Preparation Of CM-zein And Its Applied Research On Pharmaceutics

Zein is a strongly hydrophobic natural polymeric material. In order to enhance itshydrophilic, we had modified the Zein by cardiomyopathy and obtain the method ofpreparing CM-Zein by increasing the number of carboxyl in the molecular chain ofZein. We found that CM-Zein has solubility characteristics of enteric by its structuralcharacterization and determination of physical and chemical properties. According tothis feature, the aspirin enteric-coated tablet was prepared, and its the vitro releasebehavior and the in vivo pharmacokinetics characteristics was investigated.In this paper, we had studied the method of preparing CM-Zein by the single factor testand orthogonal experimental design, taking the content of carboxymethyl and the yieldas evaluation. And the optimum conditions for preparation of CM-Zein: the feedingamount of Zein and the sodium monochloroacetate by mass ratio of1:0.75, taking75%ethanol as solvent, and adding the amount of Zein’s10times, adjusting the pH of9.5, reacting for8hours at temperature of65℃.The chemical structure of CM-Zein was characterized by IR, GPC analysis, thermalanalysis and potentiometric analysis. And the results proved Zein had graftedcarboxymethyl, and there were no break and obvious changes on molecule skeleton buthad great changes in the Zeta potential of Zein. By examining the properties of theCM-Zein draw obtained in our laboratory, the CM-Zein has better hydrophily and canbe dissolved in water of about pH4.5compared to Zein. The absorption moist,inherent viscosity and strong intestinal adhesion of CM-Zein had also been examinated.Based on the above results, CM-Zein can be used as enteric-solube material.Aspirin enteric-coated tablets were prepared with aspirin as a model drug and CM-Zeinas adjunct, the in vitro release of the single factor was invested. The results showed that the dry granulation mixed accessories tablet, select drug loading was33.3%, andthe6±1kg hardness prepared aspirin enteric-coated tablet was better. Compared tocommercialise enteric-coated tablets of aspirin in vitro release, the results show thatboth of them are almost never released in the artificial gastric juice, and can bereleased completely within2hours artificial intestinal fluid.Salicylic acid in rat plasma samples was determined by high performance liquidchromatography (HPLC), and the result is accurate and reliable. The characteristics ofthe plasma concentration of aspirin were complied with enteric features after rats werehomemade aspirin enteric-coated tablets. The Cmaxwas reduced and Tpeak wasextended greatly, so it can reduce the gastric irritation of aspirin and extend the time ofdrug action and reduce drug administration times.