The Pharmacokinetics Research On Baicalin And Geniposide In Qingkailing Injection

The main ingredients of Qingkailing Injection is bile acid, nacre, hyodeoxycholic, gardenia, water buffalo, radix, baicalin and honeysuckle. The product is brown or reddish brown clear liquid. Themain therapeutic effect of injection:detoxification, phlegm meridians, refreshing fails to grasp. Fever, coma, stroke, paralysis and unconsciousness can also be used for acute and chronic hepatitis, hepatitis B, upper respiratory tract infection, pneumonia, high fever, and cerebral thrombosis, cerebral hemorrhage and other symptoms.The main subject of the study is to research pharmacokinetics of the two major components of baicalin and geniposide. It is divided into three parts:the determination of the chromatographic conditions, the optimization of pretreatment conditions in the blood, Dynamic studies in rabbits of QingKaiLing injection.The first part is to establish chromatographic conditions in reversed-phase high performance liquid chromatography of baicalin and geniposide.The main contents:chromatography conditions, the linear relationship, the inspection of precision and stability. There has big polarity difference in the two components; we can use gradient elution to shorten the analysis time. The mobile phase follows:Acetonitrile(A)-0.18%Phosphoric acid solution (B)(0-25min,5%A-18%A, λ=240nm;25-50min,18%-40%A, λ=276nm), flow rate is1ml/min, column temperature sets at30℃. Establish a good detection method for the simultaneous separation of the two main ingredients in the same chromatographic conditions. Baicalin, geniposide and other impurity peaks have better separation and peak shape.The second part is to optimize the blood sample pre-treatment conditions. This process has a great impact on the analysis result. In this study, there are some important factors:the organic precipitant (Methanol, Acetonitrile, Acetone), the neutral salt (sodium chloride), acid salt (sodium dihydrogen phosphate), centrifugation speed (4000r/min,8000r/min and12000r/min) bath temperature (60℃,70℃,80℃) to examine.And after comparision.we gain the optimum pre-treatment methods:a mixture of methanol and sodium dihydrogen phosphate as the precipitating agent, centrifugation twice to precipitate the protein, the speed is4000r/min and70℃for nitrogen to dryness, constant volume, detection, and recoveries of baicalin(71.4%) and geniposide(77.1%) are in the higher range.The third part is to study the pharmacokinetics of baicalin and geniposide in rabbits by injecting Qingkailing through ear vein and obtain whole blood in the specified time. After separation and detection, we obtain a series of the pharmacokinetic parameters about the two components. Baicalin t1/2α=35.517min, t1/2β=6931.472min, V1/F=4.038L/kg, CL/F=0.166L/min/kg. Geniposide t1/2=15.906min, Ke=0.0441/min, V1/F=1.03L/kg, CL/F=0.045L/min/kg.