The Study Of The Active Substance Of Alpinia Galangal 1'-acetoxychavicol Acetate (ACA) Injection

ACA is a natural compounds which is separated and purified from the rhizomes of Alpinia galanga(L.)Swartz. The chemical name is 1'-acetoxychavicol acetate. ACA as a Rev protein inhibitor is a significant activity against HIV-1 infection. ACA can block the fusion protein to transport from nucleus to cytoplasm and has a high level of security. Besides, ACA has anti-tumor, antioxidant and anti-cancer, anti-ulcer, anti-bacterial and the alike biological activity. For its reliable anti-HIV function and low toxicity, ACA takes on a good future of development. ACA is potential to became a new class I anti-HIV drug with independent intellectual property.Firstly, by using of complexation, the solubility of ACA can reach 10mg·mL-1 above. Based on this, the excipients of ACA injection were screened. The time of different prescriptions of ACA injection diluted with normal saline solution forming crystals and the thermal stability of ACA injection were investigated. We screened the type and amount of acid substances and complexation. For further improving prescription stability, we tried to add antioxidants and cyclodextrins to ACA injection. We decided the formulation which make up of ethanol, surfactant A and acid A and the prescription and preparation of ACA injection.Quality standard and stability make up a main part in developing new drugs. In the study, a high performance liquid chromatographic (HPLC) method was developed for the determination of ACA and its related substance. And the Quality standard was drafted and explained. The establishment of quality standard could provide scientific basis for the production of ACA injection. After that, the stability of ACA injection influenced by heat and light was inspected and elementary stability, speedup stability and long-term stability inspections were carried on as well. The results showed that heat promoted the degradation of ACA injection. The content of ACA injection was decreased about 8% and ACA related substances were increased significantly under room temperature for 12 months. The shelf life of ACA injection at 25℃was 1.2y by constant-temperature experiment. So, ACA injection should be protected from light and kept at a low temperature. At last, the degradation products of ACA injection were carried on. The results showed that ACA has low stability in strong acid, strong base or strong oxidizing, high-temperature environment, especially, in strong base.The established quality controlling method in this study was simple, reliable and specific method with good reproducibility, and can be used for the quality control of ACA injection. Stability research provided scientific reference for manufactural process, packaging, store conditions. The test of degradability of injection provided rich data sources for ACA new forms development in the future.