| Preparations have been targeted on the basis of physiological and pathological conditions of the organization of the design,to the neglect of the drug and in the micro-environment interactions,can still lead to targeted results,but the effect is still not the ideal state.Therefore,the search farnew methods and technologies targeted for manufacturing high efficiency, low toxicity of new drug agents are still necessary.With combination of Bupleurum vinegar with the Rhein to discuss influence of vinegar Bupleurum on distribution of the Rhein in rats.Through the experiment and integration of theory of Chinese medicine with modern ideas of combining targeted drug delivery to discuss the drug mechanism by modern pharmacology.1.The establishment of the test method on Rhein in the blood and organization Objective:The establishment of the test on Rhein-high performance liquid chromatography(RP-HPLC)method in the blood and organization.Methods:HyperClone C18 column to column,a mobile phase of water a methanol (ten ninety),the flow rate of 0.8 mL min-1,in the 430 nm wavelength ultraviolet scanning for detection.Results:In this analysis of the Rhein on the determination of non-interference, recovery was 99.15%to 108.2%,the day the coefficient of variation 1.26%-6.74% (n=5),the day the coefficient of variation 1.02%-7.53%(n=5),serum and Rhein in the minimum detection limits were 0.1 ug / ml and 0.02 ug /g.Oonclusion:Method evaluation results show that this law for determination of serum and tissue Rhein concentration of simple,sensitive and practical analysis,to meet the Rhein in rats the distribution of requirements.2.Influce of Vinegar Bupleurum on the distribution of RheinObjective:The discussion of influce of Vinegar Bupleurum on the distribution of RheinMethods:432 wistar purely male rats divided into 8 groups,a large group for the control group,excluding Bupleurum,the administration of the Rhein For the high-and low-dose group;second largest group vinegar Bupleurum Group, in accordance with vinegar Bupleurum dose at high,medium and low three groups, each group was on drugs at high doses,low two groups,each also The same principle is divided into six groups(each group to a point in time),each of six rats.Using rats were fed with Rhein Suancu Bupleurum and rhubarb mixture, using RP-HPLC determination of blood and viscera of the Rhein concentration, plasma concentration and calculation in the distribution of change,for nine points in time 0.25 h,0.5h,lh,1.5h,2h,3h,4h,6h,8h,each time point six mice.Results:t-test analysis showed that,Rhein and vinegar combination Bupleurum after different time points after administration of drug concentrations in the liver and single-use Rhein at different time points after administration of the drug concentration in the liver single point horizontal comparison are significant differences.Conclusion:A statistically significant,the drug in the blood,heart,liver, spleen,lungs,kidneys distribution showed significant differences.Therefore, vinegar Bupleurum significant changes in the Rhein in rats widely distributed.3.Target rateObjective:The evaluation of vinegar-baked bupleurum' s targetMethods:In order to better evaluate the drug with vinegar-baked Bupleurum the Rhein in rats of the impact of the introduction of the following parameters: the relative uptake rate Re =(AUCi)m/(AUCi)s, Re said in a one organ or tissue in two different formulations of the drug distribution;Re＞1 that the organ or tissue is targeted,Re greater the effect of targeting the better;Re＜1 that the organ or Free targeting,where AUCi by the concentration - the first time curve be called i-organ or tissue when the drug area under the curve,feet superscript m s,respectively,and that combination of vinegar Bupleurum group and single-drug group. Targeting the coefficient Te =(A UCi)m/∑(AUCi), AUCi concentration of the ground - the first time curve be called i-organ or tissue when the drug area under the curve;∑(AUCi)organizations,including the target of all the organizations and the AUC;Te said that the preparations in various organizations of the Targeting efficiency will vinegar Bupleurum Rhein and the application of the combined group targeting single-use efficiency and the Rhein group targeting efficiency of the total,compared to the numerical increase of the greater,better targeting results.Two different formulations of a certain tissues or organs in the drug distribution efficiency can be used to compare Rte =(Te)m/(Te)s Rte＞1 that compared with the control group,vinegar Bupleurum combined with the Rhein after a certain organization has a selective,The greater of Rte selectivity that the targeting is stronger.Results:The combination of vinegar Bupleurum Rhein after low-dose group and high-dose group targeting the liver coefficient(Te)were higher than the controls,Rhein low-dose group:vinegar Bupleurum low-dose group and high-dose group liver free Rhein the relative uptake rate(Re)and drug distribution efficiency(Rte)greater than 1,vinegar Bupleurum dose of drug distribution efficiency(Rte)larger than 1;vinegar Bupleurum low-dose group,the dose and high-dose group Rhein liver metabolites of the relative uptake rate(Re) and drug distribution efficiency(Rte)larger than 1;vinegar Bupleurum low-dose group,the dose and high-dose group in the liver and free Rhein Rhein sum of the metabolites Relative uptake rate(Re)and drug distribution efficiency(Rte)greater than 1.Rhein high-dose group:vinegar Bupleurum low-dose group,the dose and high-dose group in the liver of a relatively free Rhein uptake rate(Re)and drug distribution efficiency(Rte)larger than 1; vinegar Bupleurum low-dose group and In the Rhein-dose group liver metabolites of the relative uptake rate(Re)and drug distribution efficiency(Rte)greater than 1,vinegar Bupleurum high-dose group of drug distribution efficiency(Rte) larger than 1;vinegar Bupleurum in the low-dose group and Dose group and liver free Rhein Rhein metabolites sum of the relative uptake rate(Re)and drug distribution efficiency(Rte)greater than 1,vinegar Bupleurum high-dose group of drug distribution efficiency(Rte)greater than 1.Conolusion:After combination of Rhein Bupleurum and vinegar,distribution of Rhein in rats changes significantly,liver targeting increases,and the study have a high value with the guidance of the drug in the clinical application of science and technology.
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