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Related Concept Videos

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 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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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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Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry01:20

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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...
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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 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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Related Experiment Video

Updated: May 5, 2026

Targeting the Rat's Small Bowel: Long-Term Infusion into the Superior Mesenteric Artery
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Rectal motility and bioavailability.

J J Tukker1, C J de Blaey, G A Charbon

  • 1Dept. of Pharmaceutics, State University, Catharijnesingel 60, 3511 GH, Utrecht, The Netherlands.

Pharmaceutical Research
|November 27, 2013
PubMed
Summary

Canine rectal wall contractions significantly impact fatty suppository drug release and absorption. This effect is more pronounced with larger drug particles, highlighting rectal motility

Area of Science:

  • Pharmacokinetics and Drug Delivery

Background:

  • Rectal drug delivery is a common route for systemic drug administration.
  • Factors influencing drug release and absorption from rectal suppositories require further investigation.

Purpose of the Study:

  • To investigate the influence of canine rectal wall contractile activity on the in vivo behavior of fatty suppositories.
  • To assess the impact of drug particle size and colloidal silicium oxide on suppository performance and drug bioavailability.

Main Methods:

  • Evaluation of fatty suppositories containing phenazone in canine models.
  • Assessment of suppository spreading, drug release rate, and extent of release.
  • Analysis of drug bioavailability in relation to rectal contractile activity and drug particle size (100-125 µm vs. < 35 µm).

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Main Results:

  • Canine rectal wall contractile activity positively influenced suppository spreading and phenazone release.
  • The effect of rectal motility on bioavailability was significant with large drug particles (100-125 µm) but minimal with small particles (< 35 µm).
  • Colloidal silicium oxide addition markedly improved spreading and bioavailability.

Conclusions:

  • Rectal motility is a significant factor contributing to variability in drug bioavailability from rectal suppositories.
  • Drug particle size plays a crucial role in the interaction between rectal motility and drug absorption.
  • Standardized animal models with well-trained subjects are essential for reproducible bioavailability studies of rectal suppositories.