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Related Concept Videos

Methods for Studying Drug Absorption: In vitro01:16

Methods for Studying Drug Absorption: In vitro

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In vitro experiments are crucial for understanding the transport and absorption of drugs through biological materials. These studies employ varied methods such as the diffusion cell method, the everted sac technique, and the everted ring technique.
The diffusion cell method uses a two-compartment cell, including a donor compartment with the drug solution, which simulates the environment where the drug is applied, and a receptor compartment with a buffer solution, which simulates the environment...
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Drug Absorption: Factors Affecting GI Absorption01:19

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The process of oral drug absorption can be influenced by several factors. Weakly acidic drugs tend to be absorbed more readily from the stomach due to their nonionized state. However, absorption may be less efficient in the upper intestine, where drugs are often ionized. Interestingly, despite the stomach's apparent advantage for drug absorption, its mucous layer can hinder diffusion. Its surface area is also smaller than the intestine's, which can further slow down the absorption rate.
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Methods for Studying Drug Absorption: In situ01:09

Methods for Studying Drug Absorption: In situ

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In situ experiments, such as the Doluisio method and Single-Pass Perfusion technique, provide critical insights into drug uptake by simulating in vivo conditions for drug absorption.
The Doluisio method involves perfusing a prepared segment of a rat's small intestine with a solution of radiolabeled drug and a non-absorbable marker. This helps to differentiate between absorbed and non-absorbed drug concentrations. The intestinal segment is connected at both ends using tubing and syringes,...
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Factors Influencing Drug Absorption: Anatomical Parameters01:23

Factors Influencing Drug Absorption: Anatomical Parameters

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Drug absorption involves the movement of drugs from the point of administration into the systemic circulation. Initially, Gastrointestinal (GI) motility propels the drug through the digestive tract and into the stomach. However, the stomach's high acidity and limited surface area restrict its role in drug absorption for most drugs. The drug then moves from the stomach to the small intestine via gastric emptying, which can be slowed by various factors, including interactions with other...
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Factors Influencing Drug Absorption: Physicochemical Parameters01:22

Factors Influencing Drug Absorption: Physicochemical Parameters

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The physicochemical characteristics of drugs play a crucial role in formulating stable and bioavailable drug products. The solubility of a drug, governed by the varying pH along the GI tract and its dissociation constant (pKa), is pivotal in determining its ionization state and absorption rate. Notably, weak acids and bases remain unionized and are absorbed more rapidly.
Enhanced drug absorption can be achieved by reducing particle sizes and increasing surface areas, thereby facilitating...
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Physiological Pharmacokinetic Models: Incorporating Hepatic Transporter-Mediated Clearance01:07

Physiological Pharmacokinetic Models: Incorporating Hepatic Transporter-Mediated Clearance

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Drug transporters are critical in drug absorption, distribution, and excretion processes. They should be included in physiological-based pharmacokinetic (PBPK) models, which help predict human drug disposition. However, predicting this is challenging during drug development, especially when liver transport is involved. However, with a realistic representation of body transport processes, an accurate model may be possible.
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Updated: Feb 24, 2026

An Intestine/Liver Microphysiological System for Drug Pharmacokinetic and Toxicological Assessment
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Physiologically Based Oral Absorption Modelling to Study Gut-Level Drug Interactions.

John Chung1, Filippos Kesisoglou2

  • 1Drug Product Technologies, Amgen, Inc., Thousand Oaks, California 91320.

Journal of Pharmaceutical Sciences
|August 30, 2017
PubMed
Summary
This summary is machine-generated.

Physiologically based oral absorption models predict drug performance and interactions in the gut. These in silico tools, increasingly mature, can guide formulation development and reduce the need for clinical studies.

Keywords:
cytochrome P450drug interactionsfood interactionsgastrointestinal transitin silico modelingoral drug deliverytransporters

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Area of Science:

  • Pharmacokinetics and Drug Development
  • In Silico Modeling
  • Drug Interactions

Background:

  • Physiologically based oral absorption models are in silico tools for formulation development and predicting clinical performance.
  • These models are increasingly utilized for understanding gut-level drug interactions, including those involving drug degradation, enzymes, transporters, and food effects.

Purpose of the Study:

  • To discuss the expanded applications of physiologically based oral absorption models beyond formulation development.
  • To highlight the role of these models in predicting drug performance considering gut-level interactions.

Main Methods:

  • Review of current literature on physiologically based oral absorption model applications.
  • Analysis of model utilization for predicting pharmacokinetic outcomes, particularly with co-administered agents or food.

Main Results:

  • Physiologically based oral absorption models have matured significantly over the past 15 years, evidenced by increased publications and successful predictions.
  • Successful pharmacokinetic predictions have been demonstrated, for example, after coadministration with acid-reducing agents or food.

Conclusions:

  • Oral absorption modeling and simulation, when appropriately validated, can serve as a surrogate for clinical studies.
  • These models provide mechanistic and quantitative insights into oral drug delivery and pharmacokinetics, aiding in drug development.