Extraction And Capsules Preparation Of Betulinic Acid

The study was based on the results of pharmacological screening. The effective component that can resist cancer in Spine Date Seed was studied. We gained a monomer by extraction, isolation, refinement and purification with the techniques and methods of chemistry. This monomer was identified as betulinic acid after being measured by ultraviolet spectrophotometry(UV), infrared spectrophotometry(IR), high performance liquid chromatography(HPLC), thin layer chromatography(TLC) and compared with references. In the course of our study, we used the method of single factor design and the method of orthogonal design to screen out our method of extracting, isolating, refining and purifying betulinc acid. Finally, the best extraction condition was 3 times 95% ethanol reflued 3 times and every time was 1 tours. The selected technique was proved to be stable and adoptd by enlarged experiment as well. In addition, high performance liquid chromatography-evaporative light scattering detector(HPLC-ELSD) method for the evaluation betulinic acid extracted by ourselves was built. At the same time, the preliminary stability of betulinic acid has been finished.Betulinic acid is water insoluble that makes its dissolution and absorption effected in stomach and intestines. In other words, the character leads to a low bioavailability and inferior curative effect. It was indicated in this paper that the dissolution of betulinic acid was improved through solid dispersion technique. Various parameters influencing the quality of betulinic acid have also been discussed. At last, betulinic acid solid dispersions were prepared by solvent methods, in which polyvinylpyrrolidone(PVP) was carrier and ethanol was solvent and the ration of drug-carrier was 1:5. Besides, differential thermal analysis(DTA) and IR were used to determine the status of betulinic acid in carriers, and dissolution characteristics in water were studied. It was showed that betulinic acid was amorphous in solid dispersions and its dissolution was improved remarkably. For the purpose of making betulinic acid solid dispersions into capsules, we did comprehensive research in the screening of formulation, optimizing of technique and pharmaceutical characteristics. The capsules release model of betulinic acid solid dispersion was in keeping with Weibull distribution. Finally, the method of determination the in vitro dissolution of capsules and evaluation the quality of capsules were established. Moreover, the preliminary stability of capsules has been completed.In conclusion, the initial study from extraction to preparation for betulinic acid has been accomplished. The quality of betulinic acid and its capsules were stable in the conditions of strong light, high temperature, high humidity and accelerated test and long-term test at present.