Using a Physiologically Based Pharmacokinetic Absorption Model to Establish Dissolution Bioequivalence Safe Space for Oseltamivir in Adult and Pediatric Populations

Miao, Lei; Mousa, Youssef M.; Zhao, Liang; Raines, Kimberly; Seo, Paul; Wu, Fang

doi:10.1208/s12248-020-00493-6

Cited by 26 publications

(21 citation statements)

References 32 publications

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“…In this case study, similar in vivo performance of slow and fast tablets of losartan compared with the target formulation was demonstrated using MAM by incorporating the available in vitro dissolution data 24 . A recent research article published by the US FDA demonstrated the utility of the PBPK absorption modeling approach to set clinically relevant dissolution “extrapolated” safe space for oseltamivir oral dosage forms with theoretical dissolution profiles as inputs using a virtual BE simulation in different age groups 25 . Similarly, virtual BE assessment through a robust PBBM model approach for several drugs have been discussed in the literature 26,27 .…”

Section: Discussionmentioning

confidence: 79%

“…24 A recent research article published by the US FDA demonstrated the utility of the PBPK absorption modeling approach to set clinically relevant dissolution "extrapolated" safe space for oseltamivir oral dosage forms with theoretical dissolution profiles as inputs using a virtual BE simulation in different age groups. 25 Similarly, virtual BE assessment through a robust PBBM model approach for several drugs have been discussed in the literature. 26,27 The literature has shown irrelevance of in vitro dissolution for dextromethorphan, which is subjected to lysosomal trapping.…”

Section: Discussionmentioning

confidence: 99%

See 1 more Smart Citation

Application of physiologically based biopharmaceutics modeling to understand the impact of dissolution differences on in vivo performance of immediate release products: The case of bisoprolol

Macwan

Fraczkiewicz

Bertolino

et al. 2021

CPT Pharmacom & Syst Pharma

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Section: Discussionmentioning

confidence: 79%

Section: Discussionmentioning

confidence: 99%

Application of physiologically based biopharmaceutics modeling to understand the impact of dissolution differences on in vivo performance of immediate release products: The case of bisoprolol

Macwan

Fraczkiewicz

Bertolino

et al. 2021

CPT Pharmacom & Syst Pharma

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“…With the recently increasing interest in developing (semi)mechanistic models for drug dissolution and absorption, 60 , 61 , 62 many efforts are now directed at further improving dissolution and absorption modeling. 63 , 64 Adopting a more mechanistic approach to drug release in children, dissolution kinetics could be measured in vitro in biorelevant media that reflect the gastrointestinal physiology in children 65 , 66 and described using a (semi)mechanistic dissolution model, which is then integrated in a whole‐body pediatric PBPK model.…”

Section: Discussionmentioning

confidence: 99%

Predictive Performance of Physiology‐Based Pharmacokinetic Dose Estimates for Pediatric Trials: Evaluation With 10 Bayer Small‐Molecule Compounds in Children

Ince

Dallmann

Frechen

et al. 2021

The Journal of Clinical Pharma

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Development and guidance of dosing schemes in children have been supported by physiology‐based pharmacokinetic (PBPK) modeling for many years. PBPK models are built on a generic basis, where compound‐ and system‐specific parameters are separated and can be exchanged, allowing the translation of these models from adults to children by accounting for physiological differences. Owing to these features, PBPK modeling is a valuable approach to support clinical decision making for dosing in children. In this analysis, we evaluate pediatric PBPK models for 10 small‐molecule compounds that were applied to support clinical decision processes at Bayer for their predictive power in different age groups. Ratios of PBPK‐predicted to observed PK parameters for the evaluated drugs in different pediatric age groups were estimated. Predictive performance was analyzed on the basis of a 2‐fold error range and the bioequivalence range (ie, 0.8 ≤ predicted/observed ≤ 1.25). For all 10 compounds, all predicted‐to‐observed PK ratios were within a 2‐fold error range (n = 27), with two‐thirds of the ratios within the bioequivalence range (n = 18). The findings demonstrate that the pharmacokinetics of these compounds was successfully and adequately predicted in different pediatric age groups. This illustrates the applicability of PBPK for guiding dosing schemes in the pediatric population.

