Dihydroartemisinin hydroxypropyl- β-cyclodextrin inclusion complex

Using the orthogonal design method, the molar ratio, wrapping temperature and wrapping time of dihydroartemisinin (dihydroartemisinin,DHA) and hydroxypropyl- β-cyclodextrin (hydroxypropyl-β-cyclodextrin,HP-β-CD) as the investigation factors, and the wrapping yield rate and drug capacity in the package as the evaluation index.The characterization of the envelopes was prepared by infrared spectroscopy, differential scanning calorimetry, and powder X- -ray diffraction, and the feasibility of HP-β-CD coated DHA was investigated using molecular simulation techniques.The results showed that the best binding conditions: DHA and HP-β-CD feeding Moore ratio is 1 ∶ 5, binding temperature is 50℃, and binding time is 1 h.Infrared spectroscopy, differential scanning calorimetry and powder X- -ray diffraction analysis all showed that DHA formed envelopes with HP-β-CD, and molecular simulations revealed low free binding energy and high solvent accessible surface area, and HP-β-CD coated DHA was feasible and significantly improved the water solubility of DHA.The DHA-HP-β-CD binding process is feasible and provides a theoretical and experimental basis for studying the production process.

hydroxypropyl-β- cyclodextrin is a derivative of β- cyclodextrin, which has high water solubility, can reach more than 50% at room temperature, and is non-toxic and non-irritating. the us FDA has approved it as an excipient for injection.