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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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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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An Intestine/Liver Microphysiological System for Drug Pharmacokinetic and Toxicological Assessment

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Published on: December 3, 2020

Understanding the effect of API properties on bioavailability through absorption modeling.

Filippos Kesisoglou¹, Yunhui Wu

¹Department of Pharmaceutical Research, Merck Research Laboratories, Merck & Co., Inc., WP75B-210, 770 Sumneytown Pike, P.O. Box 4, West Point, Pennsylvania 19486-0004, USA. filippos_kesisoglou@merck.com

The AAPS Journal

|November 13, 2008

Summary

This summary is machine-generated.

Absorption modeling can predict how active pharmaceutical ingredient (API) properties impact drug bioavailability. This approach aids in early formulation strategy and setting API specifications during drug development.

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Area of Science:

Pharmaceutical Sciences
Drug Delivery and Formulation
Pharmacokinetics

Background:

Active pharmaceutical ingredient (API) physical properties, like particle size, significantly influence drug formulation bioperformance.
Monitoring API properties is crucial throughout drug development due to their direct impact on bioavailability.

Purpose of the Study:

To explore the application of absorption modeling in understanding the effect of API properties on bioavailability.
To demonstrate how absorption modeling can guide formulation strategy and API specification setting.

Main Methods:

Review of existing literature on absorption modeling in pharmaceutical development.
Illustrative examples showcasing the practical application of absorption modeling.

Main Results:

Absorption modeling offers a valuable tool for predicting the impact of API properties on drug absorption.
The approach can be utilized early in development to inform formulation strategy and later to establish API specifications.

Conclusions:

Absorption modeling provides a predictive framework for managing API properties and optimizing formulation bioperformance.
Further development of these modeling tools could enhance their utility in drug development.