Formulation and Evaluationof Combination of Artemether and Lumefantrine as Tablets

Abstract

The objective of the present study was to fabricate and evaluate a combination of Artemether and Lumefantrine as tablets and to make Artemether in sustained form as to prolong its elimination time. Artemether was formulated in form of microspheres and was then formed into the tablet along with the Lumefantrine. Artemether microspheres were prepared and compressed into compressible tablet by direct compression process using the compressible excipients along with Lumefantrine, which entails the convenience of a sustained release product in one. The rationale behind this combination is that Artemether initially provides rapid symptomatic relief by reducing the number of parasites present before Lumefantrine eliminates any residual parasites. This is thought to minimize development of resistance because the malaria parasites are never exposed to Artemether alone due to its rapid elimination. Although they may be exposed to Lumefantrine alone, the probability of resistance developing simultaneously to both drugs used in combination is thought to below. The Artemether microspheres were formed by solvent evaporation technique using ethyl cellulose as a polymer, in presence of polyvinyl alcohol as surfactant. Due to the sustained property of polymer and surfactant property of polyvinyl alcohol, formulated microspheres can result in controlled release of drug. Ethyl cellulose coated microparticles have also demonstrated their capability to absorb pressure and therefore save the coating from fracture during tablet manufacturin gprocess.