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The Research and Validation of the Method for the Enantioseparation and Analysis of Propranolol, Metoprolol and Bisoprolol

Author: ZhaoJing
Tutor: ZhaoHua
School: Chongqing Medical University
Course: Drug analysis
Keywords: propranolol metoprolol bisoprolol enantiomers separation
CLC: R917
Type: Master's thesis
Year: 2011
Downloads: 126
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Abstract


OBJECT:The separation and retention behaviors ofβ-receptor blockers such as propranolol,metoprolol and bisoprolol enantiomers on polysaccharides chiral stationary phase columns,including Chiralpak AD column, Chiralcel OD column, Chiralpak AS column and Chiralcel OJ column was studied.The effects of mobile phase on the separation of the three enantiomers were investigated simultaneously .An effective method of separating propranolol,metoprolol and bisoprolol isomers by Normal chiral-stationary phase HPLC was established.METHODS:The experiments were carried on chiral stationary phase columns such as Chiralpak AD, Chiralcel OD, Chiralpak AS and Chiralcel OJ column,using n-hexane to alcohol consisting of isopropanol ,ethanol and methanol as the basic mobile phase and appropriate DEA as alkaline additives. The flow rate was 1.0 mL/min , the detection wavelength of propranolol,metoprolol and bisoprolol was 287 nm and 272 nm,respectively and the column temperature was 30℃.RESULTS:Propranolol , metoprolol and bisoprolol enantiomers were achieved baseline separation both on Chiralpak AD columna and Chiralcel OD column .Contrast to the other enantiomers ,only propranolol was achieved baseline separation on chiralcel OJ column and only bisoprolol got better separation on Chiralpak AS. No change of elute order of three enantiomers was observed by altering the alcohols in mobile phase. The two enantiomers of propranolol had a good linear relationship in the range of 0 ~ 37μg/mL , the regression equations were: R-propranolol, Y=18429C+7895.9 , r =0.9992 ,S-propranolol, Y=18904C+3223 , r =0.9988,respectively .The detection limit of S-propranolol was 0.27 ng,and R-propranolol was low to 0.2 ng.CONCLUSION:The established enatioseparation and analysis method of propranolol,metoprolol and bisoprolol could be applied to study the isomers’pharmacology and Pharmacokinetics and to provide a reliable method for the detection of single isomer drugs’optical purity.

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