| Ligustilide (LIG) is the main effective component in Angelica sinensis and Ligusticum chuanxiong. Previous studies had shown that LIG had significant pharmacological effects on cerebral blood vessels, the general circulatory system and immune system. LIG in the medicinal materials has two configurations, Z-ligustilide (Z-LIG) and E-ligustilide (E-LIG). Z-LIG is the main configuration. However, since LIG has a poor stability, it is very difficult to prepare and preserve it. Therefore, the study of LIG has been limited and so far is not comprehensive and systematic. In this thesis, we seek solutions for these problems. We systematically extract and isolate LIG in Angelica sinensis volatile oil (ASVO), and discovered a new isolation method of LIG that is suitable for industrial production. A patent has been granted for this new isolation method, which produces high purity LIG that could be used as the standard and also the raw material for a new medicine in first category. We also tried to increase the yield of synthesis of LIG but the yield was too low for larger scale industrial production. In the second series of experiments we characterized the physical and chemical properties as well as the stability of LIG systematically based on the high purity LIG. We also searched for specific stabilizer or any factors that could increase the stability of LIG. Based on these experiments we developed the highly stable LIG which could be used as the standard in the industrial production. Furthermore, we developed cyclodextrin (CD) inclusion complex-based and micro-emulsion (ME) of LIG preparations, with enhanced stability of LIG in both preparations, laying the foundation for the development of different LIG preparations. Finally we studied the acute toxicity of LIG, which was found to be low and complied with the safety requirement of new medicine. Therefore, LIG has good potential to be developed into a new first category medicine in the future. |
