The aims of the first part of the course are to give the student the appropriate knowledge:
- To understand and use efficiently reference documents as pharmacopoeias for quality control of a medicine or its constituents.
- To allow the student to choose the most adequate analytical method to solve a given problem in drug analysis (mixture of active molecules, related substances, )
The aims of the second part of the course are to give the student the appropriate knowledge:
- To understand the development of a drug, its mechanism of action (interaction with targets) and its production via synthesis, isolation or biotechnology
- To allow him, through chosen examples, to understand problems and methodology in pharmaceutical chemistry
Main themes
- In the analytical part, the teachers will discuss the main methods and norms used for purity and quality control of drugs (qualitative and quantitative analysis of impurities)
- In the drug synthesis part, the teachers will discuss, using several chemical families of drugs as example, the modes of preparation, and the interactions of the drugs with their targets and/or the proteins related to their metabolism. The synthesis processes will be explained with a special focus on secondary reactions and impurities produced.
Content and teaching methods
Part 1: Quality control
1. Drugs quality control - Pharmacopoeia : general aspects
2. Purity of drugs and main degradation pathways
3. Identification methods (IR, NMR)
4. General identification reactions
5. Separation methods (liquid-liquid and solid-liquid extractions, liquid, supercritical and gaz chromatographies, electrophoresis).
6. Quantification methods and validation of analytical methods
7. Introduction to MS, coupling of MS with separation methods
8. Tests
9. General monographs
Part 2: Synthesis
1. Drugs with central nervous system activities, crossing of blood-brain barrier and related prodrugs
2. Antihistamine drugs: success, failure, future developments
3. Antiviral drugs
4. Drugs of the angiotensine receptor
5. Phosphodiesterases inhibitors
6. Drugs from biotechnology
Part 3
Discussion of monographies of drugs explained in part 2.
Other information (prerequisite, evaluation (assessment methods), course materials recommended readings, ...)