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.

Type of course

elective courses

Mode

Blended learning

Prerequisites (description)

The lecture is intended for a wide range of listeners interested in solid state chemistry, the process of formulation of drugs from active pharmaceutical ingredients (APIs), and crystallography. Listeners should know the basics of mathematics and crystallography. Lecture intended for students in the fields of Chemistry II degree, Medical Chemistry II degree, Nanostructure Engineering.

Course coordinators

Anna Hoser
Maura Malińska

Learning outcomes

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

Presentation about the publication concerning one of the topic discussed in the lecture

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

Additional information (registration calendar, class conductors, localization and schedules of classes), might be available in the USOSweb system:

Description of 1200-2SPEC402M in USOSweb