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Related Concept Videos

Bioavailability: Overview01:13

Bioavailability: Overview

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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...
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Bioavailability: Overview01:17

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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...
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Modified-Release Drug Delivery Systems: Bioavailability01:30

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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...
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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...
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Bioavailability Enhancement: Drug Permeability Enhancement01:27

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

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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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Construction of Cyclic Cell-Penetrating Peptides for Enhanced Penetration of Biological Barriers
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Cyclic peptide oral bioavailability: Lessons from the past.

Conan K Wang1, David J Craik1

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Summary

Developing oral peptide therapeutics is crucial for future drug development. This review examines factors influencing peptide oral bioavailability, particularly passive permeability, to enhance drug delivery.

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Area of Science:

  • Drug Development
  • Pharmacology
  • Biochemistry

Background:

  • High oral bioavailability is a primary goal in drug development.
  • Peptides are increasingly expected to become future therapeutics, driving interest in oral peptide delivery.
  • Research has long investigated the oral bioavailability of peptides, with recent focus on cyclic peptides.

Purpose of the Study:

  • To review research on oral peptide bioavailability.
  • To identify key factors affecting passive permeability in oral peptide drug delivery.
  • To understand how to achieve oral bioavailability for peptide therapeutics.

Main Methods:

  • Literature review of scientific research on oral peptide bioavailability.
  • Analysis of factors influencing passive permeability of peptides.
  • Examination of studies comparing linear and cyclic peptides for oral delivery.

Main Results:

  • Passive permeability is a critical factor for oral peptide bioavailability.
  • Cyclic peptides, exemplified by cyclosporine A, show promising drug-like oral bioavailability.
  • Understanding permeability factors is key to designing effective oral peptide therapeutics.

Conclusions:

  • Achieving high oral bioavailability for peptides remains a significant challenge in drug development.
  • Further research into passive permeability is essential for advancing oral peptide therapeutics.
  • Cyclic peptide structures offer potential for improved oral delivery of peptide drugs.