New Technical Study On The Preparation Of Dexamethasone

As a steroid hormones product, Dexamethasone belongs to preganeadrenocortical hormones. Since its successful development in 1940's~1950's,it has been applied widely in the clinic for its anti-inflammation, less dosage,slight action of water and sodium retention and potassium depletion andlighten the pathological reaction of organism caused by impairing irritation.Now it becomes the important drug to cure encephaledema, shock,anaphylactic disease and inflammation. It is praised as "King ofcorticosteroids". Additionally, the series of Dexamethasone, includingDexamethasone Acetate, Dexamethasone Sodium Phosphate, are prepared forinjection, oral tablet and external use.Dexamethasone is a high-technology product and its production process iscomplicated and intermittent, involving many chemical steps. In the wholeproduction, each step can influence on the drug quality and yield, especiallyfluorination and hydrolysis reactions, which are key steps to ensure theproduct quality. With the purpose of lowering the manufacturing cost andimproving the quality of the product, this paper start from the currentproduction process of Tianjin Tianyao Pharmaceuticals Co., Ltd. and selectabove two reaction steps to optimize. The process conditions of test study aredetermined through the research of operation parameters influence (such asthe concentrations and ratios of starting materials, temperature and activator)on intermediates quality, yield and relevant technical items in Dexamethasonesynthesis as well as other factors also are taken into consideration.As for the test study is mature, the new process can be put into practicefor industrialization. This paper performs the yield, quality and operability ofthe new process examination and analysis.Based on the systemic study, it provides the basic data for Dexamethasonesynthesis test study and industrialization. Meanwhile, the optimizationconditions of new process are validated in the industrialization. Theapplication of new process improves the product quality, decreases themanufacturing cost, strengthens our product competition in the internationalmarket and obtains considerable economical and social benefits.