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Related Concept Videos

Bioavailability Enhancement: Drug Stability Enhancement and GI Retention01:05

Bioavailability Enhancement: Drug Stability Enhancement and GI Retention

Improving a drug's stability in the gastrointestinal (GI) tract is paramount for enhancing its bioavailability and therapeutic effectiveness. Various strategies are employed to protect the drug from the harsh gastric milieu and to ensure its release and absorption at the desired site within the GI tract.Polymer coatings are one such method used to shield drugs from the stomach's acidic environment. By preventing premature drug release, these coatings improve the bioavailability of unstable...
Factors Affecting Dissolution: Drug pKa, Lipophilicity and GI pH01:21

Factors Affecting Dissolution: Drug pKa, Lipophilicity and GI pH

Drug absorption within the gastrointestinal (GI) tract is a complex process influenced by several critical factors, including the site pH, the drug's dissociation constant (pKa), and the drug's lipophilicity. The GI tract exhibits a pH gradient, with an acidic environment in the stomach and a more alkaline environment in the small intestine. This pH variation directly affects the ionization state of drugs.
A drug's pKa and the pH of the gastrointestinal (GI) tract play crucial roles in drug...
Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry01:20

Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry

Orally administered drugs primarily enter the systemic circulation via passive diffusion through the intestinal membranes. The drug's absorption is influenced by drug stability in the gastrointestinal GI tract, membrane permeability, the surface area available for absorption, luminal drug concentration, and residence time in the lumen. Drug permeability can be enhanced by adjusting the lipophilicity, polarity, or molecular size of the drug, promoting its passive transport across intestinal...
In Vitro Drug Dissolution: Alternative Methods01:17

In Vitro Drug Dissolution: Alternative Methods

Alternative drug dissolution methods include the rotating bottle, intrinsic dissolution test, peristalsis, and the Franz diffusion cell method. The rotating bottle method involves meticulously rotating tightly capped controlled-release beads in a temperature-controlled bath. Periodic decanting of samples allows for residue assay, followed by refilling with fresh medium and testing at various pH levels to emulate the gastrointestinal tract conditions.In contrast, the intrinsic dissolution test...
Modified-Release Drug Delivery Systems: Bioavailability01:30

Modified-Release Drug Delivery Systems: Bioavailability

Modified-release (MR) dosage forms are designed to extend drug release over time, thereby maintaining stable plasma concentrations and reducing dosing frequency. However, their bioavailability is typically below 100% due to incomplete drug release and presystemic metabolism, and limitations in drug permeability across the gastrointestinal epithelium, all of which can restrict the fraction of the drug reaching systemic circulation. Consequently, studying the in vivo bioavailability of MR...
Drug Dissolution: Requirements and Profile Comparison01:14

Drug Dissolution: Requirements and Profile Comparison

The acceptance criteria for dissolution profile data are anchored in Q values, representing the percentage of drug dissolved within a specified period. This assessment unfolds in three stages:First Stage: The test passes if all six drug dosage units are equal to or greater than Q plus 5%; otherwise, the sample proceeds to the second stage.Second Stage: The average of twelve units must be equal to or greater than Q, with no unit falling below Q - 15% to pass; if not, it progresses to the final...

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Related Experiment Video

Updated: Jun 28, 2026

An Intestine/Liver Microphysiological System for Drug Pharmacokinetic and Toxicological Assessment
08:59

An Intestine/Liver Microphysiological System for Drug Pharmacokinetic and Toxicological Assessment

Published on: December 3, 2020

Solution stability--plasma, gastrointestinal, bioassay.

Li Di1, Edward H Kerns

  • 1Wyeth Research, Princeton, NJ 08543-8000, USA. dil@wyeth.com

Current Drug Metabolism
|November 11, 2008
PubMed
Summary
This summary is machine-generated.

Early screening of drug candidate solution stability in biological fluids is crucial for successful drug discovery. Optimizing stability methods ensures reliable data for prioritizing compounds and improving drug properties like bioavailability.

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Basic Research in Plasma Medicine - A Throughput Approach from Liquids to Cells
07:37

Basic Research in Plasma Medicine - A Throughput Approach from Liquids to Cells

Published on: November 17, 2017

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Last Updated: Jun 28, 2026

An Intestine/Liver Microphysiological System for Drug Pharmacokinetic and Toxicological Assessment
08:59

An Intestine/Liver Microphysiological System for Drug Pharmacokinetic and Toxicological Assessment

Published on: December 3, 2020

Basic Research in Plasma Medicine - A Throughput Approach from Liquids to Cells
07:37

Basic Research in Plasma Medicine - A Throughput Approach from Liquids to Cells

Published on: November 17, 2017

Area of Science:

  • Pharmacokinetics and Drug Metabolism
  • Medicinal Chemistry
  • Drug Discovery and Development

Background:

  • Solution stability of drug candidates in plasma, gastrointestinal fluids, and bioassays is critical for achieving low clearance, good oral bioavailability, and robust structure-activity relationships (SAR).
  • Early screening for solution stability helps avoid pursuing high-risk unstable compounds, enabling better prioritization of chemical series and guiding structural modifications.

Purpose of the Study:

  • To emphasize the importance of early solution stability screening in the drug discovery process.
  • To highlight key factors influencing the relevance and reliability of solution stability data.
  • To discuss methodologies, applications, structure-stability relationships, and provide case studies.

Main Methods:

  • Discusses critical parameters for solution stability assays, including test compound concentration, enzyme source and preparation, solubility limits, and cosolvent use.
  • Examines the impact of plasma protein binding and compares detection techniques such as liquid chromatography-ultraviolet (LC-UV) versus liquid chromatography-mass spectrometry (LC-MS).
  • Addresses the importance of monitoring parent compound disappearance versus the formation of degradants.

Main Results:

  • Early identification of solution stability issues can significantly enhance the chances of project success by preventing the pursuit of unstable drug candidates.
  • Optimized assay conditions are essential for generating meaningful data that accurately reflects in vivo behavior.
  • Understanding structure-stability relationships allows for rational design and modification of compounds to improve stability.

Conclusions:

  • Solution stability is a key determinant of drug candidate success, impacting clearance, bioavailability, and SAR.
  • Rigorous and well-defined solution stability screening methods are indispensable for efficient and effective drug discovery.
  • Proactive assessment and optimization of drug stability contribute to a higher probability of developing successful therapeutics.