In Vitro–In Vivo Correlations of Carbamazepine Nanodispersions for Application in Formulation Development

Warnken, Zachary N.; Puppolo, Michael M.; Hughey, Justin R.; Duarte, Íris; Jansen‐Varnum, Susan A.

doi:10.1016/j.xphs.2017.10.014

Cited by 14 publications

(6 citation statements)

References 42 publications

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“…Warnken et al [13] investigated the capability of an in vitro dissolution/absorption method using simulated media based on human data to predict in vivo performance in mice. The authors found that especially the change in pH to a value relevant for the preclinical species improved the IVIVC [13].…”

Section: Introductionmentioning

confidence: 99%

Developing a predictive in vitro dissolution model based on gastrointestinal fluid characterisation in rats

Christfort

Strindberg

Plum

et al. 2019

European Journal of Pharmaceutics and Biopharmaceutics

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Section: Introductionmentioning

confidence: 99%

Developing a predictive in vitro dissolution model based on gastrointestinal fluid characterisation in rats

Christfort

Strindberg

Plum

et al. 2019

European Journal of Pharmaceutics and Biopharmaceutics

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“…Dispersity and the shape of the crystals of APIs and excipients are of high importance in the development of the solid dosage forms [1, 27]. Therefore it is advisable to estimate the size (distribution by fractions) and the shape of particles of the potential pharmaceutical substance's candidate already at the stage of the first screening.…”

Section: Resultsmentioning

confidence: 99%

“…To predict expected bioavailability characteristics for drug substances the pharmaceutical scientists give their significant attention to investigate the dependence of the pharmaceutical ingredient's activity on the degree of dispersion [1, 2].…”

Section: Introductionmentioning

confidence: 99%

Mechanical Transformation of Compounds Leading to Physical, Chemical, and Biological Changes in Pharmaceutical Substances

Сыроешкин

Uspenskaya

Pleteneva

et al. 2018

The Scientific World Journal

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This study demonstrates the link between the modification of the solid-phase pharmaceutical substances mechanical structure and their activity in waters with different molar ratio «deuterium-protium». Mechanochemical transformation of the powders of lactose monohydrate and sodium chloride as models of nutrients and components of dosage forms was investigated by the complex of physicochemical and biological methods. The solubility and kinetic activity of substances dispersed in various ways showed a positive correlation with the solvent isotope profile. Substances dissolved in heavy water were more active than solutes in natural water. Differential IR spectroscopy confirmed the modification of substituents in the sample of lactose monohydrate, demonstrating physicochemical changes during mechanical intervention. The biological activity of the compounds was determined by the method of Spirotox. The activation energy was determined by Arrhenius. Compared with the native compound, dispersed lactose monohydrate showed lower activation energy and, therefore, greater efficiency. In conclusion, proposed data confirm the statement that mechanical changes in compounds can lead to physicochemical changes that affect chemical and biological profiles.

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“…In actuality, non-sink conditions can be more reflective of the in vivo environment in which the available volume for dissolution is less than 500 mL [31]. Other authors have recently proposed a non-sink dissolution permeation method to discriminate among CBZ formulations with and IVIVC developed with mice data [32].…”

Section: Modeling Dissolution Datamentioning

confidence: 99%

In Vivo Predictive Dissolution (IPD) for Carbamazepine Formulations: Additional Evidence Regarding a Biopredictive Dissolution Medium

et al. 2020

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The aim of the present study was to bring additional evidence regarding a biopredictive dissolution medium containing 1% sodium lauryl sulphate (SLS) to predict the in vivo behavior of carbamazepine (CBZ) products. Twelve healthy volunteers took one immediate release (IR) dose of either test and reference formulations in a bioequivalence study (BE). Dissolution profiles were carried-out using the medium. Level A in vitro–in vivo correlations (IVIVC) were established using both one-step and two-step approaches as well as exploring the time-scaling approach to account for the differences in dissolution rate in vitro versus in vivo. A detailed step by step calculation was provided to clearly illustrate all the procedures. The results show additional evidence that the medium containing 1% SLS can be classified as a universal biopredictive dissolution tool, and that both of the approaches used to develop the IVIVC (one and two-steps) provide good in vivo predictability. Therefore, this biopredictive medium could be a highly relevant tool in Latin-American countries to ensure and check the quality of their CBZ marketed products for which BE studies were not requested by their regulatory health authorities.

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In Vitro–In Vivo Correlations of Carbamazepine Nanodispersions for Application in Formulation Development

Cited by 14 publications

References 42 publications

Developing a predictive in vitro dissolution model based on gastrointestinal fluid characterisation in rats

Developing a predictive in vitro dissolution model based on gastrointestinal fluid characterisation in rats

Mechanical Transformation of Compounds Leading to Physical, Chemical, and Biological Changes in Pharmaceutical Substances

In Vivo Predictive Dissolution (IPD) for Carbamazepine Formulations: Additional Evidence Regarding a Biopredictive Dissolution Medium

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