Chemistry and Physics of Solid Pharmaceuticals - B108005
Title: Chemie a fyzika pevných léčiv
Guaranteed by: Department of Solid State Chemistry (108)
Faculty: Faculty of Chemical Technology
Actual: from 2021 to 2024
Semester: both
Points: 3
E-Credits: 3
Examination process:
Hours per week, examination: 2/0, Ex [HT]
Capacity: winter:unlimited / unknown (unknown)
summer:unknown / unknown (unknown)
Min. number of students: unlimited
Qualifications:  
State of the course: taught
Language: Czech
Teaching methods: full-time
Level:  
Note: you can enroll for the course in winter and in summer semester
Guarantor: Kratochvíl Bohumil prof. RNDr. DSc.
Interchangeability : N108022
Examination dates   
Annotation -
The course is aimed at acquiring knowledge of the chemistry and physics of solid pharmaceutical substances (active or drug substances). The chemistry of solid pharmaceutical substances includes their reactivity in the solid phase, especially possible degradation by environmental influences during storage or production (stability and testing, expiry). The physics of solid pharmaceutical substances includes their molecular and crystal structure, i.e. how the structure of the molecular solids includes the binding ratios in the molecular crystal, crystal structure parameters, polymorphism phenomenon, amorphous phase, and macroscopic properties important for technological and therapeutic applications (mainly solubility, dissolution rate - dissolution profile, permeability). Attention is also paid to the final manufacturing step - crystallization, its theory and crystallization techniques, as well as to the characterization of the product (particles, their shape and distribution), and the subsequent theory of dissolution and release of the substance from the dosage form during passage through the gastro-intestinal tract. Other solidification techniques (freeze-drying and spray-drying) are also mentioned. Furthermore, the solid pharmaceutical phases, in terms of their chemical and physical typology, used in solid dosage forms, are the subject of the course. These are primarily anhydrates, hydrates (solvates), salts and cocrystals, and then drug carriers (substances) - polymers and conjugates (ADCs). The course programme concludes with an explanation of the individual steps in the development of an original and, above all, a generic medicinal product, applying the knowledge acquired throughout the course, including the overlap with patent policy, registration and regulation.
Last update: Kratochvíl Bohumil (04.04.2025)
Literature -

R:Hilfiker R.(Ed.), Polymorphism in the Pharmaceutical Industry, Wiley-VCH Verlag, Weinheim, Germany, 2006, 9783527311460

Last update: Kratochvíl Bohumil (09.01.2018)
Syllabus -

1. Introduction, basic concepts, definition of the subject

2. Solid phase in pharmacy, its chemistry and physics

3. Molecular crystal - structure and bonding

4. Polymorphism in pharmacy

5. Crystallization I - Theory

6. Crystallization II - Crystallization techniques

7. Particle size and shape

8. Solubility, dissolution rate, permaability, bioavailability

9. Amorphous and semi-crystalline state

10.Solid pharmaceutical phases I - anhydrates, hydrates, salts, amorphous, dispersions

11.Solid pharmaceutical phases II - cocrystals, derivatives

12.Solid pharmaceutical phases III - drug carriers, conjugates

13.Chemical and physical degradation, stability

14.Generic drug development

Last update: Kratochvíl Bohumil (04.04.2025)
Learning resources -

Presentations to the subject are available on the web site: https://uchpel.vscht.cz/studium/studijni_materialy

Last update: Kratochvíl Bohumil (04.04.2025)
Learning outcomes -

Students completing this course will be able to:

  • orient themselves in the problems of the internal structure of pharmaceutical substances (molecular, crystalline, amorphous) and correlate it with the resulting properties of pharmaceutical phases
  • cope with the analysis of polymorphic systems of pharmaceutical substances, including its qualitative and quantitative analysis
  • orient themselves in crystallization techniques and be able to apply them in practice
  • for a given pharmaceutical substance be able to choose its optimal chemical and physical form (polymorph, anhydrate, hydrate, salt, cocrystal) for the development of a dosage form
  • be oriented in degradation processes, be able to apply stability tests
  • have a framework idea especially for the development of a generic pharmaceutical product
  • correlate the knowledge acquired in the subject Chemistry and Physics of Solid Pharmaceuticals with the knowledge from other profile bachelor's courses: Pharmaceutical Engineering and Organic Chemistry and Pharmacochemistry

Last update: Kratochvíl Bohumil (04.04.2025)
Registration requirements -

Organic chemistry I, II

Fundamentals of Pharmacology

Analytical chemistry I

Last update: Kratochvíl Bohumil (04.04.2025)