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In vitro Digestion of Emulsions in a Single Droplet via Multi Subphase Exchange of Simulated Gastrointestinal Fluids

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Excipient-mediated supersaturation stabilization in human intestinal fluids.

Jan Bevernage¹, Thomas Forier, Joachim Brouwers

¹Laboratory for Pharmacotechnology and Biopharmacy, O&N2, Herestraat 49-Box 921, 3000 Leuven, Katholieke Universiteit Leuven, Belgium.

Molecular Pharmaceutics

|January 28, 2011

Summary

Cellulosic polymers can stabilize supersaturated poorly soluble drugs in human intestinal fluids (HIF), regardless of fed or fasted state. However, excipient effectiveness varied, and simple media had limited predictive value for HIF performance.

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Area of Science:

Pharmaceutical Sciences
Drug Delivery
Physical Chemistry

Background:

Poorly water-soluble drugs often exhibit limited oral bioavailability due to precipitation.
Controlling drug precipitation from supersaturated solutions is crucial for oral absorption.
Human intestinal fluids (HIF) present a complex environment for drug precipitation.

Purpose of the Study:

To investigate excipient-mediated precipitation inhibition of supersaturated poorly soluble drugs in human intestinal fluids (HIF).
To compare the performance of cellulosic polymers and PVP in HIF versus simple aqueous buffer and intestinal simulation media (FaSSIF/FeSSIF).
To assess the influence of the nutritional state (fasted/fed) on precipitation inhibition in HIF.

Main Methods:

Selected poorly water-soluble drugs (etravirine, ritonavir, loviride, danazol, fenofibrate) were used as model compounds.
Supersaturation was induced via solvent shift method to a degree of supersaturation (DS) of 20.
Precipitation inhibition was evaluated in HIF, aqueous buffer, FaSSIF, and FeSSIF containing various cellulosic polymers (HPMC-AS, HPMC-E5, HPMC-E50, HPMC-E4M, HPMC-P) and PVP.

Main Results:

Cellulosic polymers demonstrated the ability to reduce precipitation rates and stabilize supersaturation in HIF.
The observed stabilization was dependent on the specific drug and excipient, but not the nutritional state (fasted vs. fed).
Simple buffer and FaSSIF/FeSSIF showed limited predictive value for excipient performance in HIF, though ineffective excipients in simulation media were also ineffective in HIF.

Conclusions:

Cellulosic polymers can effectively inhibit precipitation and stabilize supersaturated solutions of poorly soluble drugs in human intestinal fluids.
The predictive capability of standard dissolution media for complex biological fluids like HIF is limited.
Excipient screening in simulation media (FaSSIF/FeSSIF) can help eliminate ineffective compounds early in formulation development.