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Objective:To develop an HPLC method for the simultaneous determination ofirinotecan(CPT-11) and its active metabolite 7-ethyl-10-hydroxycamptothecin (SN-38) in human plasma.Methods:The internal standard was 10-hydroxycamptothecin.CPT-11 and SN-38 were extracted with ethyl acetate after a complete protein precipitation with 10% perchloric acid,then injected into a Hypersil C18(250 mm×4.6 mm,5um) column; The mobile phase was potassium dihydrogenphosphate (0.1mol·L-1)-acetonitrile (75∶25,adjusted pH3.0 with phosphoric acid);monitored at excitation and emission wavelengths of 355nm and 515nm,respectively.