1. CHEE 4401 Definitions drug - any substance that affects the structure or functioning of an organism pharmaceutics - the area of study concerned with the formulation, manufacture, stability, and effectiveness of dosage forms pharmacology - the science of the properties of drugs and their effects on the body pharmacokinetics - the study of the kinetics of absorption, distribution, metabolism, and excretion of drugs and their corresponding pharmacologic response in animals/man clinic - a facility or area where ambulatory patients are seen for special study and treatment

2. CHEE 4402 PHARMACEUTICAL INDUSTRY Drug Discovery - natural sources, synthesis/modification Preclinical Studies biological properties - pharmacology, pharmacokinetics preformulation - chem/phys properties - analytical assays Formulation l development of dosage form l large-scale manufacturing Clinical Trials Approval for Distribution Post-Marketing Surveillance

3. CHEE 4403 INTRODUCTION u drugs seldom administered alone ä given as a formulation »contain additional ingredients called excipients u objective of dosage form design ä achieve a predictable therapeutic response to a drug included in a formulation which is capable of large scale manufacture with reproducible product quality u must consider physical, chemical, biological properties of all components

4. CHEE 4404 Excipients

5. 5 Need for Dosage Forms u provide safe and accurate delivery of given dosage u protect drug from environmental degradation u protect drug from GI degradation u conceal bitter, salty taste, offensive odor u allow for administration of poorly soluble drug u provide rate-controlled action u allow for admin. by desired route

6. CHEE 4406 Routes of Administration

7. CHEE 4407 Drug Action

8. CHEE 4408 Biopharmaceutics u Bioavailability ä extent of absorption and the rate at which an administered dose reaches systemic circulation in its active form drug in dosage form liver tissue, lymph blood plasma bound  free site of action excretion metabolism intravenous oral

9. CHEE 4409 u example of oral administration plasma concentration time profile plasma conc’n time after administration absorption phase elimination phase

10. CHEE 44010 ä therapeutic response is dependent on drug achieving an adequate plasma concentration plasma conc’n C p time after administration Therapeutic Window

11. CHEE 44011 Pharmacodynamics ä not all individuals respond in same manner minimum dose for response (mg/kg) no. of individuals therapeutic index (TI)

12. CHEE 44012 u absolute bioavailability ä any drug delivered extravascularly has the potential of being bound or eliminated before reaching bloodstream ä amount of drug reaching bloodstream is equal to the area under the C p vs t curve, AUC u relative bioavailability ä some drugs cannot be given by iv ä bioavailability determined by comparison to standard dosage form

13. CHEE 44013 u Bioequivalence ä comparison of amounts of same drug that are absorbed from 2 different formulations of the same dosage form (generics) ä the two formulations are considered equivalent if there is no significant difference between any of C max, T max, AUC time CpCp