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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

Bioavailability: Overview

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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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Bioavailability: Influencing Factors01:22

Bioavailability: Influencing Factors

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

Factors Influencing Bioavailability: First-Pass Elimination

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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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Bioavailability Study Design: Absolute Versus Relative Bioavailability01:27

Bioavailability Study Design: Absolute Versus Relative Bioavailability

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Bioavailability is a crucial pharmacokinetic parameter that quantifies the proportion of an administered drug that reaches the systemic circulation and is available for therapeutic action. Regulatory agencies mandate the assessment of bioavailability, typically measured as the area under the drug plasma concentration-versus-time curve (AUC), to ensure the efficacy and safety of pharmaceutical products. These evaluations are categorized as absolute and relative bioavailability studies.Absolute...
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Modified-Release Drug Delivery Systems: Bioavailability01:30

Modified-Release Drug Delivery Systems: Bioavailability

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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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Accumulation of plasma levels of anthocyanins following multiple saskatoon berry supplements.

Xenobiotica; the fate of foreign compounds in biological systems·2019
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HPLC-MS/MS analysis of anthocyanins in human plasma and urine using protein precipitation and dilute-and-shoot sample preparation methods, respectively.

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Classification of fruits based on anthocyanin types and relevance to their health effects.

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Some anthocyanins could be efficiently absorbed across the gastrointestinal mucosa: extensive presystemic metabolism reduces apparent bioavailability.

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Updated: Apr 21, 2026

Extraction and Purification of Polyphenols from Freeze-dried Berry Powder for the Treatment of Vascular Smooth Muscle Cells In Vitro
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Bioavailability of anthocyanins.

Jim Fang1

  • 1College of Pharmacy and Nutrition, University of Saskatchewan , Saskatoon, Saskatchewan , Canada.

Drug Metabolism Reviews
|October 28, 2014
PubMed
Summary

Anthocyanins, natural pigments in fruits and vegetables, are absorbed in the gut and metabolized. These metabolites, not the original compounds, may be responsible for health benefits like reduced disease risk.

Area of Science:

  • Nutritional Science
  • Biochemistry
  • Pharmacology

Background:

  • Anthocyanins are plant pigments responsible for red, blue, and purple hues.
  • Dietary anthocyanins are linked to reduced risks of cardiovascular disease and cancer.
  • Their metabolic fate differs significantly from other flavonoids.

Purpose of the Study:

  • To review the absorption, distribution, metabolism, and elimination (ADME) of anthocyanins.
  • To explore the role of metabolites and gut microbiota in anthocyanin bioactivity.
  • To synthesize current knowledge on anthocyanin gastrointestinal processing.

Main Methods:

  • Literature review of studies on anthocyanin pharmacokinetics and metabolism.
  • Analysis of data on anthocyanin absorption sites (stomach, intestines).
Keywords:
Absorptionanthocyaninbioavailabilitycyanidin-3-glucosidedistributionexcretionfirst-pass metabolismmetabolism

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  • Examination of the role of transporters and first-pass metabolism.

    • Main Results:

    • Anthocyanins are absorbed intact in the gastrointestinal tract and undergo extensive first-pass metabolism.
    • Circulating metabolites, primarily phenolic acids, are found at higher concentrations than parent compounds.
    • Significant amounts of anthocyanins reach the large intestine, where microbial decomposition occurs.

    Conclusions:

    • Anthocyanin health benefits may be mediated by their metabolites and microbial breakdown products.
    • Understanding anthocyanin ADME is crucial for elucidating their physiological effects.
    • Further research into the bioactivity of anthocyanin metabolites is warranted.