Water vapor adsorption of ground cefditoren pivoxil was studied. The amount of water adsorbed increased with a decrease in the crystallinity of cefditoren pivoxil. It was found from the microcalorimetric measurements that the differential heat of water vapor adsorption at 1.5% adsorbed water increased with decreasing crystallinity of cefditoren pivoxil, suggesting that hygroscopicity of cefditoren pivoxil was enhanced by grinding. These results indicated that hydrophilic adsorption sites in cefditoren pivoxil increased through the grinding process. The results of infrared (IR) spectra examination suggested that the increment of hydrophilic adsorption sites through the grinding process resulted from the change of the environment of the carbonyl groups in two esters and amide.