Drug Stability & Drug development: Course Outline (P2, P-III)

Introduction to drug design and discovery

• Terms used
• Brief discussion of research phases of drug discovery
• Rational drug
• Designing including biological phase
• Chemical phase
• Pre-clincial and clinical phases
• Approval phase

Development of new drugs

• Sources of drugs including serendipity
• Natural source
• Soil
• Shemical libraries
• Brief discussion of drug development pathways

Concept of Pro-drug and application in drug designing

• Application in the formulation development for example I/V
• Oral drugs

Drug designing through studies of metabolites of drugs

• Phase I and phase II reactions
• Role of cytochrome P450
• Oxidative
• Reductive and hydrolytic reaction

Receptor theories

• Concept of agonists and antagonists
• Clark’s theories
• Occupational theory
• Macromolecular perturbation theory
• Brief discussion of drug receptor interaction with special reference to with the
• Mechanism of action of the drug molecule

Introduction and objectives of drug stability studies significance of stability

• Stability testing during development stages of pharmaceutical products
• Types of stability testing
• GMP requirements regarding stability
• Compendial requirements FDA
• Guidelines and stability protocols
• Introduction to product stability of different pharmaceutical dosage form
• Tablets
• Capsule
• Suspensions
• Solutions
• Emulsions
• Ointments

Mode of degradation of drugs kinetic principles in drug stability

• Chemical degradation rates
• Pharmaceutical compatibilities
• Physical degradation
• Kinetics of degradation
• The arhenius equation and calculated stability testing

Physical and photo-stability of pharmaceutical substances in solid and liquid

forms

• Physical degradation
• Factors affecting physical stability
• Kinetics of solid-phase transitions

Chemical factors affecting the stability of drugs

• The role of molecular structure
• Temperature pH and pH rate profiles buffer
• General and acid base
• Nucleophilic and electrophilic catalysis dielectric constant

Stereochemistry of drug molecules and pharmacological activity

• Conformational isomers
• Geometrical isomerism
• Optical isomers and analysis of stereochemistry of the drugs in terms of pharmacological activity