The invention relates to tyrosine hydroxylase inhibitors for the treatment of intestinal hyperpermeability, and provides methods, compositions and kits for the treatment of intestinal hyperpermeability in a subject in need thereof, the intestinal hyperpermeability includes conditions such as hyperglycemia and conditions such as diabetes, autism, fibromyalgia, inflammatory bowel disease (IBD), graft versus host disease (GVHD), HIV / AIDS, multiple organ dysfunction syndrome, irritable bowel syndrome (IBS), celiac disease, eczema, psoriasis, acute pancreatitis, Parkinson's disease, depression, chronic fatigue syndrome, asthma, multiple sclerosis, arthritis, and the like. The medicine can be used for treating basic diseases such as ankylosing spondylitis, non-alcoholic fatty liver disease, alcoholic cirrhosis, environmental intestinal lesion or malignant dystrophy.