The Brief Introduction of Aclatonium Napadisilste

Release time:2014-12-02 15:18:34 viewed:
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1.Brief Introducing the Product 
      Aclatonium napadisilate was a kind of drug as a excitomotor for digestive tract and smooth muscle,the chemical name was 2-[2-(Acetyloxy)-1-oxopropoxy]-N,N,N-trimethylethanaminium-1,5-
naphthalenedisulfonate.This product was firstly introduced into Japanese market,It could be available to many clinical diseases,Using this product could excite the stomach,intestines and the biliary tract,which lie great function on the parts of the pylorus and the vestbule in the stomach with the less function on the other parts of the digestive tract.Besides, the product could hyperfunction the movement of the end of the biliary tract, raised the inner pressure of the gall bladder, and advanced the bile to flow into the duodenum. It also enhanced the movement function in bad condition caused by cutting the vagus and morphine. When this product was used to the healthy people or people with chronic gastritis, or the patients after operation, it could do something to help to drain out the digested food in the stomach. It also could be applied to cure the abnormal function of the digestive tract such as disgusting, vomiting, inappetence, physogastry, chronic gastritis, the obstacle preventing the biliary tract from moving, the digestive tract after operation and so on.
 
2.The Related Research and Invention at China and Abroad
      In regarding to the synthesis of Aclatonium Napadisilate, We had not found any related reports at China. But there were the related statements in USP3803214,BP1336350 and USP5011973.alfa-acetoxy-alfa-methylacetic acid anhydride taked for starting material in those patent,which reacted with N,N-dimethylaminoethanol,to obtain the alfa-acetoxy-alfa-methylacetic acid dimethylaminoethyl ester It was very difficult to synthesis alfa-acetoxy-alfa-methylacetic acid anhydride and costed a lot.However,In JP54-14092 which obtained alfa-acetoxy-alfa-methylacetic acid dimethylaminoethyl ester by reacting a alfa-acetoxy-alfa-methylacetyl chloride with N,N-dimethylaminoethanol, This way reduced the cost greatly, but the synthesis,separation and purification the alfa-acetoxy-alfa-methylacetyl chloride was difficult,Meanwhile,it requested the reaction instruments with a higher level. Therefore, we improved and innovated the Synthesis technics of Aclatonium Napadisilate on the basis of  previous documents.
 
3.Technics Characteristic
      The improved technics employed a new method synthesize alfa-acetoxy-alfa-methylacetic acid dimethylaminoethyl ester in one reactor vessel, then reacting with dimethyl 1,5-naphthalenedisulfonate to obtain highly purified Aclatonium Napadisilate. This way decreased the separating process and the reacting instruments, increasing the yield of the product, reducing the production costs greatly and being more helpful for the industrial production.
 
4.The improved process as follows
    Lactic acid taked for starting material,reacted with acetyl chloride to obtain alfa-acetoxy-alfa-methylacetic acid,the excessive acetyl chloride was removed under reduced pressure, the residue reacted with thionyl chloride to obtain alfa-acetoxy-alfa-methylacetic acid dimethylaminoethyl ester as crude products, then extracting, separating, drying and contracting to obtain Aclatonium Napadisilate with highly purity.The improved Synthesis route obviously shortened and decreased the separating process. It was easy to manipulate with the mildly reacting condition, easy controlling, easily getting the raw materials, and the product with high purity. Its purity could reach 99.5% according to the analysis of High Performance Liquid Chromatography.
 
5.The Procedure of Research and Invention
      Our company had finished the Synthesis technics, structure certification and quality research of the medical material and its capsule of Aclatonium Napadisilate. We gave a systematic research to the product��s quality standard such as character,identification, inspectation, dissolution rate, the related compounds and assay,the content in the light of CP2005 requirement for the quality of the medical material and capsule.So we made up the corresponding standard of quality controlling according to the experiment results. The results showed that the purity of the medical material from this technics could reach above 99.5%, related material less than 0.5%, and other standard of physics and chemistry being in line with the documents'reports. Besides, we were dealing with the research of the stability. So far we had finished the inspectation of stability for the product being tested as long as 12 months. The results showed us this product was stable under the room temperature condition, and the long-time experiment was proceeding. At the same time, the related patent application(CN1948271) and administration protection are application.