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

Modified-Release Drug Delivery Systems: Bioavailability

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...

Bioavailability: Influencing Factors

Bioavailability: Influencing Factors

Bioavailability refers to the extent and rate at which a drug reaches systemic circulation in its active form. Extent refers to the amount of the drug that makes it into circulation, while rate is the speed at which it enters circulation. It is influenced by several factors critical for optimizing drug formulations, dosing regimens, and therapeutic outcomes.Physicochemical properties of drugs and formulationsThe solubility, stability, and dissolution rate of a drug significantly impact its...

Bioavailability: Overview

Bioavailability: Overview

Bioavailability refers to the proportion of an unaltered drug that, after administration, enters the systemic circulation and can be distributed to the desired action site. Factors such as gastrointestinal (GI) absorption and liver biotransformation influence the bioavailability of a drug when it is administered orally. When a drug is administered intravenously, it enters the systemic circulation directly; by definition, its bioavailability is assumed to be 100%. The bioavailability of an...

Bioavailability: Overview

Bioavailability: Overview

Bioavailability refers to the proportion of an administered drug that reaches the systemic circulation in its active, unaltered form. It is a crucial pharmacokinetic parameter that determines the effectiveness of a drug in achieving its intended therapeutic outcomes. The route of administration significantly influences bioavailability, with intravenous administration achieving 100% bioavailability as the drug directly enters the bloodstream. In contrast, oral administration often results in...

Measurement of Bioavailability: Pharmacokinetic Methods

Measurement of Bioavailability: Pharmacokinetic Methods

Pharmacokinetics is a vital branch of pharmacology that examines how drugs are absorbed, distributed, metabolized, and excreted by the body. Two key methodologies in pharmacokinetics are plasma drug concentration studies and urinary drug excretion analyses, both of which provide critical insights into a drug's therapeutic efficacy and bioavailability.Plasma Drug Concentration-Time StudiesPlasma drug concentration-time studies involve analyzing blood samples at specific intervals to quantify...

Factors Influencing Bioavailability: First-Pass Elimination

Factors Influencing Bioavailability: First-Pass Elimination

When a drug is taken orally, it undergoes a journey starting from the gastrointestinal (GI) tract, passing through the portal vein, reaching the liver, and finally entering the systemic circulation. This process involves the absorption of the drug across the GI tract. The liver is the primary site for metabolizing the drug, with some metabolism also occurring in the gut wall. This journey significantly reduces the quantity of the drug that reaches the systemic circulation, a phenomenon known as...

You might also read

Related Articles

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

Sort by

Same author

Early Weight Regain After GLP-1 Receptor Agonist Discontinuation: Mechanisms and Implications for Treatment De-Escalation Strategies.

Diabetes, obesity & metabolism·2026

Same author

Delayed cardiac arrest after hydrofluoric acid ingestion.

Clinical toxicology (Philadelphia, Pa.)·2024

Same author

The perceived waning of biologics in severe asthma.

Respiratory medicine·2023

Same author

Healthcare professionals' perceptions on barriers and facilitators to DMARD use in rheumatoid arthritis.

BMC health services research·2022

Same author

Fifteen years' experience with methylphenidate for attention-deficit disorder during pregnancy: Effects on birth weight, Apgar score and congenital malformation rates.

General hospital psychiatry·2021

Same author

High prevalence of peripheral neuropathy in multiple myeloma patients and the impact of vitamin D levels, a cross-sectional study.

Supportive care in cancer : official journal of the Multinational Association of Supportive Care in Cancer·2021

Same journal

The expanded cardiovascular risk prediction score as a cardiovascular mortality predictor in rheumatoid arthritis.

Clinical and experimental rheumatology·2026

Same journal

Rising overweight and obesity in Swiss psoriatic arthritis patients, 2007-2022: a nationwide registry-population comparison.

Clinical and experimental rheumatology·2026

Same journal

Clinical features and gastrointestinal bleeding risk factors in IgA vasculitis patients: a retrospective study in a large volume centre.

