Pharmacokinetics and absolute bioavailability of resveratrol solid dispersion in rats / 中草药

ABSTRACT

Objective To study the pharmacokinetics and pharmacokinetic parameter of resveratrol (RES) crude drug and solid dispersion (RES-PEG) in rats. Methods HPLC-UV was established for detecting plasma concentrations of RES and investigating its pharmacokinetics in rats with ig and iv administration. The software of DAS3.0 was used to process the pharmacokinetic parameters. Results The linear calibration curve was obtained in the range of (10-2.5 × 104) ng/mL for RES, and the lower limit of quantitation was 10 ng/mL. Intra- and inter- day precision for all samples were less than 5.1%, and the accuracy of three different concentrations was in the range from -1.1% to 0.7%. The extraction recovery of RES from rat plasma was from 97.8% to 104.1%. The main pharmacokinetics parameters of RES crude drug and RES-PEG after ig administration, and RES after iv administration were shown as follows t1/2, (2.6 ± 2.0), (2.3 ± 0.8), and (6.3 ± 1.1) h; AUC 0-12, (514.7 ± 117.5), (1 084.6 ± 836.9), and (2 697.3 ± 289.8) ng∙mL/h, respectively; the Cmax of RES crude drug and RES-PEG after ig administration were (473.3 ± 200.8) and (814.1 ± 246.6) ng/mL, respectively. Compared to crude drug, the relative bioavailability of of RES-PEG was about 200%; And the absolute bioavailability of RES crude drug was 5%. Conclusion The oral bioavailability of RES was low. The relative bioavailability of RES crude drug was significantly improved after being prepared into solid dispersion.