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 1st and 2nd 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
Subject Physical Principles of Dosage Forms is taught in the third year of study and builds on Biophysics and Physical Chemistry. The aim of the subject is to provide comprehensive information on the basic physical principles used in formulation, function and stabilizing pharmaceutical forms. In particular, it describes the properties of solid phase (active compounds and Excipients), liquid phase and dispersion (molecular, colloidal and macrodispersion) and interfacial interfacacial phenomena that are related to the physical and chemical stability of pharmaceutical products. In the subject of the Physical Principles of Dosage Forms, students will also be acquainted with the basics of polymer chemistry necessary to understand the structure, properties and function of these substances in pharmaceutical formulations and modern drug delivery systems. The basic principles of pharmaceutical nanotechnologies will also be included.
Considering that the physical properties of materials and physical processes at the interface significantly affect resulting quality of pharmaceutical formulations, understanding these principles is essential for further study of pharmaceutical technology and dosage forms. From this perspective, the Physical Principles of Dosage Forms can be viewed as an interdisciplinary subject with a linking function between fundamental subjects taught in the first section of study and highly specialized pharmaceutical technology.
Topics: Solution properties, Solid phase, Solid phase properties, Solubility and dissolution, Diffusion, Interfacial phenomena in pharmaceutical Systems, Pharmaceutical surfactants, Pharmaceutical polymers, Polymer systems, Rheology, Dispersion systems and their stability,