SFKKA9081U Pharmaceutical Preformulation - Profiling Drug Substances for the Biomedical Sciences

Volume 2013/2014
Education
MSc in Pharmaceutical Sciences - elective, MSc in Medicinal Chemistry - elective, Cand.Scient.Pharm. - elective, Cand.Pharm. - elective
Content
The course focuses on preformulation activities in drug discovery and in the drug development phase with emphasis on a practical approach. Experimental methods and data related to physical chemical characterization and stability studies of drug substances are presented and discussed. The following subjects are covered:
  1. Solid state properties and characterization
    • polymorphism, amorphous/crystalline forms, solvates
    • experimental methods such as X-ray diffraction, DSC and TGA
  2. Aqueous solubility
    • pH-solubility profiles, salt selection, intrinsic dissolution rate
    • solubility enhancing methods
    • experimental measurements
    • prediction
  3. pKa
    • experimental methods
    • prediction
  4. Partitioning
    • pH-distribution profiles, extra thermodynamic relationships,
    • experimental and calculation methods
  5. Kinetics and chemical reactivity
    • types of chemical reactions
    • simple and complicated rate equations
    • pH-rate profiles
    • prodrugs
  6. Stability testing
    • planning stability tests
    • temperature accelerated degradation
    • solid state stability including drug-excipient compatibility
    • experimental methods
Case studies and project work are used as the basis for discussing the application of the knowledge of physicochemical and stability properties of substances for selecting drug candidates and designing dosage forms . Further, the course is designed with emphasis on providing practical skills related to prediction and calculation of basic preformulation parameters.
Learning Outcome

Formål / Objective

To give students:

insight into the methods used for physicochemical characterization of drug substances and instability studies as well as interpretation and assessment of experimental data.

understanding of the importance of pharmaceutical profiling of drug substances in relation to selecting formulation strategies anddrug administration route.


Målbeskrivelse / Course outcome

At the end of the course students should be able to:

  • understand the importance of basic physicochemical and stability properties of drug substances in drug development.
  • calculate/predict basic prefomulation parameters.
  • account for the advantages and limitations of methods used in pharmaceutical profiling of drug substances.
  • design experiments related to physicochemical characterization and stability studies of drug substances.
  • assess experimental data obtained in preformulation studies.
  • discuss the selection of drug candidates and design of dosage forms on the basis of their stability and measured physical chemical properties.
Literature
Selected scientific articles, chapters from relevant books and supplementary notes.
Course teaching is based on the assumption that students have basic skills in organic, analytical and physical chemistry.
•Lectures: 26 hours
•Student activities (project work, poster preparation, theoretical exercises, case studies, discussion of scientific articles, oral presentations): 18 hours
•Excursion: 3 hours
  • Category
  • Hours
  • Exam
  • 3
  • Excursions
  • 3
  • Lectures
  • 26
  • Practical exercises
  • 18
  • Preparation
  • 156
  • Total
  • 206
Credit
7,5 ECTS
Type of assessment
Oral examination, 15-20 min
Written assignment
Prøvedesign / Examination design

Individual oral examination based on the project work. A short presentation (7 min) followed by discussion.
Exam registration requirements
Prerequisites for taking the oral examination are (i) approval of four written reports with solutions to exercises and (ii) a poster prepared as the final product of a project work on a specific drug substance. The project work and the written reports are performed in groups of 2-3 students.
Aid
All aids allowed
Marking scale
passed/not passed
Censorship form
No external censorship
Criteria for exam assesment

Beskrivelse af prøven og bedømmelse / Description of examination and assessment criteria

Beståkrav / Pass criteria

Approval of the written reports and preparation of a poster. Acceptable individual oral examination based on the project work