Pharmaceutical Preformulation - Profiling Drug Substances for the Biomedical Sciences

Course 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.

Education

MSc in Pharmaceutical Sciences - elective, MSc in Medicinal Chemistry - elective, Cand.Scient.Pharm. - elective, Cand.Pharm. - elective

Learning outcome

The objectives of the course are 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 and drug administration route.
     

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

Knowledge

  • define concepts and terms related to preformulation.
  • identify and discuss the importance of basic physicochemical and stability properties of drug substances in drug development.
  • account for the advantages and limitations of methods used in pharmaceutical profiling of drug substances.

 

Skills

  • calculate/predict basic prefomulation parameters.
  • 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 physicochemical properties.
  • present and discuss preformulation issues in the form of a poster.

 

Competencies:

  • design experiments related to physicochemical characterization and stability studies of drug substances.
  • obtain further and specialized knowledge and skills related to preformulation.

•Lectures: 26 hours
•Student activities (project work, poster preparation, theoretical exercises, case studies, discussion of scientific articles, oral presentations): 18 hours
•Excursion: 3 hours

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.

ECTS
See exam description
Type of assessment
Continuous assessment
Course certificate
Three written reports with acceptable answers to assignments and satisfactory participation in project work in groups of 2-3 students
Aid
All aids allowed
Marking scale
passed/not passed
Censorship form
No external censorship
Criteria for exam assessment

To pass the course the students should be able to:

Knowledge

  • define concepts and terms related to preformulation.
  • identify and discuss the importance of basic physicochemical and stability properties of drug substances in drug development.
  • account for the advantages and limitations of methods used in pharmaceutical profiling of drug substances.

 

Skills

  • calculate/predict basic prefomulation parameters.
  • 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 physicochemical properties.
  • present and discuss preformulation issues in the form of a poster.

 

Competencies:

  • design experiments related to physicochemical characterization and stability studies of drug substances.
  • obtain further and specialized knowledge and skills related to preformulation.
ECTS
See exam description
Type of assessment
Oral examination, 15-20 min
Individual oral examination based on the project work. A short presentation (7 min) followed by questioning and discussion with course teacher(s).
Aid
All aids allowed
Marking scale
passed/not passed
Censorship form
No external censorship
Criteria for exam assessment

To pass the course the students should be able to:

Knowledge

  • define concepts and terms related to preformulation.
  • identify and discuss the importance of basic physicochemical and stability properties of drug substances in drug development.
  • account for the advantages and limitations of methods used in pharmaceutical profiling of drug substances.

 

Skills

  • calculate/predict basic prefomulation parameters.
  • 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 physicochemical properties.
  • present and discuss preformulation issues in the form of a poster.

 

Competencies:

  • design experiments related to physicochemical characterization and stability studies of drug substances.
  • obtain further and specialized knowledge and skills related to preformulation.
  • Category
  • Hours
  • Lectures
  • 26
  • Preparation
  • 156
  • Practical exercises
  • 18
  • Excursions
  • 3
  • Exam
  • 3
  • English
  • 206