Water Soluble Analgetic
Water Soluble Analgetic
Tech Area / Field
- BIO-CGM/Cytology, Genetics and Molecular Biology/Biotechnology
- MED-DRG/Drug Discovery/Medicine
3 Approved without Funding
Biysk Oleum Factory, Russia, Altay reg., Biysk
- Siberian Branch of RAS / Novosibirsk Institute of Organic Chemistry, Russia, Novosibirsk reg., Novosibirsk\nCombiotech Ltd., Russia, Moscow
Project summaryProblem actuality.
Researchers in the Held of pharmacology arc actively working over super-aspirin problem, being pain and inflammation reliever as aspirin, but having no concurrent harmful effect. Attention is paid to water-soluble forms of analgesics. At present water-soluble analgesics (WA) are not made in Russia. The price of imported WA is on the order of magnitude higher than the same of Russian aspirin and imported WA is inaccessible to most of the people.
Weapons specialists of Biysk Oleum Plant together with chemists and pharmacologists have conducted preliminary development of WA , conventionally called Aspitrin, and the process of its production. Synthesis is carried out on the base of TRISamine (2-amino-2 (oxymethyl)-propanediol-l,3) and aspirin (acetylsalicylic acid).
Aspitrin pharmacopoeia substance is VFS № 42-2561-95, its preliminary check in clinical conditions showed good results.
Besides being pain and inflammation reliever, Aspitrin has anti-aggregate properties too and may be recommended for insults, ischemia and high blood pressure prophylaxis.
Unlike aspirin, aspitrln does not irritate the mucosa of gastro-intestinal tract that permits to use it by patients suffering from gastritis, ulcer disease, colitis.
There are two publications on composition production on the base of TRISamine and aspirin. We have no information on their commercialization. In our opinion there are two reasons hindering the commercial production of the compositions: significant process costs when manufacturing TRISamine and synthesizing aspitrin.
TRISamine is produced by two methods. According to the first method TRISamine is made by hydrogen reduction of the synthesis product of nitromethane and formalin solution in the autoclave at pressure 6 to 10 kg-m/cm2 (0,6-1,0 MPa) in the presence of Raney nickel catalyst and to the second method via its electro-chemical reduction . The both methods are technologically complicated. Main and auxiliary raw material costs are essential when synthesizing aspitrin. Thus calculated aspitrin cost made according to these processes is over 30 USD/kg.
The project purpose is the development of more economical water-soluble analgesic process, construction of a pilot plant, production of aspitrin pilot batch to study the market and in the future to create peaceful production at BOZ conversion facilities.
Tasks - the following problems are solved to achieve the stated purposes:
- increase in nitromethane and TRISamine production efficiency using new catalysts of "palladium on carbon" type with TRISamine yield increase;
- creation of the original process equipment implementation;
- modification of aspitrin synthesis, reduction in process cost.
Development of new production method of required quality nitromethane. Based on this method it is possible in the future to prepare other nitroalkanes (nitroethane, nitropropane), being raw material to make pharmaceutical preparations. Creation of fundamentally new process of nitro-compounds reduction at air pressure, that permits to adapt process principles to other numerous ways of pharmaceutical drug production.
Evaluation of theoretical dependence of reactive components concentration on the reaction time and distance from the catalyst surface.
Realization of the project allows to reduce aspitrin cost by 30-35% and bring it to 17 to 20 USD/Kg. In this case aspitrin becomes accessible to most of Russian people.
The Russian market demand of various forms aspitrin (domestic and foreign) is about 700 t/yr.
With our assumption aspitrin can occupy 10-15% Russian analgesics market, 70 to 100 t/yr for the first 5 years, promoting health prevention and lifetime increase.
We are ready to co-operate with you on ISTC project mb 458.
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