Search research articles

ABOUT JoVE

Overview Leadership Blog JoVE Help Center

AUTHORS

Publishing Process Editorial Board Scope & Policies Peer Review FAQ Submit

LIBRARIANS

Testimonials Subscriptions Access Resources Library Advisory Board FAQ

RESEARCH

JoVE Journal Methods Collections JoVE Encyclopedia of Experiments Archive

EDUCATION

JoVE Core JoVE Business JoVE Science Education JoVE Lab Manual Faculty Resource Center Faculty Site

Terms & Conditions of Use

Related Concept Videos

Bioavailability Enhancement: Drug Permeability Enhancement

Bioavailability Enhancement: Drug Permeability Enhancement

After oral administration, poor permeability often limits the rate at which drugs are absorbed through the intestinal epithelium. Enhancing drug permeability is crucial for effective therapy, and several strategies have been developed to overcome this challenge.One effective strategy involves the use of lipid-based formulations. These formulations enhance dissolution and solubility, targeting physiological mechanisms to increase drug absorption. This includes stimulating bile salt secretion,...

Factors Influencing Drug Absorption: Presystemic Elimination

Factors Influencing Drug Absorption: Presystemic Elimination

The pharmacokinetic journey of oral drugs begins with a crucial first pass through the hepatic portal system, called the first-pass effect. This first pass significantly impacts bioavailability — the proportion of a drug that enters systemic circulation and is available for therapeutic action. The primary route sees the drug absorbed by intestinal membranes and then shunted to the liver via the hepatic portal vein. Here, pre-systemic elimination occurs as drugs face metabolism or biliary...

Drug Delivery: Enteral Route

Drug Delivery: Enteral Route

The enteral drug administration involves three primary routes: oral, sublingual, and buccal. Oral ingestion is the most prevalent, safe, economical, and convenient method for drug administration. However, it has certain drawbacks, including limited absorption due to the drug's low water solubility or poor membrane permeability, possible emesis from GI mucosa irritation, destruction of drugs by digestive enzymes or low gastric pH, and irregular absorption along with food or other drugs.
Drugs in...

Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry

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...

Bioavailability Enhancement: Drug Stability Enhancement and GI Retention

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...

Additional Routes of Drug Administration

Additional Routes of Drug Administration

Choosing the appropriate route of drug administration is significantly influenced by two key factors: the therapeutic objectives and the inherent properties of the drug being used.
Administering drugs via inhalation allows for the direct delivery of gaseous, volatile substances or droplets to different parts of the respiratory tract. One of the advantages of the inhalation route is the rapid absorption of drugs into the circulatory system, which is possible because of the large surface area of...

You might also read

Related Articles

Articles linked to this work by shared authors, journal, and citation graph.

Sort by

Same author

Corrigendum to 'changing Pseudo-nitzschia and Dinophysis distributions in the North Sea and Western approaches (NE Atlantic) and their potential use in biodiversity assessments' [harmful algae 156 (2026) 103113].

Harmful algae·2026

Same author

Changing Pseudo-nitzschia and Dinophysis distributions in the North Sea and Western Approaches (NE Atlantic) and their potential use in biodiversity assessments.

Harmful algae·2026

Same author

Discovery of Atirmociclib (PF-07220060): A Potent and Selective CDK4 Inhibitor.

Journal of medicinal chemistry·2025

Same author

Human Factors: Affect Everyone, Involve Everyone.

The clinical teacher·2025

Same author

Noninvasive monitoring with bowel ultrasound (NIMBUS) in paediatric inflammatory bowel disease: Feasibility in a single centre.

Journal of pediatric gastroenterology and nutrition·2025

Same author

Clinical validation of an individualized auto-adaptative serious game for combined cognitive and upper limb motor robotic rehabilitation after stroke.

Journal of neuroengineering and rehabilitation·2025

Search research articles

Related Experiment Video

Updated: Jun 20, 2026

Self-Nanoemulsification of Healthy Oils to Enhance the Solubility of Lipophilic Drugs

Self-Nanoemulsification of Healthy Oils to Enhance the Solubility of Lipophilic Drugs

Published on: July 27, 2022

Using the Golden Triangle to optimize clearance and oral absorption.

Ted W Johnson¹, Klaus R Dress, Martin Edwards

¹Pfizer Global Research and Development, 10770 Science Center Dr., La Jolla, CA 92121, USA. ted.w.johnson@pfizer.com

Bioorganic & Medicinal Chemistry Letters

|September 2, 2009

Summary

The Golden Triangle tool aids drug discovery by visualizing compound properties like permeability and metabolic stability. It helps medicinal chemists optimize drug candidates for potency, stability, and permeability simultaneously.

More Related Videos

Utilizing an Orally Dissolving Strip for Pharmacological and Toxicological Studies: A Simple and Humane Alternative to Oral Gavage for Animals

Utilizing an Orally Dissolving Strip for Pharmacological and Toxicological Studies: A Simple and Humane Alternative to Oral Gavage for Animals

Published on: March 23, 2016

Related Experiment Videos

Last Updated: Jun 20, 2026

Self-Nanoemulsification of Healthy Oils to Enhance the Solubility of Lipophilic Drugs

Self-Nanoemulsification of Healthy Oils to Enhance the Solubility of Lipophilic Drugs

Published on: July 27, 2022

Utilizing an Orally Dissolving Strip for Pharmacological and Toxicological Studies: A Simple and Humane Alternative to Oral Gavage for Animals

Utilizing an Orally Dissolving Strip for Pharmacological and Toxicological Studies: A Simple and Humane Alternative to Oral Gavage for Animals

Published on: March 23, 2016

Area of Science:

Drug discovery and development
Medicinal chemistry
Computational chemistry

Background:

Optimizing drug candidates requires balancing multiple properties such as metabolic stability, permeability, and potency.
Existing methods may not effectively integrate diverse data types for comprehensive property optimization.

Purpose of the Study:

To introduce the Golden Triangle, a novel visualization tool for drug discovery.
To demonstrate how integrating in vitro and computational data can guide the optimization of drug candidates.

Main Methods:

The Golden Triangle tool integrates in vitro permeability, in vitro clearance, and computational data.
Compounds are classified and plotted based on molecular weight (MW) and distribution coefficients (logD or elogD).
Analysis of orthogonal trends, such as permeability and clearance, is employed.

Main Results:

The Golden Triangle reveals useful trends for classifying compounds as permeable and stable.
Simultaneous optimization of potency, clearance, and permeability is achievable.
Balancing and optimizing multiple drug properties is facilitated through the analysis of orthogonal trends.

Conclusions:

The Golden Triangle is an effective visualization tool for medicinal chemists.
It aids in the development of metabolically stable, permeable, and potent drug candidates.
The tool enables simultaneous optimization of key drug properties for improved drug discovery outcomes.