Physiochemical and Biopharmaceutical Properties of Drug substances and Pharmacokinetics

Gastrointestinal Physiology
Biologic membrane
Mechanisms of Drug Absorption
Passive Diffusion
Carrier-Mediated or Active Transport
Convective Absorption
Ion-Pair Absorption

Physiochemical Factors Affecting Drug Absorption
The pH-Partition Hypothesis on Drug Absorption
Ionization and pH at Absorption Site
Lipid Solubility
Partition Coefficient
Estimation of Drug Absorption
Measurement of Permeability
Cell Monolayer
Biopharmaceutical Drug Classification
Class I Drugs (High Solubility and HIgh Permeability)
Class II Drugs (Low Solubility and HIgh Permeability)
Class III Drugs (High Solubility and Low Permeability)
Class IV Drugs (Low Solubility and Low Permeability)
Role of Transporters in Drug Absorption
Efflux Transporters
Prodrugs
Strategic Considerations
Type of Prodrugs
Hard Prodrug
Soft Prodrug
Carrier-Linked Prodrug
Major Objectives of Prodrug Design
Improved Bioavailability
Improved Aqueous Solubility
Improved Passive Intestinal Absorption

Factors Affecting the Absorption of Drugs from Solid Dosage Forms and Suspensions
Dissolution
pH and Solubility of Weak Acids and Bases
Salts
Solubility and Dissolution Rate
Surface Area and Particle Size
Polymorphism
Estimate of Dose Absorbed

Summary

Pharmacokinetics
Introduction
Compartmental Concepts
Linear and Nonlinear Pharmacokinetics
Linear PK
Nonlinear PK
Intravascular Administration
IV Bolus Administration and One-Compartment Model
Elimination Rate Constant and Half-Life
Apparent Volume of Distribution
Clearance
Hepatic Clearance
IV Bolus Administration (Two-Compartment Model)
Extravascular Route of Administration
Importance of Absorption Rate
Determination of Peak Time
Determination of Peak Plasma Concentrations
Peak Time and Peak Plasma Concentration
Bioavailability
Estimating the Extent of Absorption
Presystemic or First-Pass Metabolism
Repetitive Drug Administration (Multiple Dosing)
Plasma Protein Binding in Pharmacokinetics

Statistical Moment Analysis

Summary

	Erstellt von Shannon Grady vor mehr als 11 Jahre

Medicinal Chemistry (CH3) Notiz am Outline Chapter 3, erstellt von Shannon Grady am 10/08/2013.