48 Questions
What is drug absorption?
The process of the movement of a drug from the site of administration into the extracellular compartment of the body.
What is the most common mechanism of absorption?
Passive non-ionic diffusion.
What factors influence drug absorption?
Molecular size, shape, degree of ionization, and lipid solubility.
What is disintegration?
The breaking of oral solid dosage forms (SDFs) into small particles to allow drug release.
Which types of SDFs are exempt from disintegration requirements according to USP guidelines?
Troches, chewable tablets, and modified release DFs.
What is dissolution?
The process where the drug dissolves in a solvent.
How is solubility determined in pharmaceutical development?
By dissolving a known quantity of a drug in 250mL buffer (pH 1.0-8.0).
What is the relationship between dissolution and absorption?
The rate of dissolution is often directly related to the rate of absorption.
What is the purpose of the Disintegration Apparatus 5?
To assess the disintegration of oral solid dosage forms.
What are the factors affecting oral drug absorption?
Disintegration, dissolution and solubility.
What are the official guidelines for disintegration of most SDFs according to USP?
Chapter 4.
Where can the USP disintegration diagram be found?
What are the factors affecting oral drug absorption?
Disintegration, dissolution (testing), solubility, permeability, rate-limiting steps
What are the dosage forms discussed?
solutions, suspensions, caps, tabs
What is drug absorption?
The process by which a drug enters the bloodstream and reaches its site of action
What is the difference between controlled-release and immediate release products?
Controlled-release products release the drug particles slowly over time, while immediate release products release the drug particles immediately
How do the plasma concentration time-curves differ between controlled-release and immediate release products?
The plasma concentration time-curve for controlled-release products shows a gradual increase and sustained release of drug, while the plasma concentration time-curve for immediate release products shows a rapid increase and rapid decline of drug concentration
What are drug bioavailability and bioequivalence?
Drug bioavailability is the extent to which a drug reaches its site of action, while bioequivalence compares the bioavailability of the same drug in different formulations
How do drug bioavailability and bioequivalence differ?
Bioavailability refers to the extent of drug reaching its site of action, while bioequivalence compares the bioavailability of the same drug in different formulations
What are the three indices of bioavailability?
Cmax, tmax, AUC
What is the Biopharmaceutics Classification System (BCS)?
A system that classifies drugs based on their solubility and permeability
What are the factors considered in the Biopharmaceutics Classification System (BCS)?
Solubility and permeability
What is the purpose of dissolution testing?
To determine the rate at which a drug dissolves in a specified medium
What is the rate-limiting step for low water soluble (hydrophobic) drugs?
Dissolution
Drug absorption is the process of the movement of drug from the site of administration into the extracellular compartment of the body. GI tract is an important factor in oral ______.
absorption
Passive non-ionic diffusion is the most common mechanism of ______.
absorption
Absorption is influenced by 4 factors 1. ______ 2. ______ 3. ______ 4. lipid solubility.
molecular size, shape, degree of ionization
Disintegration is required for oral solid dosage forms (SDFs) to allow drug ______.
release
Permeability is an ______ measurement of absorption.
indirect
Disintegration guidelines apply to most SDFs with the exception of ______, chewable tablets, and modified release DFs.
troches
Rate-Limiting Steps in Drug Absorption - Slowest step = the ______ step
rate-limiting
Dissolution is the process where the drug ______ in a solvent.
dissolves
Generally, tablet ______ is the fastest step.
disintegration
For pharmaceutical development, ______ is determined by dissolving a known quantity of a drug in 250mL buffer (pH 1.0-8.0).
solubility
Dissolution is often the ______ step for low water soluble (hydrophobic) drugs.
rate limiting
Rate of dissolution is often directly related to the rate of ______.
absorption
Permeability is often the ______ step for high water soluble (hydrophilic) drugs.
rate limiting
The factors affecting oral drug absorption include ______, disintegration, dissolution and solubility.
molecular size, shape, degree of ionization, lipid solubility
Solutions are already ______ so dissolution is not a rate limiting step
dissolved
The factors affecting oral drug absorption also include disintegration, ______ and solubility.
dissolution
Drug particles are ______ in a vehicle
suspended
The official guidelines for disintegration of most SDFs according to USP can be found in ______.
USP, chapter 4
Efficient dosage form distinguished by a shell that holds the drug formulation. Shell must release the drug particles before absorption can take place. Can be formulated as controlled-release to alter absorption kinetics. Must first break into granules/large pieces and then into drug particles. Can be formulated as ______ to alter absorption kinetics.
controlled-release
The Disintegration Apparatus 5 is used to test the ______ of oral solid dosage forms.
disintegration
For oral products, bioavailability depends on the drugs ______ and absorption
dissolution
Can be altered by the drugs stability in gastric fluids, formulation components, and first-pass effect (hepatic metabolism).
bioavailability
Used to describe the bioavailability of same drug in two different formulations. Important for comparing generic products with the name-brand product. Testing typically involves in vivo human PK studies to evaluate the rate and extent of ______.
absorption
Biopharmaceutics Classification System (BCS) – ______ – Permeability
Solubility
Test your knowledge on the factors influencing oral drug absorption including molecular size, shape, degree of ionization, and lipid solubility.
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