A population approach to in vitro–in vivo correlation modelling for compounds with nonlinear kinetics

Gaynor, Clare; Dunne, Adrian; Costello, Cian; Davis, John D.

doi:10.1007/s10928-011-9195-3

Cited by 14 publications

(16 citation statements)

References 11 publications

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“…In the second stage, the aim is to predict the in vivo plasma concentrations from the in vitro data. The predicted in vivo fractions dissolved must be ''reconvolved'' with estimates of the pharmacokinetic parameters obtained from the reference data to produce plasma concentration profiles 89 .…”

Section: Two-stage Methodsmentioning

confidence: 99%

In vitro–in vivocorrelations: general concepts, methodologies and regulatory applications

González‐García

Mangas‐Sanjuán

Merino-Sanjuán

et al. 2015

Drug Development and Industrial Pharmacy

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The major objective of in vitro-in vivo correlations is to be able to use in vitro data to predict in vivo performance serving as a surrogate for an in vivo bioavailability test and to support biowaivers. Therefore, the aims of this review are: (i) to clarify the factors involved during bio-predictive dissolution method development; and (ii) the elements that may affect the mathematical analysis in order to exploit all information available. This article covers the basic aspects of dissolution media and apparatus used in the development of in vivo predictive dissolution methods, including the latest proposals in this field as well as the summary of the mathematical methods for establishing the in vitro-in vivo relationship and their scope and limitations. The incorporation of physiological relevant factors in the in vitro dissolution method is essential to get accurate in vivo predictions. Standard quality control dissolution methods do not necessarily reflect the in vivo behavior, so they rarely are useful for predicting in vivo performance. The combination of physiological based dissolution methods with physiological-based pharmacokinetics models incorporating gastrointestinal variables will lead to robust tools for drug and formulation development, nevertheless their regulatory use for biowaiver application still require harmonization of the mathematical methods proposed and more detailed recommendations about the procedures for setting up dissolution specifications.

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Section: Two-stage Methodsmentioning

confidence: 99%

In vitro–in vivocorrelations: general concepts, methodologies and regulatory applications

González‐García

Mangas‐Sanjuán

Merino-Sanjuán

et al. 2015

Drug Development and Industrial Pharmacy

View full text Add to dashboard Cite

show abstract

“…Using the NONMEM package, a nonlinear mixed effects model can be fitted to the data with a time-scale model linking the in vitro and in vivo components [10].…”

Section: Convolution Modelmentioning

confidence: 99%

“…Based on the IVIVC model, the predicted fraction of the drug absorbed is calculated from the observed fraction of the drug dissolved. It is the most commonly cited and used method in the literature [10]. However this approach is conceptually difficult to use.…”

Section: Deconvolution Modelmentioning

confidence: 99%

“…As a result, considerable effort goes into their development and the main outcome is "the ability to predict, accurately and precisely, expected bioavailability characteristics for an extended release (ER) drug product from dissolution profile characteristics [10]. Once the IVIVC is established and defined it can be then used to guide the final cycle of formulation and process optimization program statistically based experimental design studies looking at critical formulation and process variables.…”

Section: Ivivc Developmentmentioning

confidence: 99%

“…A typical medium volume is 500 to 1000 ml. (8)(9)(10) should be withdrawn to obtain a smooth dissolution profile leading to complete dissolution within the dosing interval of the test product in humans.…”

Section: In Vitro Dissolutionmentioning

confidence: 99%

See 2 more Smart Citations

In Vitro?In Vivo Correlation (IVIVC): A Strategic Tool in Drug Development

Sakore¹,

Chakraborty²

2011

J Bioequiv Availab

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An updated overview with simple and practical approach for developing in vitro–in vivo correlation

Jacob

Nair

2018

Drug Development Research

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Preclinical Research & Development An in vitro-in vivo correlation (IVIVC) is as a predictive mathematical model that demonstrates a key role in the development, advancement, evaluation and optimization of extended release, modified release and immediate release pharmaceutical formulations. A validated IVIVC model can serve as a surrogate for bioequivalence studies and subsequently save time, effort and expenditure during pharmaceutical product development. This review discusses about different levels of correlations, general approaches to develop an IVIVC by mathematical modelling, validation, data analysis and various applications. In the current setting, the dearth of success associated with IVIVC is due to complexity of underlying scientific principles as well as the practice of fitting/matching in vivo plasma level-time data with in vitro dissolution profile. Hence, a simple, straightforward practical means to predict plasma drug levels by convolution technique and percentage drug absorbed computed from in vitro dissolution profile based on deconvolution method are illustrated. The bioavailability/bioequivalence assessment and evaluation are frequently validated by the pharmacokinetic parameters such as maximum concentration, time to reach maximum concentration, and area under the curve. The implementation of a quality by design manufacturing based on in vivo bioavailability and clinically relevant dissolution specification are recommended because corresponding design safe space will guarantee that all batches from relevant products are met with sufficient quality and bioperformance. Recently, United States Food and Drug Administration and European Medicines Agency have proposed that in silico/physiologically based pharmacokinetic modelling can be used in decision making during preclinical experiments as well as to recognize the dissolution profiles that can forecast and ensure the desired clinical performance.

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A population approach to in vitro–in vivo correlation modelling for compounds with nonlinear kinetics

Cited by 14 publications

References 11 publications

In vitro–in vivocorrelations: general concepts, methodologies and regulatory applications

In vitro–in vivocorrelations: general concepts, methodologies and regulatory applications

In Vitro?In Vivo Correlation (IVIVC): A Strategic Tool in Drug Development

An updated overview with simple and practical approach for developing in vitro–in vivo correlation

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