ODD2012: Predicting Drug Absorption


Program Goal

To provide an in-depth focus on oral drug delivery, biopharmaceutics, methods for estimating and evaluating drug absorption, and strategies for achieving optimal drug delivery and absorption from the gastrointestinal tract. The course will include problem and demonstration sessions, and attendance will be limited to 40 participants, to enhance interaction between faculty and students.

New Features

  • Hands-On Computational Sessions
  • Software and Computers Provided
  • OpenOffice™, GastroPlus™, ADMET Predictor™, MedChem Designer™
  • Predicting Absorption
  • Provisional BCS Classification
  • Classical Bioequivalence Determination
  • Absorption Analysis
  • Poster and Exhibit Session with Discussion

Educational Objectives

Following this course, participants will be able to:

  • Understand the gastrointestinal, drug and dosage form processes controlling absorption.
  • Understand the relevance and utility of in vitro tissue culture models to in vivo absorption.
  • Understand and apply methods for estimating and evaluating oral drug absorption, including high throughput screening (HTS) methods and computer simulation and prediction methods.
  • Evaluate and develop appropriate methods to optimize oral delivery.
  • Be able to identify the potential rate limits to oral drug absorption.
  • Understand intestinal and hepatic metabolic pathways and their impact on absorption and systemic availability.
  • Identify appropriate types of controlled release dosage forms for specific drugs.
  • Identify GI physiological variables influencing absorption rate and extent.
  • List metabolism and transporter factors e.g., P-gp, influencing absorption and systemic availability.
  • Have an understanding of molecular membrane transporters and their importance for drug absorption and excretion.
  • Analyze and simulate pharmacokinetic absorption rate and plasma level.
  • Understand the current FDA bioavailability (BA) and bioequivalence (BE) standards and how they may evolve in the future.

Faculty List

Amidon, Bermejo, Bolger, Cook, Langguth, Lennernäs, Lionberger, Polli, Tamai

Agenda

Sunday, February 26

  • 5:00-7:00 PM: Registration – Hospitality Room
  • 7:00-9:00 PM: Welcome Reception – Tahoe D to Tahoe C

Monday, February 27

  • 7:30–8:30 AM: Breakfast:  Sand Harbor I
  • 8:30–5:00 PM: Predicting Absorption and BCS - Location:  Sand Harbor II

Morning Program: Predicting Oral Drug Absorption: Soluble Drugs

  • 8:30-9:30 AM: Human Absorption Prediction: The Global View (Amidon)
  • 9:30-10:30 AM: Gastrointestinal Physiological Variables (Bermejo)
  • 10:30-10:45 AM: Refreshment Break
  • 10:45-11:45 AM: Mechanisms of Intestinal Membrane Permeation (Amidon)
  • 12:00-1:30 PM: Lunch – Location: Sand Harbor I

Afternoon Program: “Hands-On” Computations: Predicting Absorption and Provisional BCS Classification

  • 1:30-2:30 PM: Partition Coefficient in silico and Absorption Estimation (Amidon) (OpenOffice.org™ Calc  (MS Excel compatible)     
  • 2:30-3:30 PM: BCS Classification in silico using log P as a surrogate for Peff (Amidon/Bolger) (OpenOffice.org™ Calc  (MS Excel compatible)
  • 3:30-3:45 PM: Refreshment Break
  • 3:45-5:00 PM: Intro to MedChem Designer™ and  S+LogP,  Provisional BCS (Amidon/Bolger)

Tuesday, February 28

  • 7:30-8:30 AM: Breakfast:  Sand Harbor I
  • 8:30-5:30 PM: Permeability - Location: Sand Harbor II

Morning Program: Experimental Methods to Measure Permeability

  • 8:30-9:30 AM: Human Jejunal Permeability:  The Gold Standard (Amidon)
  • 9:30-10:30 AM: Permeability Methods in situ:  Rat/Mouse/Dog (Bermejo/Amidon)
  • 10:30-10:45 AM: Refreshement Break
  • 10:45-11:45 AM: Cell Culture Permeability Methods in vitro (Polli)
  • 11:45-12:30 PM: Estimating Solubility (Amidon)
  • 12:30-1:30 PM: Lunch - Location: Sand Harbor I

