Chiral HPLC determination and stereoselective pharmacokinetics of tetrahydroberberine enantiomers in rats.

Tetrahydroberberine (THB), a racemic mixture of (+)- and (-)-enantiomer, is a biologically active ingredient isolated from a traditional Chinese herb Rhizoma corydalis (yanhusuo). A chiral high performance liquid chromatography method has been developed for the determination of THB enantiomers in rat plasma. The enantioseparation was carried out on a Chiral®-AD column using methanol:ethanol (80:20, v/v) as the mobile phase at the flow rate 0.4 ml/min. The ultraviolet detection was set at 230 nm. The calibration curves were linear over the range of 0.01-2.5 μg/ml for (+)-THB and 0.01-5.0 μg/ml for (-)-THB, respectively. The lower limit of quantification was 0.01 μg/ml for both (+)-THB and (-)-THB. The stereoselective pharmacokinetics of THB enantiomers in rats was studied after oral and intravenous administration at a dose of 50 and 10 mg/kg racemic THB (rac-THB). The mean plasma levels of (-)-THB were higher at almost all time points than those of (+)-THB. (-)-THB also exhibited greater C(max), and AUC(0-∞), smaller CL and V(d), than its antipode. The (-)/(+)-enantiomer ratio of AUC(0-∞) after oral and intravenous administration were 2.17 and 1.43, respectively. These results indicated substantial stereoselectivity in the pharmacokinetics of THB enantiomers in rats. Copyright © 2012 Wiley Periodicals, Inc.

Citation

Yinying Zhang, Kuan Shi, Jun Wen, Guorong Fan, Yifeng Chai, Zhanying Hong. Chiral HPLC determination and stereoselective pharmacokinetics of tetrahydroberberine enantiomers in rats. Chirality. 2012 Mar;24(3):239-44

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PMID: 22271601

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