Clinical and experimental rheumatology·2026

Same journal

Reply to the comment on: The microbiota in axial spondyloarthritis: what have we learned from Mendelian randomisation studies?

Clinical and experimental rheumatology·2026

Same journal

Comprehensive evaluation of bone structural and microarchitectural changes in rheumatoid arthritis treated with baricitinib using HR-pQCT, imaging, and biomarker analyses.

Clinical and experimental rheumatology·2026

Same journal

Tracking interstitial lung disease in systemic sclerosis: integrating lung magnetic resonance imaging into a clinically oriented multimodal follow-up strategy.

Clinical and experimental rheumatology·2026

See all related articles

Search research articles

Related Experiment Video

Updated: Jun 7, 2026

Comprehensive Evaluation of the Effectiveness and Safety of Placenta-Targeted Drug Delivery Using Three Complementary Methods

Comprehensive Evaluation of the Effectiveness and Safety of Placenta-Targeted Drug Delivery Using Three Complementary Methods

Published on: September 10, 2018

Methotrexate bioavailability.

E N van Roon¹, M A F J van de Laar

¹Department of Pharmacotherapy and Pharmaceutical Care, University of Groningen, Groningen, Netherlands. e.n.van.roon@znb.nl

Clinical and Experimental Rheumatology

|November 4, 2010

Summary

This summary is machine-generated.

Methotrexate (MTX) bioavailability decreases with higher oral doses due to absorption limits. Splitting doses or using parenteral administration improves MTX bioavailability for better efficacy and safety.

More Related Videos

Multi-Gene Single Nucleotide Polymorphism Detection in Gastric Cancer Based on Ion Semiconductor Sequencing Platform

Multi-Gene Single Nucleotide Polymorphism Detection in Gastric Cancer Based on Ion Semiconductor Sequencing Platform

Published on: May 10, 2024

Quantification of the Immunosuppressant Tacrolimus on Dried Blood Spots Using LC-MS/MS

Quantification of the Immunosuppressant Tacrolimus on Dried Blood Spots Using LC-MS/MS

Published on: November 8, 2015

Related Experiment Videos

Last Updated: Jun 7, 2026

Comprehensive Evaluation of the Effectiveness and Safety of Placenta-Targeted Drug Delivery Using Three Complementary Methods

Comprehensive Evaluation of the Effectiveness and Safety of Placenta-Targeted Drug Delivery Using Three Complementary Methods

Published on: September 10, 2018

Multi-Gene Single Nucleotide Polymorphism Detection in Gastric Cancer Based on Ion Semiconductor Sequencing Platform

Multi-Gene Single Nucleotide Polymorphism Detection in Gastric Cancer Based on Ion Semiconductor Sequencing Platform

Published on: May 10, 2024

Quantification of the Immunosuppressant Tacrolimus on Dried Blood Spots Using LC-MS/MS

Quantification of the Immunosuppressant Tacrolimus on Dried Blood Spots Using LC-MS/MS

Published on: November 8, 2015

Area of Science:

Pharmacology
Clinical Pharmacy

Background:

Bioavailability is crucial for drug efficacy and safety, linking systemic concentration to clinical outcomes.
Methotrexate (MTX) bioavailability is a key factor in optimizing patient dosing regimens.

Purpose of the Study:

To review the current understanding of methotrexate bioavailability.
To identify factors affecting MTX bioavailability and suggest strategies for dose optimization.

Main Methods:

Literature review of existing studies on methotrexate bioavailability.
Analysis of factors influencing MTX absorption and systemic concentration.

Main Results:

Higher oral doses of MTX show reduced bioavailability, likely due to gastro-intestinal absorption limitations.
Both splitting oral doses and parenteral administration are proposed to enhance MTX bioavailability compared to a single high oral dose.

Conclusions:

Methotrexate bioavailability is critical for effective and safe treatment.
Strategies like dose splitting or parenteral routes may improve MTX bioavailability, but further comparative studies are needed.