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Related Concept Videos

Measurement of Bioavailability: Pharmacodynamic Methods01:20

Measurement of Bioavailability: Pharmacodynamic Methods

Pharmacodynamic methods provide insights into a drug's effects on physiological processes over time and play a crucial role in understanding bioavailability and therapeutic efficacy. These methods can be broadly classified into acute pharmacological and therapeutic response approaches, each with distinct mechanisms and applications.The acute pharmacological response method directly correlates a drug's physiological effects, such as ECG or pupil diameter changes, to its time course in the body.
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...
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...
Measurement of Bioavailability: Pharmacokinetic Methods01:30

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...
Bioavailability Study Design: Single Versus Multiple Dose Studies01:11

Bioavailability Study Design: Single Versus Multiple Dose Studies

Bioavailability studies are essential for understanding how a drug is absorbed, distributed, metabolized, and excreted in the body. These studies assess the extent and rate at which the active pharmaceutical agent becomes available at the site of action. The design of bioavailability studies can involve single-dose or multiple-dose regimens, each with distinct advantages and limitations.Single-dose studies are the preferred approach due to their simplicity and reduced drug exposure for...

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Related Experiment Video

Updated: May 29, 2026

Dynamic Continuous Blood Extraction from Rat Heart via Noninvasive Microdialysis Technique
04:52

Dynamic Continuous Blood Extraction from Rat Heart via Noninvasive Microdialysis Technique

Published on: September 13, 2022

Skin microdialysis-based estimation of systemic bioavailability fraction.

Ravi Juluru1, Chinmay Shukla, Hongjun Yin

  • 1Division of Pharmaceutical Sciences, Arnold and Marie Schwartz College of Pharmacy and Health Sciences, Long Island University, Brooklyn, New York 11201, USA.

Journal of Pharmaceutical Sciences
|September 22, 2011
PubMed
Summary

This study shows that skin microdialysis can estimate systemic bioavailability, offering an alternative to plasma measurements, especially when plasma access is challenging. Skin microdialysis provides a viable method for calculating the fraction of drug absorbed systemically.

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In Vivo Microdialysis Method to Collect Large Extracellular Proteins from Brain Interstitial Fluid with High-molecular Weight Cut-off Probes

Published on: September 26, 2018

Area of Science:

  • Pharmacokinetics
  • Drug Delivery Systems
  • Biomedical Engineering

Background:

  • Systemic bioavailability is crucial for drug efficacy and is typically measured using plasma concentrations.
  • Accessing plasma can be difficult in certain populations, such as pediatric patients, necessitating alternative methods.
  • Microdialysis (MD) is a technique for sampling substances in tissues.

Purpose of the Study:

  • To investigate the feasibility of calculating systemic bioavailability fraction (F) using skin concentrations obtained from microdialysis.
  • To compare bioavailability estimations from skin microdialysis with traditional plasma-based measurements.
  • To evaluate the utility of continuous and intermittent microdialysis for bioavailability assessment.

Main Methods:

  • Systemic bioavailability fraction (F) was calculated from drug concentrations measured in the skin using continuous and intermittent microdialysis (MD).
  • Two model drugs, amoxicillin and ketoprofen, were administered to rabbits via intravenous infusion and oral suspension in a randomized crossover design.
  • Skin-derived F values were compared against F values calculated from plasma data collected concurrently.

Main Results:

  • The systemic bioavailability fraction (F) estimated using both continuous and intermittent skin microdialysis methods showed no significant difference compared to plasma-derived values for both amoxicillin and ketoprofen.
  • While comparable, the drug concentration data obtained from skin microdialysis exhibited greater variability than plasma data.
  • The study confirmed a direct proportionality between skin drug concentration-time curves and systemically absorbed drug.

Conclusions:

  • Skin microdialysis (MD) is a viable alternative method for estimating systemic bioavailability fraction (F).
  • This technique is particularly beneficial in scenarios where plasma sampling is challenging, such as in pediatric studies.
  • Further research may be needed to address the variability observed in skin microdialysis data for improved clinical application.