HPLC with pre-column derivatization for determination of taurine and aminocaproic acid in compound taurine ophthalmic solution was established.A Hypersil ODS (4.6 mm × 200 mm, 5 μm) was used with the mobile phase of phosphate buffer (pH 7.0)-acetonitrile-water (70:12:18), and detection wavelength was at 360 nm.The linear ranges of taurine and aminocaproic acid were 77.64-116.50 μg/mL and 77.96-116.93 μg/mL, resp.The average recoveries of taurine and aminocaproic acid were 99.83% and 99.78% with RSD of 0.43% and 0.49%, resp.The detection limit of taurine and aminocaproic acid was 4 ng/mL.The method was accurate, and could be used for quality control of compound taurine ophthalmic solution