Abstract
Background: Artemether (ARTM) under Biopharmaceutical Classification System (BCS), is a class IV drug, due to its poor water solubility and permeability. It is very effective against acute and severe forms of falciparum malaria, thus the need to improve its solubility and short half-life. Objective: To enhance the solubility and dissolution rate of ARTM by preparation of solid dispersions using the solvent evaporation method. Materials and method: The solid dispersion of ARTM was prepared using okra and acacia gums as polymers in the ratio of 1:1 to 1:5. The direct compression method of formulation was used to formulate them and coated in order to control drug release. Formulations were evaluated and characterized as loading efficiency, flow properties, tablet thickness, weight uniformity, hardness, disintegration time and in vitro studies on the coated tablets. Result: ARTM coated tablets exhibited weight range of 299.4±0.25 to 305.7±1.70 mg. Friability ranged from 0.7 to 1.0% and hardness ranged from 2.4±0.08 to 3.7±0.08 Kgf. The disintegration time was within the range of 4.42±0.01 to 5.64±0.02. The hardness and disintegration time of the tablets increased as the quantity of the polymers increased, while the friability decreased as amount of the polymers increased. The drug content ranged from 85.3±0.47 to 89.1±0.08. Conclusion: These findings suggest that preparation of ARTM tablets using okra gum as a carrier, could be a viable option for enhancing the dissolution rate and controlling the drug release of ARTM.
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