Study Of Wuweizi Enteric Microspheres

Objective To optimize the extraction technology of effective components of Schisandra by alcohol;To optimize the preparation methods of wuweizi enteri c microsphere, and to evaluate its release behavior in vitro and its metabol ism dynamics research;To establish the method of effective component conten t determination for wuweizi microspheres and make the research of methodolo gy;To establish the fingerprint of wuweizi microspheres and Schisandra of d ifferent areas, and to evaluate the there quality as an intrinsic evaluation system.Methods Using orthogonal test method, Using the γ-schizandrin, the contents of extraction ratio as as evaluation index in the extracted solution. The f actors were inclutiong:ethanol concentration, ratio of feed.and liquid, ext raction time and extraction times;the polyacrylic acid resin (II) as the ca rrier, and using method of two phase separation, The factors were inclutiong: encapsulating rate, recovery, and appearance shape. To optimize preparation te chnology optimization method of wuweizi enteric microsphere by single facto r, and optimize the cumulative release degree in different digestion medium. at the same time, LC-MS method was used to study fruit of Chinese γ-schiza ndrin element metabolic behavior in mice.The high performance liquid chroma tography (HPLC) was used to check wuweizi microspheres of effective compon ent content determination, C18column, temperature was40℃, detection wavelen gth was220nm, mobile phase was used water-acetonitrile(gradient elution). The high performance liquid chromatography (HPLC) method was used to establ ish the fingerprint of wuweizi microspheres and fructus schisandrae of diff erent areas, C18column was used, temperature:40℃, detection wavelength was254nm.Results The best extraction technology was:the ethanol concentration:85%, ratio of feed and liquid:1:6, extraction time120min, extraction times:3, the best preparation technology of Fruit of Chinese wuweizi enteric microsphere s, solution concentration of the polyacrylic acid resin11:10%, the ratio of 0.5%gelatin solution and the proportion of liquid paraffin:1:4, the best speed:500r/min, the average encapsulating rate of three batch sample was30.2±0.8%, the accumulated release in3hours in pH6.8buffer solution reac hed95%;the research of pharmacokinetics in rat body shows:the fruit of Chi nese γ-schizandrin AUC was598.0±238. lng·h/mL, T1/2was9.3h, CL was7.74±3.44L/h/kg. The research of method of effective component content dete rmination of wuweizi microspheresshows:The linear ranges of deoxyschizandri n, schisandrin and γ-schisandrin were0.003～0.3μg,0.02～2μg and0.003～0.3μg, respectively. The average recoveries were99.40%,98.15%and98.15%, respectively.the fingerprint research of wuweizi microspheres shows that: the common peaks were appeared.of21in HPLC-DAD chromatogram, the similarit y was more than0.99in different each batch sample. And the fingerprint of different areas show:difference is bigger, the correlation of the HPLC-DAD f ingerprint of different areas was better.Conclusion The optimized process is feasible and stable, The schisandra prep aration procedure was practical and stable, and the microspheres was showed good dissolubility. The release of schisandra from microspheres could reach above95%. The method is accurate, simple and suitable for determination of deoxyschizandrin, schisandrin and γ-schisandrin in Wuweizi Microspheres.The method is simple,sensitive and accurate. it is suitable to be used to evalu ate the qualities of wuweizi Microspheres and fructus schisandrae.