The invention discloses riboflavin derivatives, and a process of preparing the same, and their applications. The w/o suspending preparation of the riboflavin derivatives has high stability, and the effects could last for 3 months after intramuscular injection at dose of 150 mg. This invention increases significantly the bioavailability of riboflavin in vivo, and provides an important treatment method for cure of ariboflavinosis. The preparation is found to have remarkable effect on dermatitis, oral and digestive tract catarrhs caused by bone marrow transplantation for leukemia and chemotherapy for tumor. It is also found to have noticeable effect on persistent oral ulcer, and enhance the tolerability to chemotherapy and radiotherapy. In the treatment of coronary heart disease and hypertension syndrome, arthritis and burn wound, the preparation also has significant effects. This invention has a wide application perspective for its simple techniques, definite long-acting action and effectiveness.