What is Pharmaceutical Intermediate
Pharmaceutical intermediates, as the name suggests, are intermediate products or raw materials used to produce medicines, and can also be understood as pharmaceutical precursors. To define them clearly, you must first understand what medicines are, the composition of medicines, and the source of medicines.
What is medicine?
Medicines are chemical or biological products composed of chemical elements used to regulate people's body functions, improve people's quality of life, and remove pain.
Medicines or Drugs can be divided into central nervous system drugs (such as sedative-hypnotics, antipsychotics, central stimulants, etc.), peripheral nerve drugs (such as anticholinergics, adrenergic drugs, local anesthetics, etc.), circulatory Systemic drugs (such as drugs acting on ion channels, drugs acting on receptors, enzyme inhibitors, etc.), digestive system drugs, antipyretic analgesics, antitumor drugs, antibiotics, hormones, etc.
Drugs can be divided into injections, tablets, capsules, granules and other forms of administration from different routes of administration. Each form of administration has its own specific advantages. Due to the rapid distribution and absorption of the drug, it avoids the drug passing through the stomach, which may cause gastric acid destruction, as well as the first-pass effect of the liver, and enhances the stability of the drug. For some drugs that are not chemically stable, this dosage form is the first choice. , such as vaccines, antibiotics, etc. Tablets, which are easy to transport, convenient to take, enhance patient compliance, and are the patient's preferred mode of administration. Capsules, granules, etc. have their corresponding advantages, some are to solve the problem of drug absorption, and some are convenient for children to take.
Composition of medicine
Medicines or Drugs are composed of active ingredients (API) and pharmaceutical excipients. Thanks to the development of chemistry, there are various active ingredients, including inorganic substances, organic substances, natural products, genetically engineered drugs, etc. The active ingredients can act on specific drugs. The target has a certain curative effect, that is, what we call the effect of drugs on people, also known as PD. Pharmaceutical excipients are good partners of active pharmaceutical ingredients and the carrier of active pharmaceutical ingredients. In layman's terms, they are the nanny of active pharmaceutical ingredients, which can make the drug exert the best effect, improve the exposure of the drug in the body, and enhance the stability of the drug. To facilitate the storage of medicines, etc.
Origin of medicine
The discovery of drugs is both accidental and inevitable. The first antibiotic penicillin discovered in 1928 was discovered by Fleming by accident, but the development of modern medicinal chemistry has made the discovery of drugs a necessity. Pharmacologists Through countless screening experiments, the optimal active ingredients that can act on a specific target are obtained. The active ingredients can be inorganic substances, organic substances, natural products, etc. Of course, inorganic substances and organic substances are not directly obtained in nature like natural products. Thanks to the development of computational chemistry, analytical chemistry and other disciplines, the target structure of active ingredients can be designed with computer aids, and then by the hands of chemists, through the The knowledge of chemical knowledge is gradually synthesized, which is the intersection of multiple disciplines and the crystallization of the wisdom of countless chemists.
Pharmaceutical active ingredients (API) are like a mobile phone. Its display panel, built-in chip, communication antenna, etc. need to be assembled one by one. Pharmaceutical intermediates are display panels, chips and antennas, which are precursors of active pharmaceutical ingredients. , are some chemical raw materials or chemical products used in the pharmaceutical synthesis process. This kind of chemical product does not require a production license for drugs, and can be produced in ordinary chemical plants. As long as it reaches some levels, it can be used for the synthesis of drugs.
Pharmaceutical intermediates can be used in research and development, as well as in the production of drugs. They are the bricks of buildings, the steel bars of buildings, and the oil, salt, sauce and vinegar in vegetables. It is because of their existence that medicinal chemists can be like Chefs make delicious dishes.​
The prospect of pharmaceutical intermediates
Medicine is a special commodity with all the characteristics of fine chemicals. The development of medicine is inseparable from intermediates, which are the basis for the development of medicine. Pharmaceutical intermediates are the general term for all the compounds in the synthesis and manufacture of pharmaceuticals, pesticides, and veterinary drugs before they become drugs. Fine chemicals, including organic pharmaceutical intermediates, are an important part of the chemical industry, and their level of development is a sign of a country's chemical modernization level. Over the years, the fine chemical industry has been the focus of investment and fierce competition from countries all over the world. The global pharmaceutical industry has thus made unprecedented progress, and the world pharmaceutical market continues to exhibit high growth characteristics. Due to the characteristics of high investment and high benefit in the research and development of new drugs, in order to maintain their high growth rate, major pharmaceutical companies increasingly focus on the research and development of new drugs, new drug products and their market development. Therefore, the development of pharmaceutical intermediates has broad market prospects.
Main applications of pharmaceutical intermediates
The research on pharmaceutical intermediates is mainly reflected in the synthesis of heterocyclic compounds, fluorine-containing compounds, chiral compounds, biological compounds, etc.
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(1) Heterocyclic compounds, which are widely used in medicines, pesticides and veterinary drugs and intermediates, are mostly the parent (nucleus). At present, losartan potassium tablets, amlodipine, etc., which are widely used in clinical treatment of hypertension, are all heterocyclic compounds.
(2) Fluorine-containing compounds, introducing new elements into pharmaceutical intermediates for modification, the most successful should be fluorine. Organic fluorine-containing compounds have broad application prospects in medicine. At present, the best-selling anti-infective drug on the market, fluoxetine, is a fluorine-containing organic compound. In addition, fluorine anesthetics such as halothane, penthrane, ethrane, isoflurane, etc. are all anesthesia. Highly potent, non-post-anaesthetic organofluoride. 5-Fluorouracil, fluoxymesterone (halotestin) and others have been used to treat cancer, haloperidol for sedatives, sulindac for rheumatoid arthritis, and hydroflumethizaide Used as a diuretic, etc.
(3) Chiral compounds. On the basis of stereochemistry, chiral compounds are obtained by asymmetric synthesis or resolution. Asymmetric synthesis began in 1966. The application of asymmetric hydrogenation, asymmetric catalysis and other reactions has made the directional reaction yield as high as 93%. Many intermediates such as Viagra drugs are obtained through asymmetric synthesis.
(4) Biological compounds. The key research direction of modern medical biotechnology is the application of DNA recombination technology, cell engineering technology and enzyme engineering technology to study and treat cardiovascular diseases, diabetes, hepatitis, tumors, anti-infection, anti-aging and other drugs, as well as the application of modern biotechnology to transform the traditional pharmaceutical industry.
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Pharmaceutical intermediate engineering technology is an important means to change the level of pharmaceutical intermediates, and it is also the key to the development of pharmaceutical intermediates, so it is imperative to carry out research on it.