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MacroFLUX

In many cases, dissolution experiments alone cannot predict the in vivo response to drug products due to the complicated interplay of solubility and permeability in complex media. By introducing a stirred absorption chamber into familiar USP dissolution apparatus, Pion’s MacroFLUX™ allows you to extend the utility of in situ UV concentration monitoring to provide an accurate assessment of transmembrane FLUX.

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Introduction

The Pion MacroFLUX™ apparatus can be used for conducting simultaneous dissolution-absorption studies. Such studies allow assessment of the complex interplay between solubility, permeability and dissolution rate in-vitro and provide valuable tools for understanding in vivo outcomes.

MacroFLUX™ can be used (i) during formulation development for optimising product performance and to evaluate whether certain formulation changes will affect the bio-performance of a certain drug product, (ii) during life-cycle management and product extensions to demonstrate bioequivalence, (iii) to compare brand and generic formulations to demonstrate bioequivalence, (iv) to compare test to reference formulations, (v) to ensure continuity of product quality (batch to batch consistency) and performance of the manufacturing process (in order to differentiate bioequivalent batches from non-bioequivalent batches within a range that guarantees comparable biopharmaceutical performance in vivo).

Sample submission details

Formulated products, number of tablets/capsules dependent on type of study and required number of replicates. Pure API is required for calibration purposes.

Key deliverable

Acceptor drug concentrations and flux values across the membrane. Additionally, the percent release (%mass/time) of drug for each donor vessel is determined showing release profiles and dissolution performance. A full study report is provided.

Experiment overview

The MacroFLUX device consists of an absorption (receiver) chamber integrated with a permeation membrane, overhead stirrer and fiber optic (FO) UV probe that is inserted in to a modified cover of a standard 900 mL vessel of a USP II apparatus. The filter-supported artificial permeation membrane separates the dissolution (donor) compartment from the receiver compartment, containing pH 7.4 Pion Acceptor Sink Buffer. The dissolution compartment typically holds 900 mL of compendial or biorelevant dissolution buffer. The modified vessel cover allows fiber-optic UV probes to be positioned in both the donor and receiver compartments allowing real-time dissolution and absorption concentration monitoring in both chambers. Concentration monitoring is enabled by connecting the fiber optic UV probes to the Rainbow Dynamic Dissolution Monitor® instrument (Pion Inc.).

The use of in situ fibre-optic dip-probe UV analysis, overcomes many of the challenges of traditional testing methods. Issues typically encountered with external sampling of test solutions (e.g., sampling errors due to filter clogging, mechanical sipper malfunction, sample contamination, adsorption of compound to tubing) are minimized since the concentration measurements are performed directly in the dissolution media, with processed results plotted in real time. Interference due to background turbidity is minimized when needed by a spectral second derivative method. Spectral scans (200 – 720 nm) of all channels takes less than five seconds.

Resources

Using Biorelevant Flux Measurements for Prediction of Fraction Absorbed for the Drug Products of Poorly Soluble Compounds

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From Traditional Dissolution to In Vivo Predictive Flux Measurements

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Prediction of Bioequivalence and Food Effect Using Flux- and Solubility-Based Methods

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Biorelevant Flux Measurements And Prediction Of Fraction Absorbed For The Drug Products Of Poorly Soluble Compounds

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Combining biorelevant in vitro and in silico tools to simulate and better understand the in vivo performance of a nano-sized formulation of aprepitant in the fasted and fed states

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MacroFLUX DDI

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The effect of formulation additives on in vitro dissolution-absorption profile and in vivo bioavailability of telmisartan from brand and generic formulations

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Using pH Gradient Dissolution with In-Situ Flux Measurement to Evaluate Bioavailability and DDI for Formulated Poorly Soluble Drug Products

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Video: Use of Flux Measurements in Lieu of In Vitro Dissolution to Assess the Complex Interplay Between Solubility, Permeability and Formulation Effects

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MacroFLUX Generics

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Application of MacroFLUX™ Apparatus for Screening Formulations before Bioequivalence Studies

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Using Integrated Absorption Chamber with USP II Dissolution Apparatus to Predict Risk of Drug‐Drug Interaction from pH‐Modifying Agents: Application Notes

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FLUX Measurements using Pion µFLUX™ and MacroFLUX™ Devices

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Application of MacroFLUX™ Apparatus for Screening Formulations before Bioequivalent Studies

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Using Integrated Absorption Chamber with USP II Dissolution Apparatus to Predict Risk of Drug-Drug Interaction from pH Modifying Agents: Poster

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Application of simultaneous dissolution-absorption apparatus for screening formulations before bioequivalence studies

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MacroFLUX An Integration of Absorption Chamber with USP II Dissolution Apparatus

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Assay part number

Platinum Standard FLUX determination in Aqueous Media/MacroFLUX

1818111

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Platinum Standard FLUX determination in Biorelevant Media/MacroFLUX

1818112

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