Background: Oral anti-diabetic drugs (OAD) cannot effectively control blood glucose for patients with type 2 diabetes mellitus (T2DM). The selection of insulin in elderly patients should be smooth in lowering blood glucose, and as far as possible to reduce blood glucose fluctuation, hypoglycemia and weight gain to ensure the safety of medicine. Purpose: To compare the efficacy and safety between insulin detemir combined with repaglinide and insulin aspart 30 (BIAsp30) in treating aged type 2 diabetes mellitus (T2DM) patients who were inefficacious to OAD drugs therapy. Methods: 98 elderly T2DM patients inefficacious to oral anti-diabetic drugs therapy were randomized into detemir combined with repaglinide (Det+Rep) group (50 cases) and BIAsp30 group (48 cases), which were treated with corresponding drugs, respectively. The treatment duration was 12 weeks. Before and after treatment, the indexes in blood glucose, blood lipids, islet cell function, weight increase, hypoglycemia and insulin dosage between two groups were compared. Results: After treatment, the levels of FPG, 2hPG, HbA1c, HOMA-IR, TG, TC, LDL-C in two groups were decreased significantly (P < 0.05), and the levels of FC-P, 2hC-P and HOMA-beta were increased (P < 0.05). The levels of MAGE, CV and HOMA-IR in Det+Rep group were significantly lower than those in BIAsp30 group (P < 0.05), and the levels of FC-P and HOMA-beta in Det+Rep group were significantly higher than BIAsp30 group (P < 0.05). The weight increase rate, incidence of hypoglycemia and insulin dosage in Det+Rep group was significantly lower than BIAsp30 group (P < 0.01). Conclusion: Insulin detemir combined with repaglinide have better efficacy and safety in treating T2DM patients inefficacious to OAD therapy, compared with insulin aspart 30.