Rifampicin-arginine complex was prepared to increase the solubility and dissolution rate of rifampicin. Solvation method was applied to make the complex and its formation was identified by the solubility method, powder x-ray diffractometry, differential thermal analysis and spectroscopic determination. The complex was formed in the molar ratio of 1 : 1 which was proved by the slope ratio method and continuous variation method. The complex was a non-crystalline form determined by the x-ray powder diffractometric analysis. The solubility of complex in water was significantly higher than that of rifampicin itself. The stability constant and thermodynamical properties of the complex were determined to investigate the solubilization phenomena. The thermodynamic data showed that the complexation between rifampicin and arginine was an exothermic and spontaneous reaction. Simulated absorption studies carried out through the artificial lipid barrier in artificial gastric and intestinal juices. The results showed that the complex had an enhanced absorption rate of rifampicin nearly twice compared with that of rifampicin itself.