A simple and efficient ultrasonic-assisted extraction of bioactive compounds from raw Bupleuri Radix and vinegar-baked Bupleuri Radix was developed and optimized by using quantitative analysis of multi-components by a single-marker combined with response surface methodology approaches. The quantitative analysis of multi-components by a single-marker analytical method based on high-performance liquid chromatography coupled with a photodiode array detector was established and applied to determine the contents of six bioactive compounds in raw Bupleuri Radix and vinegar-baked Bupleuri Radix. In order to maximize extraction of six bioactive compounds in raw Bupleuri Radix and vinegar-baked Bupleuri Radix, the ultrasonic-assisted extraction conditions were obtained by the response surface methodology coupled with Box–Behnken design. The conditions of ultrasonic-assisted extraction were found to be effective for the extraction of bioactive compounds from raw Bupleuri Radix and vinegar-baked Bupleuri Radix. The test results showed that the difference in saikosaponins contents in these samples was obvious; a quantitative analysis of saikosaponins will contribute significantly to improving the quality control of raw Bupleuri Radix and vinegar-baked Bupleuri Radix. In conclusion, the designed protocol is suitable for the quality control of raw Bupleuri Radix and vinegar-baked Bupleuri Radix.
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