RESUMO
The concentrations of berberine (BBR) and 8-cetylberberine (8-BBR-C16) in rat plasma and tissue were determined by RP-HPLC. Both the plasma pharmacokinetics characteristic and tissue distribution differences of BBR and 8-BBR-C16 were compared to provide experimental data for the mechanism research and further drug development. After the oral administrations of BBR and 8-BBR-C16 at the dose of 80 mg x kg(-1) for rats, the pharmacokinetics result showed that compared with BBR, the C(max) and AUC(0-t), of 8-BBR-C16 increased by 2.8 times and 12.9 times respectively, t1/2 extended from 3.61 h to 11.90 h. The tissue distribution result showed that compared with BBR, the concentration of 8-BBR-C16 in various organizations increased and the retention time extended remarkably. The maximum concentration was achieved in lung and the highest concentration in it was 3 731.82 ng x g(-1). After being derived, the C(max) in plasma and bioavailability of 8-BBR-C16 increased remarkably and the circulation time in vivo extended. The drug concentration in tissue increased remarkably, and the distribution ratio changed too, with strong targeting selection in lung.
RESUMO
Duosuike Tiancha contain multiple dihydrochalcone sweet constituents, which are mainly active constituents. For the purpose of overall assessment on quality Duosuike Tiancha, 5 sweet dihydrochalcones in Duosuike Tiancha, phloridzin, phloretin-4'-beta-D-glucopyranoside, 3'-O-acetylphloridzin, 2'-O-acetylphloridzin and phloretin are determined as indicators. The separation was carried out through a isocratic elution using a Waters Acquity UPLC BRH C18 (2.1 mm x 100 mm, 1.7 microm) column and a mobile phase consisting of water (75%) and acetonitrile (25%) at a flow rate of 0.5 mL x min(-1). The detection wavelength was set at 285 nm. The column temperature was 40 degrees C. Under the optimized conditions, all the 5 sweet constituents were successfully separated with in 6 min, and good linearity (r2 > 0.999 1) was achieved. The linear range (g x L(-)) and recoveries were tested with results of 0.022 2-0.444 (98.37%), 0.102 84. 112 (97.32%), 0.003 39-0.067 68 (96.77%), 0.005 1-0.204 (98.85%) and 0.000 538-0.010 76 (100.91%) respectively. The results indicate that the content of the 5 dihydrochalcones were 7.83-62.37, 114.24-272.35, 0-1.02, 0-5.11 and 0.10-1.19 mg x g(-1), respectively. Furthermore, with certain regularity between their content and the sample size, harvest time. The separation and analysis method are fast and simple, as evidenced by the fact that the gradient elution is adopted to rapidly determine one sample within six minutes. Therefore, it can be used for dsetermine 5 sweet dihydrochalcones Duosuike Tiancha.