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Cyclodextrin-modified CZE was applied to the chiral separation of two basic drugs, i.e.,esmolol and terazosin. Selector screening and concentration optindzation experiments wereperformed. Resolution 3.1 for esmolol, 1 .2 for terazosin were achieved when using 60 mmol/L γ-CD and 60 mmol/L DM-β-CD, respectively, in 50 mmol/L pH 2.5 sodium phosphate buffer.