Solid Dispersion of Artemether in Fast Disintegrating Tablet to Enhance Dissolution Rate and Oral Bioavailability

Abstract:

Objectives: Artemether (ART), an antimalarial drug, have poor solubility and low bioavailability. Therefore, solid dispersion of the drug was formulated using Soluplus (SOL) and was incorporated in the fast disintegrating tablet. Materials and Methods: The solid dispersion (SD) was prepared using the solvent evaporation method using a rotary evaporator. The optimized SD was evaluated and then incorporated into the tablet. Results: Solubility studies revealed that ART SD A3 of ratio 1:3 (ART: SOP) showed a significantly higher solubility and dissolution rate than plain ART. FTIR results indicated that there was no incompatibility between the drug and hydrophilic carrier. The DSC as well as XRD studies indicated the transformation from crystalline state of drug into the amorphous form. SEM studies revealed the deposition of ART on the surface of the hydrophilic carrier. In-vitro antimalarial activity was improved of the ART due to the SD formulation. Fast disintegrating tablet of ART SD A3 was produced by using directly compressible excipients such as Ludiflash and Ludipress. Ludiflash containing tablet showed fast disintegration with higher drug release. The pharmacokinetic study in mice showed increased Cmax and AUC0–24 by 1.88- and 3.19-fold as compared to those of plain drug. Conclusion: The prepared SDs using SOP provided a platform for increased solubility and also improved the bioavailability of ART with feasibility for tablet formulation.

Key words: Artemether, Solid dispersion, Fast disintegrating tablet, Malaria, in-vivo study.