Design, synthesis, and characterization of pharmaceutical cocrystal of testosterone and 4, 4-dihydroxybiphenyl

Testosterone (T) is a steroid hormone with poor solubility, which can maintain muscle strength and enhance physical strength. The cocrystal (T·DOD·H2O) of testosterone and 4, 4-dihydroxyl biphenyl (DOD) was synthesized using solution crystallization technology in the stoichiometric ratio of 1: 1, and then characterized by single crystal X-ray diffraction (SXRD), powder X-ray diffraction (PXRD), Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and thermogravimetry (TG). Subsequently, the solubility and powder dissolution rate of the cocrystal were tested, and the results show that the solubility of the cocrystal is increased by 8.37 times and the powder dissolution rate is risen to 34.1 times compared with the pure testosterone. Obviously, the solubility of testosterone is highly increased by pharmaceutical cocrystal, which is a potential strategy of improving poorly soluble active pharmaceutical ingredients.