SFKKA9081U  Pharmaceutical Preformulation - Profiling Drug Substances for the Biomedical Sciences

Volume 2015/2016
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:

Solid state properties and characterization

  • polymorphism, amorphous/crystalline forms, solvates
  • experimental methods such as X-ray diffraction, DSC and TGA

 

Aqueous solubility

  • pH-solubility profiles, salt selection, intrinsic dissolution rate
  • solubility enhancing methods
  • experimental measurements
  • prediction

 

pKa

  • experimental methods
  • prediction

 

Partitioning

  • pH-distribution profiles, extra thermodynamic relationships,
  • experimental and calculation methods

 

Kinetics and chemical reactivity

  • types of chemical reactions
  • simple and complicated rate equations
  • pH-rate profiles
  • prodrugs

 

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

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.

 

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
Credit
7,5 ECTS
Type of assessment
Oral examination, 15-20 min
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

To pass the course the student must 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
  • Total
  • 206