Principle And Applicability Of Api Active Pharmaceutical Ingredient
api active pharmaceutical ingredient Traditional Chinese medicine is not clear that the drug substance is one of the bottlenecks that restricts the modernization and internationalization of Chinese medicine. Traditional Chinese medicine pharmacological studies often take the "chemical composition separation - molecular structure identification - biological activity evaluation or activity-oriented separation" model. This model is one of the important methods of pharmacological study of traditional Chinese medicine, which leads to the discovery of artemisinin. However, the clinical application of traditional Chinese medicine attention to the overall regulation, syndrome differentiation, with multi-component, multi-target integration of the characteristics of the role. Therefore, in the study of pharmacodynamics of traditional Chinese medicine, it is necessary to further develop and improve the method and technology of the discovery of monomer api active pharmaceutical ingredient, but also to establish the theoretical and technical system of api active pharmaceutical ingredient discovery in line with the overall action characteristics of traditional Chinese medicine. Based on the research work of the author, this paper summarizes the system of "active monomer screening" and "active component discovery", so as to provide technical support for the rapid development of Chinese medicine.
The Key Technology System, Principle and Applicability of api active pharmaceutical ingredient in Traditional Chinese Medicine
1 api active pharmaceutical ingredient monomer screening strategy
As 50% of the listed drugs directly or indirectly derived from natural products, traditional Chinese medicine in the new drug research and development has a unique advantage. It is suitable for the rapid identification of traditional Chinese medicine (TCM), which can be used for the rapid identification of traditional Chinese medicine (TCM), which can be used for rapid identification of traditional Chinese medicine (TCM), which can be used for rapid identification of traditional Chinese medicine. The lead compound in the extract.
1.1 compound library preparation - activity evaluation - structural identification integration technology
The study of api active pharmaceutical api active pharmaceutical ingredient in early Chinese medicine is mainly dependent on chemical separation, but its operation is cumbersome and the shortcomings of long cycle reduces the efficiency of api active pharmaceutical api active pharmaceutical ingredient discovery. In this paper, the theory and methods of multidisciplinary crossover of chemical, biological and analytical methods were developed, and the compound library was prepared by high precision compound library preparation, high throughput activity screening and high resolution mass spectrometry. Structural integration technology. The compound library preparation system introduces the technology of mechanical automation, and the component collection time window of high performance liquid chromatography is precisely set by software to realize the whole component sampling and compound library construction. The effluent of the preparation column is carried out by splitting into the mass spectrometry Structural recognition; prepared compounds are delivered to high throughput activity screening systems (eg, microplate reader) for api active pharmaceutical ingredient. A run to complete the entire screening process, without the need to invest too much manpower, greatly reducing the screening time. Using this technique, the investigators first discovered 16 Nrf2-ARE agonists and 19 thrombin inhibitors from Salvia miltiorrhiza extract. 39 fractions were prepared from the licorice extract, nine of which were Nrf2-ARE Agonists.
1.2 fishing technology
1.2.1 Biological fishing technology
At present, the target of drug use is mainly enzymes and receptors. Biological fishing technology based on receptor-ligand binding theory, with the disease-related enzymes or receptors as a bait target, api active pharmaceutical ingredient directly from the complex Chinese medicine extract in a rapid, sensitive and accurate extraction of small molecules of activity, so that the screening efficiency doubled Ascension. The following two-dimensional vortex chromatography, ultrafiltration mass spectrometry and cell membrane chromatography as an example to illustrate its application and technical characteristics.