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A Stratified Analysis of Supersaturation and Precipitation Effects Based on the Refined Developability Classification
Kristian Beran1, Eline Hermans2, René Holm3
1Fraunhofer Institute for Translational Medicine and Pharmacology, Frankfurt am Main, Germany; Janssen Pharmaceutica NV, Pharmaceutical & Material Sciences, Beerse, Belgium.
Journal of Pharmaceutical Sciences
|June 22, 2024
Summary
Supersaturation behavior of active pharmaceutical ingredients (APIs) in the gut impacts oral absorption. Integrating this into the refined Developability Classification System (rDCS) aids formulation selection for better bioavailability.
Area of Science:
- Pharmaceutics
- Biopharmaceutical Sciences
- Drug Delivery
Background:
- Oral absorption of active pharmaceutical ingredients (APIs) is significantly influenced by their supersaturation and precipitation behavior within the gastrointestinal tract.
- Weakly basic APIs can enhance absorption through supersaturation upon intestinal transfer, while salt forms of weak acids may achieve this in both stomach and intestine.
- Solubility-limited APIs often require enabling formulations to generate supersaturated solutions for improved gut absorption.
Purpose of the Study:
- To revisit and refine the Developability Classification System (rDCS) for a more comprehensive assessment of drug developability risks.
- To integrate in vitro supersaturation and precipitation characteristics of APIs into the biopharmaceutical risk classification framework.
- To guide formulation selection strategies for optimizing oral bioavailability (BA) by considering API physicochemical properties.
Main Methods:
- Revisiting the existing refined Developability Classification System (rDCS) strategy.
- Proposing a stratified approach for classifying APIs based on their developability.
- Integrating in vitro data on supersaturation and precipitation behavior of APIs and their formulations.
Main Results:
- The study proposes a refined approach to the rDCS by incorporating in vitro supersaturation and precipitation data.
- This integration allows for a more accurate mapping of potential developability risks associated with APIs.
- The proposed stratified approach aids in selecting appropriate formulations to enhance oral absorption.
Conclusions:
- Integrating in vitro supersaturation and precipitation behavior into the rDCS provides a robust strategy for developability assessment.
- This approach enables better prediction of oral absorption and guides formulation development for solubility-limited APIs.
- The refined rDCS facilitates optimized formulation selection to improve oral bioavailability.
Keywords:
Biopharmaceutical risk analysisDevelopabilityFormulation guidanceOral absorptionPrecipitationRefined developability classification system (rDCS)SupersaturationMore Related Videos
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