Developing Quantitative In Vitro–In Vivo Correlation for Fenofibrate Immediate-Release Formulations With the Biphasic Dissolution-Partition Test Method

Xu, Hao; Shi, Yi; Vela, Socrates; Marroum, Patrick; Gao, Ping

doi:10.1016/j.xphs.2017.06.018

Cited by 40 publications

(35 citation statements)

References 37 publications

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“…Hydrodynamic influences drug dissolution and precipitation as well as partitioning in the organic layer [12,17,19]. Therefore, sufficient mixing is of vital importance to avoid an unstirred water layer.…”

Section: Hydrodynamic Assessmentmentioning

confidence: 99%

“…The reference biphasic dissolution test for the present study basically consists of a combination of an USP II and an USP IV apparatus [12,33,39]. Initially, the ritonavir drug product disintegrates/dissolves in 41 mL SGF (pH = 1.6) in the flow-through cell (USP IV) at 5 mL/min for 30 min in a closed loop [33]).…”

Section: Comparison Of the Bipha+ Test With Established Usp Ii/iv Bipmentioning

confidence: 99%

“…A general purpose of the present study was to combine the advantages of a small-scale one-vessel method as a useful tool in formulation screening [13,14,34] and the proven biorelevance of the USP II and USP IV model [12,35,36]. All experiments were conducted in triplicate.…”

Section: Comparative Studiesmentioning

confidence: 99%

“…The aqueous phase, in turn, is covered with an organic phase creating an absorption-sink. Currently, most setups are working with a pH-shift simulating the gastrointestinal passage [12][13][14]. This setup is capable of simulating the behavior of these formulations more meaningfully [15], which includes dissolution, precipitation, and absorption.…”

mentioning

confidence: 99%

See 3 more Smart Citations

A Rational Design of a Biphasic Dissolution Setup—Modelling of Biorelevant Kinetics for a Ritonavir Hot-Melt Extruded Amorphous Solid Dispersion

et al. 2020

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Biphasic dissolution systems achieved good predictability for the in vivo performance of several formulations of poorly water-soluble drugs by characterizing dissolution, precipitation, re-dissolution, and absorption. To achieve a high degree of predictive performance, acceptor media, aqueous phase composition, and the apparatus type have to be carefully selected. Hence, a combination of 1-decanol and an optimized buffer system are proposed as a new, one-vessel biphasic dissolution method (BiPHa+). The BiPHa+ was developed to combine the advantages of the well-described biorelevance of the United States Pharmacopeia (USP) apparatus II coupled with USP apparatus IV and a small-scale, one-vessel method. The BiPHa+ was designed for automated medium addition and pH control of the aqueous phase. In combination with the diode array UV-spectrophotometer, the system was able to determine the aqueous and the organic medium simultaneously, even if scattering or overlapping of spectra occurred. At controlled hydrodynamic conditions, the relative absorption area, the ratio between the organic and aqueous phase, and the selected drug concentrations were identified to be the discriminating factors. The performance of a hot-melt extruded ritonavir-containing amorphous solid dispersion (ritonavir-ASD) was compared in fasted-state dissolution media leading to different dissolution-partitioning profiles depending on the content of bile salts. An advanced kinetic model for ASD-based well described all phenomena from dispersing of the ASD to the partitioning of the dissolved ritonavir into the organic phase.

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Section: Hydrodynamic Assessmentmentioning

confidence: 99%

Section: Comparison Of the Bipha+ Test With Established Usp Ii/iv Bipmentioning

confidence: 99%

Section: Comparative Studiesmentioning

confidence: 99%

mentioning

confidence: 99%

See 2 more Smart Citations

A Rational Design of a Biphasic Dissolution Setup—Modelling of Biorelevant Kinetics for a Ritonavir Hot-Melt Extruded Amorphous Solid Dispersion

et al. 2020

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“…This is especially an issue when surfactants are present in the media, such as in Level II biorelevant media containing bile salts and phospholipids [2], or in the formulation, which is typical for bio-enabling formulations. Many groups have studied biphasic dissolution experiments as a method to improve the predictive capabilities compared to single phase dissolution [3][4][5][6][7][8][9][10][11][12]. The majority of these experiments have been carried out using full scale dissolution apparatus.…”

Section: Introductionmentioning

confidence: 99%

On the Usefulness of Two Small-Scale In Vitro Setups in the Evaluation of Luminal Precipitation of Lipophilic Weak Bases in Early Formulation Development

et al. 2020

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A small-scale biphasic dissolution setup and a small-scale dissolution-permeation (D-P) setup were evaluated for their usefulness in simulating the luminal precipitation of three lipophilic weak bases-dipyridamole, ketoconazole and itraconazole. The transition from the gastric to intestinal environment was incorporated into both experimental procedures. Emulsification during the biphasic dissolution experiments had a minimal impact on the data, when appropriate risk mitigation steps were incorporated. Precipitation parameters estimated from the in vitro data were inputted into the Simcyp ® physiologically based pharmacokinetic (PBPK) modelling software and simulated human plasma profiles were compared with previously published pharmacokinetic data. Average C max and AUC values estimated using experimentally derived precipitation parameters from the biphasic experiments deviated from corresponding published actual values less than values estimated using the default simulator parameters for precipitation. The slow rate of transport through the biomimetic membrane in the D-P setup limited its usefulness in forecasting the rates of in vivo precipitation used in the modelling of average plasma profiles.

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Essentials of Dissolution Testing of Pharmaceutical Systems

2022

Pharmaceutical Dissolution Testing, Bioavailability, and Bioequivalence

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Developing Quantitative In Vitro–In Vivo Correlation for Fenofibrate Immediate-Release Formulations With the Biphasic Dissolution-Partition Test Method

Cited by 40 publications

References 37 publications

A Rational Design of a Biphasic Dissolution Setup—Modelling of Biorelevant Kinetics for a Ritonavir Hot-Melt Extruded Amorphous Solid Dispersion

A Rational Design of a Biphasic Dissolution Setup—Modelling of Biorelevant Kinetics for a Ritonavir Hot-Melt Extruded Amorphous Solid Dispersion

On the Usefulness of Two Small-Scale In Vitro Setups in the Evaluation of Luminal Precipitation of Lipophilic Weak Bases in Early Formulation Development

Essentials of Dissolution Testing of Pharmaceutical Systems

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