OBJECTIVE: To optimize the methanol extraction technology of tripterine in the fruit of Celastrus monospermus. METHODS: HPLC was adopted to determine the content of tripterine. Using extraction time, extraction times, solid-liquid ratio as investigation factors, extraction rate of tripterine as investigation index, orthogonal test was designed, and verification test was conducted. RESULTS: The optimal methanol extraction technology was as follow as 45% methanol extracting 2 h each time with solid-liquid ratio of 1 ∶ 8 for 3 times. In the verification test, the average extraction rate of tripterine was 0.917 mg/g (RSD=2.85%, n=3). CONCLUSIONS: The optimized methanol extraction technology is stable and feasible with high extraction rate, and is suitable for the extraction of tripterine in the fruit of C. monospermus.