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Intravenously injectable emulsion of β-elemene was studied in detail. Both blank and β-elemene-loaded microemulsions were prepared using a simple water titration method. The pseudoternary phase diagram was constructed for the optimization of microemulsion. The loading capacity test, dilutability test, and especially the influence of antioxidants were conducted for further optimization of β-elemene-loaded microemulsion. Transmission electron microscope showed intact and spherical microemulsion droplets. Conductivity and viscosity measurements were used to study the phase behaviors of β-elemene-loaded microemulsions, providing convincing explanation. In vitro release study showed that β-elemene was steadily released until 12 h, which most fitted the first order.