Studys On Fructus Gardenia Antidepressant Active Site And Preparation Of Microspheres

Fructus gardenia is the dry ripe fruit of Mountain gardenia Rubiaceae, cold-natured, bitter in taste, innocuity, with the function of reducing fire except vexed, clearing away heat evil and promoting diuresis, cooling blood eliminating stasis to activate blood circulation. The drug is one piece of the 2010 edition of China pharmacopoeia, it is mainly used for treat fever upset, acute icteric hepatitis, cystitis, conjunctival congestion score pain, upper gastrointestinal hemorrhage and partly to bleed, bruised. At present the pharmacological research of fructus gardenia is increasing, main is concentrated in resistance to asthma action, anti-inflammatory analgesic action, cholaneresis hepatoprotective effect, antiviral effect and the function of nervous system etc. The early experiment proofed the ethanol extract of fructus gardenia has antidepressant activities. However ,the geniposide which is the active of fructus gardenia the feature of the short of half-life.So this subject adopts ethanol refluxing extraction geniposide, uses the macroporous adsorption resin in purification, And through the pharmacodynamics experiment verify the extract of fructus gardenia antidepressant effect, make it into microspheres through method of spray drying. In order to extend its half-life, improve the bioavailability, better to play its curative effect.Objective:Research the best extraction and purification technology of fructus gardenia antidepressant active site, and prepare it into microspheres.Methods:With the cumulative swimming fixed time as the assessment index, to optimize active fraction of Gardenia by mice depressed model. The best extraction technology of fructus gardenia was optimized by L₉(3⁴) orthogonal experiment with the anointed rate and geniposide content as the assessment index, by the method of HPLC to survey the content of geniposide .To optimized the best purification technology, using the method of macroporous adsorption resin of fructus gardenia coarse extracts of purification, through of macroporous adsorption resin type, adsorption speed, adsorption time, elution concentration, elution speed and volume of use elution as the assessment index. By spray drying microspheres are prepared, the best carrier material is determined by single factor experiment, the effect of drugs than with carrier material, inlet temperature, outlet temperature, feed flow rate on the degree of encapsulated efficiency, yield, the envelope yield are investigated by orthogonal experiment, by which the optimum Preparation Technology is determined. Meanwhile, check the form of microspheres, particle diameter and distribution, burst effect,and by means of measuring the release degrees In vitro,to preliminary study the fructus gardenia antidepressant active site microspheres in Drug delivering mechanism.Results:60% ethanol extract of fructus gardenia have apparente anti- depression effect. The best extraction technology of fructus gardenia is: add 6 times of 60% ethanol solution, extract three times, each time 1h; The purification technology of geniposide is: the type of macroporous resin is AB-8, the rate of uploading is 2.0mL/min, the amount of uploading is 2BV, the concentration of uploading is 0.25g crude drug /ml of fructus gardenia extracting solution, adsorb 1h, wash with 5BV water for eluting impurity, then used 6BV 40% ethanol as eluent, the rate of elution was 3.0mL/min. the method of prepare microsphere is Spray drying .The best technology is :the ratio of the drugs and the carrier material is 1:, 130℃is intake airflow temperature and extake airflow temperature is 90℃, the rate of sample injection is 300ml/h. the release behavior of geniposide of anti-depression active site in microsphere is agree with higuchi model.Conclusion:The process is simple and reasonable, and suitable for big industrial production.