Comparative Study On Pharmacokinetics And Antibacterial Activity Of Super - Pieces And Traditional Pieces In Clinical Application

Object:To make comparative study about pharmacokinetic parameters and pharmacodynamic of bacteriostatic action with honeysuckle superfine yinpian and traditional yinpian. To explore whether the proportion of the clinical dosage of the superfine and traditional yinpian is proper. Try to provide experiment basis on reasonable conversion of clinical dosage.Methods:Make honeysuckle superfine yinpian and traditional yinpian as the research object,given the rabbits with honeysuckle superfine yinpian and traditional yinpian,whose dosage ratio is 1:6.Make chlorogenic acid,which is the main active ingredient in honeysuckle,as test index. Determine chlorogenic acid concentration in rabbit blood plasma by using Liquid ms chromatograph. Fit the kinetic parameters of chlorogenic acid by using DAS software.Make research on bacteriostatic action of honeysuckle superfine yinpian and traditional yinpian through the pharmacological method. Filter method is used to determine honeysuckle ultra-fine slices and traditional yinpian bacteriostatic activity.double dilution method is used to determine the minimal inhibitory concentrations of honeysuckle ultra-fine slices and traditional yinpian.Results:Make honeysuckle superfine yinpian and traditional yinpian as the research object,and make chlorogenic acid,which is the main active ingredient in honeysuckle,as index. The experiment determined chlorogenic acid’content in different time after by LCMS,and calculated the pharmacokinetic parameters such as Cmax,Tmax,Tl/2,AUC and MRT by drug-time curve to compare the differences of pharmacokinetic.Consider the appropriate internal standard substance, plasma sample pretreatment and testing method in the methodology The half life of chlorogenic acid in superfine yinpian and traditional yinpian are 0.452±0.076 and 0.379±0.007 hour(P<0.05),the peak time of chlorogenic acid in superfine yinpian and traditional yinpian are 0.246±0.078 and 1.245±0.605 hour(P<0.01);the maximum concentration of chlorogenic acid in superfine yinpian and traditional yinpian are 1554.826±250.700 and 1558.993±243.371 ng/ml(P>0.05);the area under curve of chlorogenic acid in superfine yinpian and traditional yinpian are 1395.795±354.844 and 2603.232±589.874 ng/ml.h (P<0.01);the mean retention time of chlorogenic acid in superfine yinpian and traditional yinpian are 0.749±0.249 and 1.313±0.464 hour(P<0.01). The pharmacodynamics result show these:The MIC of honeysuckle superfine yinpian and traditional yinpian against Staphylococcus aureus are 6.25 mg/ml and 3.12mg/ml;that against E. Coli are 12.50mg/ml and 12.50mg/ml,that against Pseudomonas aeruginosa are 12.50mg/ml and 12.50mg/ml,and that against Salmonella typhi are 12.50mg/ml and 12.50mg/ml;that against Bacillus subtilis are 25.00mg/ml and 12.50mg/ml.Conclusions:1.The AUC of chlorogenic acid in superfine yinpian is less than traditional yinpian’s, with filling the rabbit with different slices of honeysuckle.The result shows that the former dosage proportion of superfine yinpian and traditional yinpian isn’t proper.2. The maximum concentration of chlorogenic acid in superfine yinpian is similar to traditional yinpian’s with filling the rabbit with different slices of honeysuckle.That shows the maximum concentration of superfine yinpian is 6 times of traditional yinpian’s3.The half life of chlorogenic acid in superfine yinpian is longer than traditional yinpian’s with filling the rabbit with different slices of honeysuckle.That shows the metabolism rate is more slowly than traditional yinpian’s.4.Honeysuckle superfine yinpian has similar antibacterial effect to traditional yinpian when the dose of superfine powder is 1/6 of Lonicera japonica waterextract.Considering pharmacokinetic parameter,that shows honeysuckle antibacterial activity may be associated with Cmax...