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“…The verified model was used to demonstrate the lack of effects of acid reducing agents on the drug exposure of saxagliptin (Dong et al., 2020). In another study (Miao et al., 2020), the PBPK model was developed for a putative BCS Class I/III drug, oseltamivir phosphate and its metabolite oseltamivir carboxylate in both adults and pediatrics. Virtual BE simulations were conducted to establish the BE dissolution safe space for oseltamivir phosphate in both adults and pediatrics.…”

Section: Current Scientific Considerations For Supporting Bcs III Drug Waiver and Modeling Bcs Iii Drug Absorptionmentioning

confidence: 99%

“…The recently published papers also demonstrated the utility of PBPK absorption modeling and simulation to support the pharmacokinetic evaluation for BCS Class III Drugs (Dong et al., 2020; Miao et al., 2020). A PBPK model for a BCS class III drug, saxagliptin, has been developed and optimized after optimization of permeability and intersystem extrapolation factor (ISEF).…”

Section: Current Scientific Considerations For Supporting Bcs III Drug Waiver and Modeling Bcs Iii Drug Absorptionmentioning

confidence: 99%

Scientific considerations to move towards biowaiver for biopharmaceutical classification system class III drugs: How modeling and simulation can help

Cristofoletti

Zhao

et al. 2021

Biopharm & Drug Disp

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The 2017 Guidance by U.S. Food and Drug Administration (FDA) has recommended the criteria to qualify for a Biopharmaceutical Classification System (BCS)-based biowaiver that includes high solubility of the drug across the physiological pH range as well as the formulation considerations, e.g., being qualitatively the same and quantitatively very similar to the reference product. These were ratified by the International Council for Harmonization (ICH) in 2018. The FDA has used the similar verbiage when referring to the BCS-based biowaiver option for BCS class III drugs (highly soluble but poorly permeable). However, establishing in vitro-in vivo correlations (IVIVC) using conventional mass balance deconvolution approaches, which assumes a single absorption compartment, is not likely for very rapidly dissolving dosage forms containing BCS III drugs. Unlike conventional mass balance deconvolution techniques, physiologically based pharmacokinetic models are able to disentangle different processes contributing to the input function, e.g., dissolution, gastrointestinal transit, and permeation and to establish IVIVC using variants of the compartmental absorption and transit model, supporting biowaiver for formulations containing BCS III drugs. However, there are knowledge gaps that need to be filled.This review provides a systematic assessment of the advancements in applications of physiologically based pharmacokinetic (PBPK) models for IVIVC and biowaiver for such cases with the aim of identifying the most important gaps and hurdles. It concludes by calling for research efforts on the impact of excipients on dissolution and permeation, alongside the development of PBPK modeling to link these in vitro characteristics to in vivo bioequivalence outcomes through simulations of virtual clinical studies

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Using a Physiologically Based Pharmacokinetic Absorption Model to Establish Dissolution Bioequivalence Safe Space for Oseltamivir in Adult and Pediatric Populations

Cited by 26 publications

References 32 publications

Application of physiologically based biopharmaceutics modeling to understand the impact of dissolution differences on in vivo performance of immediate release products: The case of bisoprolol

Application of physiologically based biopharmaceutics modeling to understand the impact of dissolution differences on in vivo performance of immediate release products: The case of bisoprolol

Predictive Performance of Physiology‐Based Pharmacokinetic Dose Estimates for Pediatric Trials: Evaluation With 10 Bayer Small‐Molecule Compounds in Children

Scientific considerations to move towards biowaiver for biopharmaceutical classification system class III drugs: How modeling and simulation can help

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