Research Of Preparation And Processing About Nano-artemisinin And Artemisinin Lyophilized Powders

The artemisinin is an antimalarial drug, with quality of quick-acting, efficient and low toxicity. The artemisinin as antimalarial drug has been assigned safe and effective by WHO. however, artemisinin insoluble in water and quality unsteady, which limit the clinical application.Supercritical fluid technology is a new method for preparation of ultra-fine powder materials in recent years. The artemisinin ultrafine powders prepared by RESS has many disadvantages, such as small particles, regular granularity, The inner portion of particles is not destroyed and so on. In this paper, by the preparation of artemisinin ultrafine powders used RESS technology. The parameters such as temperature, pressure, nozzle diameter in the process of artemisinin ultrafine powders RESS were examined, micro-devices of the rapid expansion of supercritical solution technology was optimized, and the rules of the influence on particle shape, size and size distribution for each parameters were mastered. The orthogonal experiment has determined the best preparation condition: Dissolves the cauldron temperature 62℃, Dissolves the cauldron Pressure 25MPa, crystallizes the cauldron temperature 45℃, spray nozzle aperture 1000nm. The artemisinin ultrafine powders with average size of 550nm were prepared. After the infrared spectrum examination, theLC/MS/MS examination, the DSC examination, the X-Ray test, the artemisinin bulk density research discovered that, The artemisinin ultrafine powders functional group structure have not change, its chemical property have not had the change; the molecular structure of artemisinin ultrafine powders has not changed; the body crystallinity of artemisinin ultrafine powders had to be lower than the primitive artemisinin is far the artemisinin ultrafine powders particle size changes small has caused the crystal structure change; The artemisinin ultrafine powders bulk density is primitive artemisinin sample bulk density 4.33 times.Cyclodextrins are cyclic oligosaccharides. The three-dimensional structure forms a truncated cone and Provides a cavity, which Presents a cavity with the appropriate size to accommodate another molecule, thus forming an inclusion compound through host—guest interactions.2-hydroxypropyl-β-cyclodextrin(HP-β-CD) is a derivation ofβ-cyclodextrin and has been already approved as oral medical supple materials by the FDA and SFDA. The FDA also warrants HP-β-CD in intravenous administration.In this article, the artemisinin lyophilized powders were prepared with filling agent of HP-β-CD and mannitol, the structure and morphology of artemisinin ultrafine powders and lyophilized powders were studied by AFM, DSC and XRD methods. The results: artemisinin ultrafine powders/HP-β-CD inclusion complex was formed. The condition of preparation artemisinin lyophilized powders is: The best mole ratio of artemisinin ultrafine powders and HP-β-CD is 1:6; the artemisinin lyophilized powders were prepared with filling agent of 5% HP-β-CD and 5% mannitol. The artemisinin lyophilized powders have good water solubility and it can have practical potentiality on new dosage form of artemisinin.