Pharmaceutics & Pharmacology

Course goals

After completing this course you are able to:

1. Describe physicochemical concepts that are relevant to pharmaceutical dossage forms
2. Explain and predict the stability, sedimentation rate and viscosity of colloidal systems (emulsions, micelles, suspensions).
3. Determine, explain and predict the phase behavior of emulsions and the type of emulsion (w/o or o/w).
4. Describe and explain the action of excipients and their influence on the properties of pharmaceutical formulations.
5. Describe and predict the dissolution rate of a solid and the release of an active substance from a dosage form, and relate it to substance properties and environmental factors in the gastrointestinal tract
6. Perform simple mathematical operations related to the topics mentioned above. Interpret and apply formulas correctly and work with the right units and the significant number of decimals.
7. Describe the anatomy and physiology of the gastrointestinal tract with regard to the absorption of drug.
8. Be familiar with the most common drug delivery routes, the associated dosage forms, and the requirements imposed on these drug administrations with regard to their composition and biopharmaceutical behavior.
9. Use the biopharmaceutical classification system and predict the absorption of the active substance in the blood and relate it to substance properties and environmental factors in the gastrointestinal tract.
10. Apply the factors that influence the absorption of the active substance into the blood.
11. Explain the relation of drug absorption, distribution, metabolism and excretion (ADME) with drug efficacy and the consequences for dosing regimens, both qualitatively and quantitatively. 
12. Report and interpret the results of self-performed experiments in a correct and clear manner (in a lab journal, concise report, measurement report and/or oral presentation) using the usual graphic images.
13. Work in a laboratory setting while respecting your own and other people's safety

Content

Introduction:
The main focus of this course will be on different aspects that are related to pharmaceutical technology (drug formulation design and stability), pharmaceutics (drug administration and pharmaceutical availability) and pharmacokinetics (absorption, distribution, metabolism and excretion).
 
Set up of the course:
Course MBLS-310 lays the scientific foundations for physical pharmacy/chemistry, in order to understand the design and application of pharmaceutical preparations. In addition, you will learn to apply pharmacokinetic principles such that the effect of the dosage form, administration route, the absorption rate and drug metabolism/excretion on the residence time of the drug in the body is understood.

In pharmaceutical preparations, there are often two- or multi-phase systems, such as a solid in contact with a liquid or a system consisting of two immiscible liquids. All kinds of physico-chemical phenomena at the interfaces play an important role in this. Consider, for example, the preparation and stability of emulsions and suspensions by mixing of liquids and solids and how these are influenced by the addition of excipients. The course will pay attention to stability of dispersions, solubility, dissolution rate, diffusion and interfacial phenomena.

Within this course, different routes of drug administration are discussed, with the focus on the oral and to a lesser extent rectal routes of administration. The composition of the most common oral and rectal dosage forms and the role that the different excipients have in the formulation including the physical background are discusssed. The factors that are important for the release of a drug from a solid dosage form such as polymorphism, particle size, diffusion, dissolution rate and solubility are explained in this course.

The absorption of the pharmacon in the body are discussed. Important themes within this course are pharmaceutical availability with an emphasis on the characteristics of the pharmacon and the oral dosage form, and bioavailability in which release from the dosage form and absorption into the body play a major role. The knowledge from previous courses is used and supplemented within this course to make an estimate of how well a medicine will be absorbed into the body (pH, pKa, charge, lipophilicity, BCS classification, Lipinsky's rule of 5), and how these will influence the pharmacokinetics by applying different multi-compartment models.

The education is both theoretically and practically oriented and thematic in design.

Teaching methods & concepts:
Various lectures are given during course MBLS-310. The aim of these lectures is to introduce and support a number of topics that are elaborated in the tutorials and on the practicum, and to deal with and place them in a broader context.

In the tutorials, you practice with the course material under supervision in relatively small working groups, which are a good preparation for the intermediate and final exams.

During the practicals, you will study physicochemical parameters such as interfacial tension and stability of emulsions and suspensions in a number of experiments. You investigate how these parameters can be influenced and what the consequences are for a pharmaceutical product. The practical assignments are discussed during seminars. The results obtained during the practical work and the associated backgrounds are presented and discussed.

A final assignment in this course includes preparation of a drug dossier, in which for a given drug several aspects are reviewed related to its formulation, stability, bioavailability, and ADME of the drug.

Estimation of each teaching method in this course:
Lectures = 10%
Tutorials = 10%
Practicals = 10% (incl. preparative tutorials and seminars)
Self study = 70% (incl. writing of reports and drug dossier)

Relation to other courses:
This elective course fits the profile Molecules & Medicine, and guides students deeper into pharmaceutical research and drug development.  Pharmacodynamics (drug – target interaction) has been addressed in MBLS-205. With the complete set of knowledge and skills you gain in both courses, you will be trained in the whole chain from drug formulation and application to its function. Hence this course connects to other courses in the bachelor programme College of Pharmaceutical Sciences (CPS), and to the master programme Drug Innovation.  

Grading (check course manual for details):
Midterm exam (20%)
Final exam 2 (50%)
Drug dossier (15%)
Practicals (15%)

The course is completed with a pass if the final grade is sufficient (≥ 6; a rounded six) and at the same time the grades of the final test and the drug dossier are ≥ 5.5.
For this course, attendance is compulsory for the tutorials prior to the practicals, the practicals, the presentations during the seminars and the tests.