Physical Principles of dosage forms

Teachers: Dr. Georgios Paraskevopoulos Ph.D., PharmDr. Eva Šnejdrová, Dr. Monika Smékalová, PhD

School year 2022/2023, 3rd year, lecutres: 2/0 =28/0, Exam, 2 credits

Lecture topics

1. Introduction into Physical Pharmacy

Definitions

History

Physical principles affecting pharmaceutical preparations

Physical principles affecting bioavailability of drugs, bioavailability significance

Specific technological processes influencing bioavailability

Interactions between pharmaceutical preparations and organism

2. Solid state

Properties of solid state

Crystallography, crystal properties, polymorphism, crystal hydrates, liquid crystals

State shifts

Real density

Solid state characterization methods (RTG diffraction, DSC, TGA)

3. Surface properties of solid state

Specific surface

Porosity (porosimetry, permeametry, pycnometry)

Adsorption, factors influencing adsorption, adsorption based pharmaceutical systems

Physical adsorption

Chemical adsorption

Adsorption isotherms

Wettability of solid particles, contact angle

Solid particles interactions

4. Solubility and dissolution

Solubility of solids (liquids, gasses)

Factors influencing solubility of solids

Thermodynamics of solids dissolution

Noyes - Whitney equation – dissolution kinetics and the effect on pharmaceutical systems efficiency

Solvent – solute interactions, solvatation – relevant examples

Liberation of drugs

5. Solutions

Types of pharmaceutical solutions and relevant examples

Ideal vs. real solutions, practical applications of Raoult’s law

Isotonic solutions, isotonization

Colligative properties

Solubility product

Types of concentration

6. Diffusion

Diffusion rate and influencing factors

Diffusion principles, Fick’s 1^st and 2^nd law and practical applications

Charged particles diffusion/ uncharged particles diffusion

Diffusion driving forces in pharmacy

Principles and applications of osmosis and ultrafiltration

Diffusion based pharmaceutical systems

Diffusion characteristics within biological systems

7. Diffusion through polymeric membrane

Principles of diffusion through polymeric membrane

Pore diffusion, Fibrous membrane diffusion

Monolithic matrix diffusion

Multilayer membrane diffusion

Diffusion through polymeric barrier based preparations and relevant examples

Principles of controlled diffusion

Drugs permeation, permeability

8. Application of interfacial phenomena in pharmaceutical systems

Relevant properties of interfacial phenomena on l/l, s/g, s/l

Concept and calculation of surface tension and surface free energy

Relationship between ability to act on interface and efficiency of pharmaceutical systems

Cohesion and adhesion of surfaces

Relevant examples of pharmaceutical systems based on interfacing

9. Pharmaceutical surfactants

Surfactants’ structural predispositions

Structural types of pharmaceutical surfactants

Utilization of surfactants in pharmaceutical systems

HLB System

10. Pharmaceutical polymers

Types of pharmaceutical polymers

Molecular weirght of pharmaceutical polymers

Structure and organization of polymers

Copolymers

Polymers’ physical states

Polymer crystallization

Biodegradability, biocompatibility

11. Polymer systems

Polymeric solutions

Water soluble/water insoluble polymers

Polymer swelling

Polymeric gels

Stimuliresponsive polymers

Bioadhesive/ mucoadhesive polymers

12. Disperse systems

Properties of disperse systems and their use in pharmacy

Factors influencing the stability of disperse systems

Electric properties of disperse systems: DLVO theory, zeta potential, Nernst potential, flocculation

13. Basic principles of nanotechnology in pharmacy

Definition and principles involved

Phase separation

Coagulation

Coacervation

Dendrimers

Potential problems and obstacles of nanotechnology based pharmaceutical systems