Dissolution Rate Enhancement and Physicochemical Characterization of Artemether and Lumefantrine Solid Dispersions

Ritesh Amol Fule, Tarique S. Meer, Ajay R. Sav, Purnima D. Amin

Abstract


The current study was conceded out with a vision to enhance solubility and thereby dissolution rate of poorly water soluble Artemether [ARTM] and Lumefantrine [LUM] [BCS-class IV drugs] using Lutrol F127 as carrier surfactant. It’s difficult to choose a single carrier which forms solid dispersion [SD] with both the drugs by melt method. For which number of polymers and combination trials were carried out and finally Lutrol F127 was selected for further studies. SD was prepared by melt method using different ratios of drug and Lutrol F127. Saturation solubility study was conducted to evaluate the effect of polymer on aqueous solubility of ARTM and LUM. Solid state characterization was evaluated by fourier transformation infrared spectroscopy, differential scanning calorimetry, x-ray diffraction study and scanning electron microscopy. In vitro dissolution study was performed in phosphate buffer at pH 7.2 [with 1% SLS] and 0.1 N HCl [with 2% Benzalkonium chloride, BKC] for ARTM and LUM respectively. Solid state study showed partial interaction between drug and Lutrol F127. In vitro dissolution rate of ARTM and LUM from SD was significantly higher compared to pure drug. The dissolution rate of SD prepared by melt method was found to be higher than that of pure drugs and their physical mixtures. Thus, SD using melt method can be successfully used for the improvement of the dissolution rate of ARTM and LUM.


Keywords


Artemether, Lumefantrine, Solid dispersion, Melt method, Solubility, Dissolution rate

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