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A rapid, selective and sensitive method using UPLC‐MS/MS was first developed and validated for quantitative analysis of koumine in rat plasma. A one‐step protein precipitation with methanol was employed as a sample preparation technique. Plasma samples were separated on an Acquity UPLC BEH C18 column (50 × 2.1 mm, i.d. 1.7 µm) with a gradient mobile phase consisting of methanol with 0.1% (v/v) formic...