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| 2. | Designing Drugs with Optimal in vivo Activity Following Oral Administration | ||||||
| Course Coordinator: | R. Borchardt (Kansas) | ||||||
| Faculty Participants: | R. Borchardt, V. Stella (Kansas), K. Brouwer (UNC), D. Thakker (UNC), P. Burton (Pharmacia) | ||||||
| Course Objective: | To provide students with the knowledge needed to design drug candidates with optimal in vivo activity after oral administration. | ||||||
| Program: | |||||||
| 8:00 - 9:00 AM | Lecture 1. Physiology of the gastrointestinal system and physical and biochemical barrier properties of the intestinal mucosa. Ronald T. Borchardt (Kansas) | ||||||
| 9:00 - 10:00 AM | Lecture 2. Use of preclinical pharmacokinetics and in vitro models to assess problems of poor oral bioavailability. Kim Brouwer and Dhiren Thakker (UNC) | ||||||
| 10:00 - 10:30 AM | Break | ||||||
| 10:30 - 11:30 AM | Lecture 3. Structural and Physicochemical Considerations in the Design of orally Absorbable Drugs. Philip Burton (Pharmacia) | ||||||
| 11:30 - 12:30 PM | Lunch | ||||||
| 12:30 - 1:45 PM | Lecture 4. Role of intestinal and hepatic metabolism in drug clearance and chemical strategies to optimize metabolic clearance. Dhiren Thakker (UNC) | ||||||
| 1:45 - 2:45 PM | Lecture 5. Role of biliary and renal clearance in drug elimination and chemical strategies designed to minimize kidney and liver clearance. Kim Brouwer (UNC) | ||||||
| 2:45 - 3:15 PM | Break | ||||||
| 3:15 - 4:30 PM | Lecture 6. Effect of formulation factors on oral drug availability. Valentino Stella (Kansas) | ||||||
| 4:30 - 5:00 PM | Panel Discussion | ||||||