Crystallization and polymoprhic forms of drugs 1200-2SPEC402M
Topics discussed in the lecture:
1. Definition of the solidstates and their various forms (crystals, powders, amorphous). Types of crystals: cocrystals, salts, polymorphs, hydrates and salts. Physico-chemical properties of solid state (mechanical properties, solubility, compressibility, particle size distribution, plasticity, stability, reactivity). Solid state characterization methods (XRD, NMR, DSC, TGA, microscopy)
2. The difference between the active pharmaceutical ingredient and the drug.
3. Theory of nucleation and crystal growth in kinetic and thermodynamic terms
4. Methods of crystallization in the solution (evaporation, cooling, vapor diffusion, solvent layering), in gels, polymers, slurry. Crystallization from solid state, melts and vapor.
5. Crystallization as a method of separating optically active compounds
6. Predicting crystal morphology: non-mechanical models (BFDH model, attachment energy model) and mechanical models
7. Polymorphism in the pharmaceutical industry
8. Methods of characterization of polymorphic forms. Solid characterization methods (XRD, NMR, DSC, TGA, microscopy, IR spectroscopy, Raman, melting point)
9. Methods of selective crystallization of polymorphic forms
10. Determination of the mutual stability of polymorphic forms
11. Essential drugs (pharmaceuticals, medicines) that have different polymorphic forms (Zantac, Aspirin, Ritonavir)
12. From idea to drug. Development of a drug from an active - chemistry, production and control. Production of tablets, suspensions, inhalers.
Student workload (total 75 hours)
30 hours – participation in classes.
20 hours – preparation for classes (reading, short assignments).
15 hours – consultations with the instructor (content-related consultations, preparing the presentation).
5 hours – preparing and delivering a presentation based on a research article.
Type of course
Mode
Prerequisites (description)
Course coordinators
Learning outcomes
K_W04 Understands the design and operation of modern measurement/instrumental equipment that supports research in solid-state chemistry.
K_U03 Is able to apply appropriate methods, techniques, and research tools in solid-form (solid-state) studies as needed to solve the stated problem.
K_U16 Is able to prepare oral presentations in Polish and in English on selected topics in chemistry, using fundamental theoretical frameworks and drawing on diverse sources.
After the lecture, students know the essential physicochemical properties of solids, their different forms, characteristic properties and applications. They understand the difference in the design, development, production process depending on the solid form of API and know the research methods used in the purification and formulation of biologically active compounds, and how polymorphic forms are used in the pharmaceutical industry.
Assessment criteria
Attendance at lectures is mandatory; up to two unexcused absences are permitted.
The final grade is based on a presentation prepared on the basis of a research publication related to the lecture topics.
Bibliography
Polymorphism in Molecular Crystals, Joel Bernstein, Oxford University Press
Crystal Growth For Beginners: Fundamentals Of Nucleation, Crystal
Growth And Epitaxy Fundamentals of Nucleation, Crystal Growth and
Epitaxy, Ivan V Markov, World Scientific Publishing Company
Additional information
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