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  • Title: [Studies on in-vivo process of the enantiomers of nicardipine in rabbit by coupled chiral and achiral HPLC].
    Author: Wang SC, He LC, Liu F.
    Journal: Yao Xue Xue Bao; 2001 May; 36(5):364-7. PubMed ID: 12584860.
    Abstract:
    AIM: To study the differences of the pharmacokinetics and tissue distribution of two enantiomers of nicardipine in the rabbit. METHODS: Biological samples were diluted by 1 mol.L-1 NaOH solution and extracted with n-hexane--ethyl acetate (1:1). The concentrations of S-nicardipine and R-nicardipine in samples were determined by coupled achiral C18 column (150 mm x 4.6 mm, 5 microns) and chiral OJ column (250 mm x 4.6 mm, 10 microns) chromatography. RESULTS: The racemic nicardipine and the enantiomers in sample were separated well by the coupled system. The linear range was 55-550 ng.mL-1 for both enantiomers. The within-day and between-days RSD (n = 5) were 5.25% and 8.97%, and the relative recoveries were 99.99% and 97.10% for R- and S-enantiomer, respectively. The mean Tmax, Cmax and AUC values were (2.49 +/- 0.03) h, (134 +/- 2) ng.mL-1 and (1082 +/- 32) ng.mL-1.h for S-nicardipine and (1.24 +/- 0.05) h, (109 +/- 2) ng.mL-1 and (778 +/- 22) ng.mL-1.h for R-nicardipine. The concentration of S-nicardipine were generally higher than that of R-nicardipine in main target tissues and cells. CONCLUSION: There were significant differences between the two enantiomers of nicardipine in rabbit in pharmacokinetics and tissue distribution.
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