The so-called pharmaceutical intermediates are actually some chemical raw materials or chemical products used in the process of pharmaceutical synthesis. This chemical product can be produced in ordinary chemical plants without a drug production license. As long as it reaches a certain level, it can be used for the synthesis of drugs.
brief introduction
China needs more than 2000 kinds of chemical supporting raw materials and intermediates every year, with a demand of more than 2.5 million tons. After more than 30 years of development, the chemical raw materials and intermediates required by China's pharmaceutical production can basically be matched, and only a small part needs to be imported. Moreover, because China is rich in resources and the price of raw materials is low, many intermediates have been exported in large quantities. So, what are the development opportunities in the field of pharmaceutical intermediates in China?
Increased demand
our country β－ After nearly 50 years of development, lactam antibiotics have formed a complete production system. Almost all in 2012 β－ Lactam antibiotics (except those within the patent period) can be produced in China, and the cost is very low. The output of penicillin ranks first in the world, and a large number of them are exported to the international market; Cephalosporins are basically self-sufficient, and some of them can be exported.
In 2012, and β－ All the intermediates supporting lactam antibiotics can be produced by our country. Except that the mother nucleus 7-ACA and 7-ADCA of semi synthetic antibiotics need to be partially imported, all side chain intermediates can be produced and exported in large quantities.
with β－ Take phenylacetic acid, the main supporting intermediate of lactam antibiotics, as an example. There are nearly 30 phenylacetic acid manufacturers in China, with a total annual production capacity of about 20000 tons. However, most of the enterprises are relatively small, with the largest annual output of 2000 tons, and most of the others produce hundreds of tons. In 2003, the total domestic demand for phenylacetic acid was about 14000 tons, and the consumption structure was: Penicillin G accounted for 85%, other medicines for 4%, spices for 7%, pesticides and other fields for 4%.
With the development of domestic perfume, medicine, pesticide and other industries, the demand for phenylacetic acid will further increase. It is estimated that by 2005, China's pharmaceutical industry will consume about 14000 tons of phenylacetic acid, the pesticide industry will consume 500 tons, and the spice industry will consume about 2000 tons. Coupled with the consumption in other fields, it is estimated that the total domestic demand for phenylacetic acid will reach 18000 tons in 2005.
Fluorinated pyridine
Fluorinated pyridine intermediates become hot spots
As of 2012, quinolone antibiotics that have been developed and put into mass production in China mainly include norfloxacin, ciprofloxacin, ofloxacin, enoxacin, lomefloxacin, fleroxacin, etc. Among them, the production of norfloxacin, ciprofloxacin and ofloxacin is the largest, accounting for about 98% of the total domestic production of fluoroquinolones.
Quinolones are generally synthesized from fluoroquinoline compounds synthesized from fluorobenzene rings and condensed with piperazine (or methylpiperazine). Due to the rich reserves of fluorite, China is one of the countries with the largest output of fluorinated drugs and intermediates in the world, and more than 80% of fluorinated intermediates are supplied for export. On the whole, fluorobenzene intermediates developed earlier in China, and the production capacity is generally surplus; Trifluoromethyl intermediates developed late and rapidly; For heterocyclic aromatic compounds, especially fluorinated pyridines, only a few research institutions and manufacturers in China have the synthesis technology of fluorinated pyridine intermediates. Therefore, fluorinated pyridine intermediates will become one of the main directions of domestic fluorinated intermediates research and development in the next few years.
Large gap
China has become the largest producer of antipyretics and analgesics in the world, with the output of aspirin, paracetamol, analgin and other varieties exceeding 10000 tons, and the output of phenacetin, aminopyrine, antipyrine and other varieties exceeding 1000 tons. At present, the output of antipyretic analgesics in China has increased rapidly, and it is expected to increase by about 8% in the future. The production of intermediates for antipyretic analgesics is large, and there are many manufacturers. With the growth of antipyretic analgesics, mesosomes have also achieved considerable development.
In 2003, domestic consumption of paracetamol increased rapidly, and exports also showed a rapid growth momentum. The export volume was 28163 tons, with a year-on-year increase of about twice. By the first half of 2004, although its export growth slowed down, it still increased. From January to May 2004, the export volume of paracetamol was 12501 tons, slightly higher than that of the same period last year. Paracetamol is an important intermediate in the synthesis of paracetamol, which grows rapidly. The annual output of paracetamol in China is 32000 tons. It is estimated that by 2005, the domestic output of paracetamol will reach more than 50000 tons, and the pharmaceutical industry will consume 45000 tons of paracetamol. Coupled with the application in other fields, the total demand for paracetamol in 2005 was about 50000 tons, with a large market gap and broad prospects for development and utilization.
Production characteristics
Looking at the whole industry, at present, the production of pharmaceutical intermediates in China has six characteristics:
First, most of the production enterprises are private enterprises, with flexible operation and small investment scale, basically between millions and 120 million yuan; Second, the geographical distribution of production enterprises is relatively concentrated, mainly in areas centered on Taizhou, Zhejiang and Jintan, Jiangsu; Third, with the increasing attention of the state to environmental protection issues, the pressure on production enterprises to build environmental protection treatment facilities has increased; Fourth, the product update speed is fast. After a product is generally launched for 3-5 years, its profit margin will decline significantly, which forces enterprises to constantly develop new products or constantly improve production processes in order to maintain high production profits; Fifth, because the production profit of pharmaceutical intermediates is higher than that of chemical products, and their production processes are basically the same, more and more small chemical enterprises have joined the ranks of producing pharmaceutical intermediates, resulting in increasingly fierce disordered competition in the industry; Sixth, compared with bulk drugs, the profit margin of producing intermediates is low, and the production process of bulk drugs and pharmaceutical intermediates is similar. Therefore, some enterprises have not only produced intermediates, but also used their own advantages to start producing bulk drugs.