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Related Concept Videos

Bioavailability Enhancement: Drug Permeability Enhancement01:27

Bioavailability Enhancement: Drug Permeability Enhancement

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,...
Bioavailability Enhancement: Drug Stability Enhancement and GI Retention01:05

Bioavailability Enhancement: Drug Stability Enhancement and GI Retention

Improving a drug's stability in the gastrointestinal (GI) tract is paramount for enhancing its bioavailability and therapeutic effectiveness. Various strategies are employed to protect the drug from the harsh gastric milieu and to ensure its release and absorption at the desired site within the GI tract.Polymer coatings are one such method used to shield drugs from the stomach's acidic environment. By preventing premature drug release, these coatings improve the bioavailability of unstable...
Bioavailability Enhancement: Drug Solubility Enhancement01:16

Bioavailability Enhancement: Drug Solubility Enhancement

Bioavailability is a critical factor in determining a drug's effectiveness. It refers to the proportion of a drug that enters the circulation when introduced into the body and is, as a result, able to have an active effect. Enhancing bioavailability is essential for drugs with poor solubility, as it can significantly impact their therapeutic efficacy. Various methods are employed to increase the solubility of drugs, thereby enhancing their bioavailability.Micronization and nanonization are...
Factors Influencing Drug Absorption: Physicochemical Parameters01:22

Factors Influencing Drug Absorption: Physicochemical Parameters

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...
Methods for Studying Drug Absorption: In vitro01:16

Methods for Studying Drug Absorption: In vitro

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...
Methods for Studying Drug Absorption: In situ01:09

Methods for Studying Drug Absorption: In situ

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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Models and Methods to Evaluate Transport of Drug Delivery Systems Across Cellular Barriers
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Models and Methods to Evaluate Transport of Drug Delivery Systems Across Cellular Barriers

Published on: October 17, 2013

Absorption enhancers: applications and advances.

Bruce J Aungst1

  • 1QPS, LLC, Newark, Delaware 19702, USA. bruce.aungst@qps.com

The AAPS Journal
|November 23, 2011
PubMed
Summary
This summary is machine-generated.

Absorption enhancers improve drug absorption by increasing membrane permeation, offering non-injection alternatives for poorly permeable drugs like peptides and proteins. Advanced formulations are nearing market for transdermal, oral, and transmucosal delivery.

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Models and Methods to Evaluate Transport of Drug Delivery Systems Across Cellular Barriers
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Ex Vivo Intestinal Sacs to Assess Mucosal Permeability in Models of Gastrointestinal Disease
06:04

Ex Vivo Intestinal Sacs to Assess Mucosal Permeability in Models of Gastrointestinal Disease

Published on: February 9, 2016

Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery
  • Biopharmaceutics

Background:

  • Absorption enhancers are excipients designed to improve drug absorption, primarily by increasing membrane permeation.
  • These agents are crucial for developing non-injection formulations for drugs with poor membrane permeability, such as peptides and proteins.
  • Research in this area has spanned over two decades, with a focus on overcoming biological barriers to drug delivery.

Purpose of the Study:

  • To review advanced absorption enhancers and formulation technologies currently in development.
  • To discuss the barriers to drug absorption and the mechanisms by which absorption enhancers overcome them.
  • To explore factors influencing the success of absorption-enhancing formulations and their potential broader applications.

Main Methods:

  • Review of scientific literature on absorption enhancers and formulation technologies.
  • Analysis of mechanisms underlying membrane permeation enhancement.
  • Discussion of factors influencing the efficacy and safety of absorption-enhancing formulations.

Main Results:

  • At least one transdermal product using an absorption enhancer is on the market.
  • Several oral and transmucosal formulations utilizing absorption enhancers are nearing market approval.
  • Advanced absorption enhancers and formulation technologies are showing promise for improved drug delivery.

Conclusions:

  • Successful development of these products will provide non-injection alternatives for peptide and protein drugs.
  • The integration of novel absorption enhancers and formulation technologies can broaden delivery options for existing drugs.
  • Optimizing the benefit/risk ratio of absorption enhancers is key to their wider acceptance and application in pharmaceutical formulations.