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Sepration Of BDMC And Its Joint Research With The New Accessories

Posted on:2015-05-09Degree:MasterType:Thesis
Country:ChinaCandidate:M YangFull Text:PDF
GTID:2284330467987933Subject:Medicinal chemistry
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Turmeric comes from zingiberceae (Curcuma longa L) plant dry rootsand its main effective components are curcumin,demethoxycurcumin andbisdemethoxyocurcumin(BDMC).Three components have broad spectrum,anti-inflammatory,anti-tumor, anti-oxidant, inhibition of plateletaggregateion, fall hematic fat aspects of pharmacological effects, of whichthe strongest activity is BDMC.On the other hand,Curcuminioids havinglow solubility, low stability and low bioavailability which would limit itsclinical application.Chitosan (CS) is non-toxic and has good biocompatibility,So it iswidely used in drug carrier,introduces the structure of hydrophilic groupreunion polyethylene glycols (PEG) preparation into PEG-CS, it canimprove the solubility and the bioavailability of free drug.Therefore, this topic attempts to isolate BDMC monomer, and use thesynthesis of new materials PEG2kD–CS50kDwith BDMC to prepare tobisdemethoxycurcumin–PEG2kD-CS50kDnanoparticles(BPSNP) to improvethe bioavailability of BDMC.This article mainly includes the followingcontents. 1.The separation and purification of BDMC.By use the columnchromatography, and through the kind and proportion of expansion agentand other influence factors of column chromatography, eventuallydetermine appropriate separation conditions are methylene chloride, ethylacetate, methanol=80:1:1, the dose of5g, column diameter ratio of15:1,flow rate of1ml/min.successfully isolated from model drug BDMCmonomer, its structure is confirmed by IR spectrum,ESI-MS spectra and1H NMR spectra, the purity of99.72%by HPLC.2.Synthesis of PEG2kD-CS50kDexcipients.Use of multi-stepsynthesis,by optimizing the synthetic route, tries to use phthalic anhydrideto chitosan amino protection of structure, again to chitosan on C6andPEG2kD after activation, respectively.and take off the protection forsynthetic target product PEG2kD-CS50kD,confirm is studied by usinginfrared spectrum.3. A preliminary study of BPSNP.BDMC prepared with syntheticmaterials PEG2kD-CS50kDinto BPSNP, measured particle size of641.4nm,Zeta potential was-29.8mV.The cumulative release percentage were(69.52±3.36)%and (72.41±0.77)%in0.1mol/L HCl solution and pH6.8PBS, respectively.There were significant differences (P <0.05) in theKa and Papp compared with the free drug,can be seen BPSNP improvedabsorption in the different intestines.The AUC is the3times of free drugsafter intragastric administration in rats,the results show that BPSNP improved the bioavailability of free drug.
Keywords/Search Tags:BDMC, separation, PEG, CS, synthesis, nanoparticles
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