| dc.description.abstract | In this thesis, we listed six points to demonstrate the significance of the work (1) the identification of conformational polymorph of FormⅡ sucrose, (2) using 23 kinds of pure solvents commonly used in pharmaceutical technology in sugar screening, (3) using solid-state instrumental methods (SSNMR, SXD) to demonstrate the presence of Form II sucrose, (4) showing that the DSC peak at 150°C was the enthalpy of the solid-solid transformation between the two conformational polymorphs of sucrose crystals changing from Form II to Form I, (5) using anti-solvent (methanol) for re-crystallizing Form II sucrose, (6) investigated the influence conformational polymorphs of sucrose as an excipient in the formulation. Three important studies in this thesis were performed to improve the efficiency of the discovery and development process. Firstly, a useful engineering data bank of solubility, polymorphism, crystal habits and crystallinity by initial solvent screening for sucrose was be established and a robust, miniature solvent screening method was be introduced. Secondly, we used several instrumental methods to demonstrate the presence of conformational polymorph of FormII sucrose such as differential scanning calorimetry (DSC), solid-state NMR (SSNMR), single-crystal x-ray, diffractometer (SXD), Karl Fischer titrimetry (KF) ,and refractometer sensor. Thirdly, we investigated the influence of sucrose in formulation as an excipient. We expect that FormⅠand FormⅡ sucrose crystals will affect the drug release rate. | en_US |