| Globally,β-adrenergic blockers are used as the drugs of choice in the treatment of hypertension, cardiac arrhythmias, angina pectoris and glaucoma in clinic. These drugs are chiral drugs as they include one or several chiral center. Because the stereo-selection of drug enantiomers with enzyme and receptor is different, the pharmacologically effective of enantiomers is different. Generally, S(-)-enantiomers are showing about 50-500-fold higher activities than R(+)-enantiomers, so the cure effect of the current prescription of racemicβ-adrenergic blockers is not very satisfied. Thus, the research of pharmacology and pharmacokinetics of drug enantiomers, and the chiral sepeartion and preparation of drug enantiomers to obtain optical pure drugs of good cure effect and low side-effect is very important.In this paper, cellulose derivation chiral stationary phase was synthesized by coating cellulose tris (3,5-dimethylphenylcarbamate) onto aminopropyl silica of different size, and chiral stationary phase high performance liquid chromatography method for resolution and determination of propranolol, metoprolol and atenolol enantioners was established. This method can be used for quality control propranolol, metoprolol and atenolol in different preparations. Based on these, the chiral separation of propranolol was enlarged from analytical scale to semipreparative scale and obtained a small quantity of propranolol enantiomer which can provide foundation of pharmacology and pharmacokinetics of propranolol enantiomers. Restricted-access material was also synthesized by bonding hydrophobic 1-hexylamine on inter silica surface and introducing hydrophilic polyvinyl alcohols on external silica surface. Then, direct analysis of propranolol in plasma using synthesized restricted-access material was established which can be used in the pharmacology and pharmacokinetics of propranolol enantiomers.
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