| Objeetive:Through the formula of heat grains, clinical application and basic pharmacodynamics research, to explore the therapeutic effect of heat-clearing and foreign particles are fever, further verify the above particle in qingrejiedu, cool blood and throat, etc. In order to further study heat particle metabolic processes in the body, with baicalin as the research object, research of baicalin in animal blood drug concentration in the body dynamic change and the law, help to elucidate the pharmacodynamics of hot particles provide basis for foundation, the compatibility of the law, and to better guide clinical drug use.Method:Pharmacodynamic study:Uses the rabbit to hot experiment, xylene, fresh egg qing inflammatory inflammatory experiment, concentrated ammonia induced cough and phenol red tag expectorant experiment, cell phagocytosis in mice, E-wreath experiment in mice, the mice used in the determination of serum hemolysin level, animals can be divided into two dose groups, negative control group and positive control group at the same time, the observed heat particles of antipyretic, anti-inflammatory, antitussive, expectorant, immune function; By Oxford cup method and double dilution method was developed for the determination of heat particles bacteriostasis and minimum bacteriostatic concentration, observation of hot particles in vitro antibacterial effect. Pharmacokinetic study:Wistar rats only6, dosing of fasting water12h, weighing dosing, prior to delivery (0h) and10min after the treatment,30min,1h,2h,3h,4h,5h,6h,8h,10h0.5ml, orbital angular vein blood of rats in heparinization Ep tube,3.5x103r. centrifugal10 min min-1. Get rid of0.2ml plasma proteins, blood drug concentration was determined by HPLC.Result:Pharmacodynamic study:Heat granule on milk to rabbit fever fever has obvious antifebrile action, on experimental inflammatory swelling, also showed good anti-inflammatory effects; Cough caused by chemical stimulation has obvious inhibitory effect, prolong cough incubation period, and has a good expectorant effect; Experiment results show that heat granule can obviously strengthen the function of phagocytes of mice, has obvious enhancement effect on cellular immunity; In vitro antibacterial test results show that the heat granule on staphylococcus aureus, hay bacillus coli, gambogic micrococcus gram positive bacteria and ordinary proteus, tzu chi’s blessing hayes bacteria gram negative bacteria has certain inhibitory effect. Pharmacokinetic study:Results show that when the rats given heat granule (after10g/kg), blood drug concentration-time curve of baicalin appear obvious bimodal phenomenon, rapid emergence in10～30m in the first peak. When baicalin instantly absorbed through the stomach and duodenum after reduction, in the small intestine blood drug concentration and increased gradually during the transfer process, in3～4h second peak. Qingre Granule in line with the second chamber inside the particle model, the main pharmacokinetic parameters for the t1/instant6.21min, Ke:0.011/min, C (Max):3.01mu g/mL, AUC:883.02mu g· min/mL. Changes from drug by speculation, baicalin blood drug concentration in the is the un-ionized absorption in the stomach, the second peak is scutellaria baicalin or its glucoside yuan transformation caused by absorption in the intestine.Conclusion:Pharmacodynamics studies suggest heat granule has obvious anti-inflammatory, antipyretic, antitussive, expectorant, strengthen the function of phagocyte, and is has the certain enhancement effect on cellular immunity, to staphylococcus aureus, hay bacillus coli, gambogic micrococcus gram-positive bacteria as well as ordinary proteus, tzu chi’s blessing hayes bacteria gram negative bacteria has certain inhibitory effect. Heat particles contain baicalin plasma half-life of about386min. |
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