmaceutical ingredient according to established methods. The dissolution rate and disintegration time were determined in simulated gastric fluid (SGF) and simulated intestinal fluid (SIF) without enzymes. The dissolution efficiency (DE) of the tablets of the various brands was used to adjudge their likely in vivo bioavailability. All brands complied with official requirements for uniformity of weight, friability and hardness tests. The disintegration test had higher times in SIF relative to SGF. The dissolution profiles in SGF revealed that two samples attained 70% dissolution in less than 50 min while other samples in more than 1 hour. Only the innovator product, brand A, had T₇₀ of 21 min and others not less than 1.5 hour in SIF. UV spectrophotometric assay of artemether content revealed only three samples containing not less than 90% (w/w) of labeled chemical content. The (DE) for the various brands was significantly higher in SIF relative to SGF (p<0.05). None of the brands evaluated in the study demonstrated comparable quality standards in SGF with respect to the investigated parameters. The method is simple and rugged in routine evaluation of the dissolution profiles of the brands of atemether-lumefantrine available in drug stores and could serve as a useful indicator for quality at the production line.

Keywords: Artemether-Lumefantrine, Multi-source, Dissolution Efficiency, Bioavailability.