In the modern pharmaceutical industry, pharmaceutical intermediates are an important part of drug synthesis, they are usually in a stage of the synthesis process of apis, or are the precursor compounds of the final pharmaceutical product. Because the quality of the intermediate directly affects the quality and safety of the final product, the detection of pharmaceutical intermediates has a crucial role.
First, the detection of pharmaceutical intermediates
1. Purity detection: This is the most basic item in the detection of pharmaceutical intermediates, usually using high performance liquid chromatography (HPLC), gas chromatography (GC) and other technologies. Through these technologies, it is possible to accurately understand whether the intermediate contains impurities such as unreacted raw materials, by-products, decomposition products, and their content.
2. Structural identification: It is crucial to ensure that the structure of pharmaceutical intermediates is correct. This is usually achieved through techniques such as nuclear magnetic resonance (NMR), infrared spectroscopy (IR), and mass spectrometry (MS). These techniques can help researchers verify the chemical structure and characteristics of intermediates.
3. Detection of related substances: In addition to purity and structure identification, it is also necessary to detect related substances in pharmaceutical intermediates. These may be compounds with similar structures or impurities with potential biological activity. The detection of related substances also needs to rely on HPLC, GC and other technologies.
4. Physical property test: the physical properties of the intermediate, such as melting point, boiling point, solubility, etc., also need to be tested, which has important guiding significance for subsequent drug preparations and storage.
Here are some commonly used detection techniques:
1. High performance liquid chromatography (HPLC) : It is a technology used to separate and determine various components in intermediates, especially for the detection of polar compounds. It can be used to determine purity, related substances, impurities, etc.
2. Gas chromatography (GC) : suitable for the analysis of volatile and heat stable intermediates. GC is often used to determine residual organic solvents and low molecular weight impurities.
3. Mass spectrometry (MS) : Mass spectrometry can provide molecular quality and structure information, often used in conjunction with chromatography techniques (such as HPLC-MS, GC-MS) for qualitative and quantitative analysis of intermediates.
4. Nuclear magnetic resonance (NMR) : NMR can provide detailed molecular structure information of intermediates, including molecular skeleton, functional groups and their relative positions. It is often used to confirm the structure of intermediates.
5. Infrared spectroscopy (IR) : IR can analyze the types of functional groups in intermediates and is a fast method for structural identification.
6. Ultraviolet-visible spectroscopy (UV-Vis) : By determining the absorption of intermediates in the ultraviolet or visible region, it can be used for qualitative and quantitative analysis of some intermediates with specific absorption characteristics.
7. Amino acid analyzer: If the intermediate is a peptide, an amino acid analyzer can be used to determine its amino acid composition and content.
8. Elemental analysis: Used to determine the exact content of each element (such as C, H, N) in the intermediate, which helps to verify the molecular formula.
9. X-ray single crystal diffraction: When very precise information about the structure of the intermediate is required, X-ray single crystal diffraction can be used to determine its three-dimensional crystal structure.
10. Melting point determination: By determining the melting point of the intermediate, its purity can be quickly assessed and different compounds can be identified.
11. Solubility test: By measuring the solubility of the intermediate in different solvents, its physical properties and purity can be understood.
12. Polarimeter determination: For optically active intermediates, their specific rotations can be determined by polarimeter to help judge their purity and optical purity.
In practical applications, these detection methods can be selected and combined according to the nature of intermediates and detection needs to ensure accurate and comprehensive evaluation of the quality of pharmaceutical intermediates.
Second, the application of pharmaceutical intermediates
1. Drug synthesis: The most important application of pharmaceutical intermediates is as a key component of synthetic apis. In the synthetic pathway, the intermediate, as the product of the conversion step, is further converted into the active pharmaceutical ingredient through a chemical reaction.
2. Research and development: In the research and development process of new drugs, intermediates are used to build different compound libraries for researchers to perform activity screening and pharmacodynamic evaluation, so as to discover potential new drug candidates.
3. Custom synthesis: For special needs research and drug development, pharmaceutical intermediates can be customized according to the specific needs of customers to adapt to special synthesis routes or research purposes.
4. Analytical standards: Pharmaceutical intermediates are also often used as standards in analytical testing to ensure accuracy and reliability in the drug quality control process.
In summary, the detection and application of pharmaceutical intermediates is a key link to ensure the safety and effectiveness of drugs. It is not only involved in the synthesis process of drugs, but also an integral part of drug development. Therefore, the quality control and research of pharmaceutical intermediates have great economic and social value.
ABOUT US
Wisdom Drugs Co .,Ltd was founded in Sep. 2011 whose headquarter located in Changzhou Creative Industry Park, having a branch in India. The company’s R&D center is engaged in not only the process development of APIs, intermediates, poly-peptide compounds and heterocyclic compounds,but also the optimization and production. We are devoted to the synthesis customization and the technology transfer, enabling compounds to be scaled from laboratory to commercial to meet the requirements of different customers.