Afternoon Program: “Hands-On” Computations using Integrated Software

  • 1:30-2:30 PM: The Absorption Spreadsheet (OpenOffice.org): Estimating: MlogP, MH-Solubility, Simple Peff, Aqueous Diffusivity (Bolger)
  • 2:30-3:30 PM: Estimating Biorelevant Solubility from Aqueous Solubility & logP (Bolger)
  • 3:30-3:45 PM: Refreshment Break
  • 3:45-5:30 PM: ADMET™ Predictor: Modeling & Applicability Domain; Comparison of Estimation methods and Applicability Domain (Woltosz)
  • 7:00-10:00 PM: Reception – Sand Harbor III; Dinner and Gaming Tournament – Sand Harbor III

Wednesday, February 29

  • 7:30-8:30 AM: Breakfast: Sand Harbor I
  • 8:30AM–12:30 PM: Dissolution and Absorption Methodologies; Location: Sand Harbor II

Morning Program: Dissolution and IVIVC

  • 8:30-9:30 AM: Dissolution Methodology and Current Challenges (Polli)
  • 9:30-10:30 AM: Analysis of Drug Absorption: PK Analysis and IVIVC (Langguth)
  • 10:30-10:45 AM: Refreshment Break
  • 10:45-11:45 AM: Oral Absorption and Bioequivalence (Bermejo)
  • 11:45-12:30 PM: “Hands-On” Hands-on Computations: Bioequivalence (Bermejo/Cook)
  • 12:30-2:00 PM: Box Lunch
  • 2:00-7:00 PM: FREE TIME; Posters available for viewing; Location: Tahoe D to Tahoe C    
  • 7:00-8:00 PM: “If we Designed Airplanes like we Designed Drugs…”; Location:  Sand Harbor II (Woltosz)
  • 8:00-10:00 PM: Posters; Wine and Cheese Reception; Location: Tahoe D to Tahoe C (Amidon)

Thursday, March 1

  • 7:30-8:30 AM: Breakfast: Sand Harbor I
  • 8:30 AM-5:30 PM: Oral Delivery Based BCS Class; Location: Sand Harbor II

Morning Program: Oral Delivery: Class I (CR), BCS Class II (Solubilization), Class III (Prodrugs) and IV

  • 8:30-9:30 AM: BCS Class I:  IR and CR (Langguth)
  • 9:30-10:30 AM: BCS Class II:  Solubilization Methods (Langguth)
  • 10:30-10:45 AM: Refreshment Break
  • 10:45-11:45 AM: BCS Class III:  Prodrugs and Transporters (Tamai)
  • 12:00-1:30 PM: Lunch: Sand Harbor I

Afternoon Program: “Hands-On” Computations Integrated Software

  • 1:30-2:30 PM: “Hands-On” Computations: Wagner-Nelson, IVIVC (Amidon/Langguth)
  • 2:30-3:30 PM: Analysis  of Examples Data (Cook/Polli/Bermejo)
  • 3:30-3:45 PM: Refreshment Break
  • 3:45-5:30 PM: Mechanistic ACAT Deconvolution and IVIVCs for Highly Variableand MR Formulations (Bolger)

Friday, March 2

  • 7:30-8:30 AM: Breakfast: Sand Harbor I
  • 8:30-11:45 AM: Oral Delivery: Future Regulation and Molecular Transport
  • 8:30 -9:30 AM: BCS Based Regulatory Standards: Evolving World Wide (Cook)
  • 9:30-10:30 AM: Regulatory Future:  Pharmaceutical Quality (Lionberger)
  • 10:30-11:30 AM: Modern Molecular Membrane Transport: Molecular ADME (Tamai)
  • 11:30-11:45 AM: Closing Remarks (Amidon)

Full Program Accessible Here