Questions and Answers
What are the four potential barriers to absorption?
The four potential barriers to absorption are solubility, permeability, dissolution rate, and absorption.
It classifies drugs into four classes according to their __________ across the gastrointestinal pH range and their ______________ across the gastrointestinal mucosa.
solubility, permeability
It proved to be a successful predictive tool for drug development.
True
Solubility and permeability are considered the major physicochemical factors that affect the rate and extent of oral drug absorption.
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Other physicochemical properties always show their effects on drug absorption via affecting solubility and permeability.
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What are the classes of the BCS?
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A drug is considered to be highly soluble where the highest dose strength is soluble in __________ mL or less of aqueous media over the pH range __________.
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The volume is derived from the __________ volume anticipated in the stomach when a dosage form is taken in the fasted state with a glass of water.
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If the volume of aqueous media taken to dissolve the drug in pH conditions ranging from 1 to 8 is greater than 250 mL then the drug is considered to have ______________.
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The classification therefore takes into account the __________ of the drug as well as its __________.
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A drug is considered to be highly permeable when the extent of absorption in humans is expected to be greater than 90% of the administered dose.
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Which class of the BCS is high solubility/high permeability?
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Examples of BCS Class I Drugs include:
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Which class of the BCS is characterized as low solubility/high permeability?
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Examples of Class II drugs include:
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Which class of the BCS includes hydrophilic molecules with low permeability?
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Examples of Class III BCS drugs include:
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What are traditional methods for improving oral permeability of BCS Class III?
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What are relatively modern approaches for improving oral permeability of BCS Class III?
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Which class of the BCS consists of drugs that are poorly soluble and poorly permeable?
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Examples of BCS Class IV Drugs include:
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Forming __________ of class IV compounds or finding an __________ route of delivery are approaches that have to be adopted to significantly improve their absorption into the systemic circulation.
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Study Notes
Biopharmaceutical Classification System (BCS) Overview
- The BCS addresses four potential barriers to drug absorption in the gastrointestinal tract.
- It classifies drugs into four classes based on solubility and permeability across the gastrointestinal pH range and mucosa.
BCS Classes Summary
- Class I: High solubility and high permeability. Examples include propranolol and metoprolol.
- Class II: Low solubility and high permeability. Drugs like ketoprofen and carbamazepine fall under this class, with dissolution rate potentially limiting absorption.
- Class III: High solubility but low permeability. Examples include ranitidine and atenolol; traditional and modern methods can enhance permeability.
- Class IV: Low solubility and low permeability, leading to poor oral bioavailability. Examples include hydrochlorothiazide and furosemide.
Solubility and Permeability Definitions
- A drug is highly soluble if the highest dose strength dissolves in 250 mL or less of aqueous media across pH 1-8.
- Solubility is directly linked to the amount of aqueous media needed for dissolution.
Drug Absorption Factors
- Solubility and permeability are crucial physicochemical factors affecting oral drug absorption rate and extent.
- Other physicochemical properties influence absorption indirectly through effects on solubility and permeability.
- High permeability is defined as an absorption extent exceeding 90% of the administered dose.
Methods for Enhancing Drug Absorption
- BCS Class II drugs can be optimized via formulation strategies to improve dissolution and bioavailability.
- BCS Class III drugs can enhance permeability through:
- Traditional approaches: Prodrugs and permeation enhancers.
- Modern techniques: Nanoencapsulation and nanosizing.
Additional Notes
- Formulating prodrugs or finding alternative delivery routes can significantly improve absorption for BCS Class IV drugs.
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Description
Test your knowledge of the Biopharmaceutical Classification System (BCS) with these flashcards. They cover key concepts including drug solubility, permeability, and barriers to absorption. Perfect for students and professionals in pharmaceutical sciences.
