Stereoselective HPLC Assay of TJ0711 Enantiomers by Precolumn Derivatization with GITC Using UV Detection and Its Application in Pharmacokinetics in Rats

【摘要】 This investigation describes a new precise,sensitive and accurate stereoselective RP-HPLC method for determination of the enantiomers of a novelα-andβ-receptor blocking agent, 1-[4-(2-methoxyethyl)phenoxy]-3-[[2-(2-methoxyphenoxy)ethyl]amino]-2-propanol(TJ0711),in rat plasma.GITC was used for precolumn derivatization of TJ0711 enantiomers.Enantiomeric resolution was achieved on a Eurospher-100 C18 column(250 mm×4.6 mm ID,5-μm particle size),with UV detection at 255 nm,and the mobile phase consisted of acetonitrile and water(58:42,v/v)containing 0.02%glacial acetic acid(v/v).Using the chromatographic conditions described,TJ0711 enantiomers were well resolved with mean retention time of 10.2 and 11.5 min,respectively.Linear response(r>0.999)was observed over the range of 0.125-12.5μg/mL of TJ0711 hydrochloride enantiomers.The mean relative standard deviation(RSD%)of the results of within-day precision was≤ 10%.The proposed method was found to be suitable and accurate for the quantitative determination of TJ0711 enantiomers in rat plasma,and it can be used in pharmacokinetic studies.更多还原

【Abstract】 This investigation describes a new precise,sensitive and accurate stereoselective RP-HPLC method for determination of the enantiomers of a novelα-andβ-receptor blocking agent, 1-[4-(2-methoxyethyl)phenoxy]-3-[[2-(2-methoxyphenoxy)ethyl]amino]-2-propanol(TJ0711),in rat plasma.GITC was used for precolumn derivatization of TJ0711 enantiomers.Enantiomeric resolution was achieved on a Eurospher-100 C18 column(250 mm×4.6 mm ID,5-μm particle size),with UV detection at 255 nm,and the mobile phase consisted of acetonitrile and water(58:42,v/v)containing 0.02%glacial acetic acid(v/v).Using the chromatographic conditions described,TJ0711 enantiomers were well resolved with mean retention time of 10.2 and 11.5 min,respectively.Linear response(r>0.999)was observed over the range of 0.125–12.5μg/mL of TJ0711 hydrochloride enantiomers.The mean relative standard deviation(RSD%)of the results of within-day precision was≤ 10%.The proposed method was found to be suitable and accurate for the quantitative determination of TJ0711 enantiomers in rat plasma,and it can be used in pharmacokinetic studies.更多还原