Pharmacokinetic Studies Of Dihydromyricetin In Mice

About pharmacokinetic study of dihydromyricetin from Ampelopsis grossdentata,which is themain active ingredient,after administration in mice, in order to lay the foundation forcomprehensive preclinical pharmacokinetic studies and drug development, and enhance the valueof traditional Chinese medicine, which will effectively promote the depth development ofTengcha resources.The main contents and results are as follows:1. use hot water to extract dried tender stems and leaves of Ampelopsis grossdentata,isolatedover a silicone column, after that, the white powder was identified as DMY by UV, TLC, HPLC,MS detection, purity is up to95.1%by HPLC, can be administered as a single dihydromyricetinfor pharmacokinetic and tissue sdudy.2. a simple and effective HPLC method with ultraviolet detection was established for thequantification of DMY in mice plasma. the method was validated, the standard curve was linearwithin the range of0.04~10μg·mL-1. the limit of detection was0.04μg·mL1; The intra-day andinter-day (RSD) for the measurements of quality control samples were less than15%.,RE wereless than15%, respectively, the recovery for plasma samples was>70%, and all datas and resultsshowed that The method established in line with the guiding principles of the analysis ofbiological sample, and HPLC method could be applied to determine the concentration of DMY inmice plasma precisely.After low, middle and high dose gavage, plasma concentrations of mice in each group wererising rapidly changing trends in mice plasma concentration is more consistent, pharmacokineticparameters of middle dose group are as follows: AUC(0-∞),35.13±3.97μg·mL-1·min， Tmax,20.00±0.03min，Cmax,0.52±0.06μg·mL-1, t1/2z,42.42±3.14min, CLz/F,85.41±8.16L·h-1·kg-1.After intravenous administration, AUC(0-∞),27.12±1.95μg·mL-1·min，t1/2z,32.04±3.41min，CLz,11.06±1.90L·h-1·kg-1, After oral administration, Tmax was about20min, indicated thatDMY rapidly absorbed in mice, t1/2was about35min, showed that half-life of the drug is short, itis eliminated quickly. After intravenous,the logC-T cave was concave trend, suggesting DMY inmice kinetics consistent with linear pharmacokinetics.This is the first bioavailability study about dihydromyricetin.the absolute bioavailability of DMY,which administered in three doses was calculated, respectively,10.3%,12.9%,10.5%, itindicated DMY have a low absolute bioavailability in mice.