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Related Concept Videos

Factors Influencing Drug Absorption: Drug Dissolution01:27

Factors Influencing Drug Absorption: Drug Dissolution

The pharmacokinetic journey of drugs from solid oral dosage forms into systemic circulation is multifaceted. It begins with disintegration, a prerequisite ensuring a solid dosage form's subdivision into minute particles. Dissolution occurs next as these granulated entities solubilize in gastrointestinal fluids. This solubilization is crucial for the succeeding stage, permeation, which describes the traversal of the drug across the intestinal membrane and its subsequent entry into the blood...
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...
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...
Bioavailability: Overview01:13

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: Overview01:17

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...
Factors Influencing Bioavailability: First-Pass Elimination01:23

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...

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Related Experiment Video

Updated: May 23, 2026

Utilizing an Orally Dissolving Strip for Pharmacological and Toxicological Studies: A Simple and Humane Alternative to Oral Gavage for Animals
04:28

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

Bioavailability of digoxin from rapidly dissolving preparations.

B F Johnson1, S Lader

  • 1Department of Clinical Pharmacology, Wellcome Research Laboratories, Langley Court, Beckenham, Kent.

British Journal of Clinical Pharmacology
|March 29, 2012
PubMed
Summary
This summary is machine-generated.

Digoxin absorption is consistent across standard tablets, rapid-dissolving forms, and solutions. Slow-dissolving tablets, however, show reduced and variable digoxin bioavailability.

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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

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Last Updated: May 23, 2026

Utilizing an Orally Dissolving Strip for Pharmacological and Toxicological Studies: A Simple and Humane Alternative to Oral Gavage for Animals
04:28

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

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

Area of Science:

  • Pharmacology
  • Drug Delivery Systems
  • Gastroenterology

Background:

  • Digoxin is a cardiac glycoside used to treat heart failure and arrhythmias.
  • Understanding factors affecting digoxin's intestinal absorption is crucial for optimizing therapeutic efficacy and minimizing toxicity.
  • Variability in drug absorption can lead to inconsistent plasma concentrations and clinical outcomes.

Purpose of the Study:

  • To evaluate the impact of different dosage forms and dissolution rates on the intestinal absorption of digoxin.
  • To compare the bioavailability of standard digoxin tablets, ultra-rapid dissolution formulations, and oral solutions.
  • To assess the effect of slow-dissolving digoxin tablets on plasma concentrations and urinary excretion.

Main Methods:

  • Assessing intestinal absorption through peak plasma concentrations (Cmax) and area under the plasma concentration-time curve (AUC) over 80 hours.
  • Quantifying 10-day urinary excretion of digoxin as a measure of overall absorption.
  • Administering single doses and conducting 14-day treatment courses with various digoxin formulations (standard tablets, ultra-rapid tablets/capsules, oral solution, slow-dissolving tablets).

Main Results:

  • No significant differences in digoxin absorption were observed between standard tablets, ultra-rapid dissolution tablets/capsules, and oral solutions after single doses.
  • Consistent mean plasma concentrations and urinary excretion were noted during 14-day courses of standard or ultra-rapid formulations.
  • Slow-dissolving digoxin tablets resulted in lower and more variable mean plasma concentrations and urinary excretion compared to other formulations.

Conclusions:

  • Encapsulation and increasing tablet dissolution rates beyond 75% in 15 minutes do not enhance digoxin bioavailability.
  • Slow dissolution rates of digoxin tablets are associated with reduced and more variable intestinal absorption.
  • Formulation and dissolution characteristics significantly influence digoxin's pharmacokinetic profile and absorption consistency.