The Preliminary Study Of The Quercetrin Sodium Chloride Injection And Pharmacokinetic Study Of Quercetrin

Objective:Receaching Quercetrin sodium chloride injection prescribe screened and technique studied; found the method that a simple sensitive reliable HPLC-MS/MS to determineQuercetrin concentration of biological samplein rat; Receach the pharmacokinetics and tissuedistributionsof Quercetrin in rat.Method:1.Use the high purityQuercetrin as material, through a single factor experiment to compare different method of cosolvent PH and sterilization,screening and optimizing the Quercetrin sodium chloride injection prescribe.2.Through the inspect of 4 ??40 ??60 ? and beam in 4500 LX to screen the influence factor of injection and preservation condition.3. Study the quality standards of Quercetrin sodium chloride injection according to injection relevant provisions in Chinese pharmacopoeia.4.Use multiple reaction monitoring,MRM to monitor Negative ion mode, to monitoring ion pair meanwhile the luteolin as internal standards:Quercetrin m/z 447.1?300.00,luteolin m/z 285.0?133.00 to test methodology.5.Detected the changes of drugconcentrationin plasma after intravenous administrationwith different dose(5?10?20 mg/kg) and intragastric administration Quercetrin(20 mg/kg);Detect the drug concentration in diffidenttissues.Result:1.Selected PEG-400 as cosolvent and filtration as the way sterilization, the pH was5.0~6.0;Process route:(1)Use absolute ethyl alcohol to dissolve the material,obtaining the dense solution according to the prescription to add PEG-400.(2)Weighed fixed NaCl and NaHSO4 to dissolve with water, activated carbon adsorbing anddecarbonization,constant volume,screened, split charging, sterilization.2.Inspected affect factor, injection stabilizing in the environment of 4 ??40 ?,while the injection content decreased in the environment of 60 ?and4500 LX.3.Making the quality standards of Quercetrin sodium chloride injection. 4.Quercetrin method curve as Y=0.0043 X+0.000611,and linear relationship was well(R=0.9972),linear extent 6~14430 ng/ml, quantitative lower limit 6 ng/ml; Precision and Accuracy were all within 15%; Quercetrin in blood plasma percent recovery was within 89%~98%; matrix effects was within 85 %~106 %. 5.After intravenous administrationwith different dose, the t1/2was within 0.3h~0.6h, while the CLz was 2.56~4.55 L/h/kg.through three dose AUC, Quercetrin showed non-linear dynamical features; After intragastric administration, the Cmax was 45.83 ng/ml,andt1/2 is 3.01 h, and Vz/F was 455.48 L/kg,the bioavailability was 2.39 %.Conclusion: Preliminary researched Quercetrin sodium chloride injection prescription and technology,provide scientific basis for intensive study. It was exact and easy to operate that method was founded which is called HPLC-MS/MS to test biological sample. The preliminary study of the pharmacokineticsand tissuedistributionsprovided a basis for clinical medication, and to provide theoretical reference for further research and development.