Age related biorelevant dissolution testing for paediatric formulations

Mencarelli, Giovanna; Jones, John W.; Brown, Jonathan; Timmins, Peter; Fotaki, Nikoletta

doi:10.1016/j.ijpharm.2017.08.015

Cited by 2 publications

(2 citation statements)

References 3 publications

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“…The same USP IV biorelevant set‐up for the fasted state was utilised to investigate age‐related differences in the dissolution performance of Tegretol ® 200 mg tablets . Paediatric biorelevant media developed by Maharaj et al .…”

Section: In Vitro Evaluation Of Drug Products For Paediatricsmentioning

confidence: 99%

“…An age‐dependent dissolution profile of carbamazepine from Tegretol ® tablet was observed in the two studied paediatric groups revealing the impact of the GI differences (fluid composition and transition times) between the age groups on dissolution. Furthermore, the use of the closed‐loop mode for the simulation of dissolution in the gastric compartment resulted in a higher discrimination of the dissolution profiles between the two age groups …”

Section: In Vitro Evaluation Of Drug Products For Paediatricsmentioning

confidence: 99%

See 1 more Smart Citation

Biopharmaceutical considerations in paediatrics with a view to the evaluation of orally administered drug products – a PEARRL review

Guimarães

Statelova

Holm

et al. 2018

Journal of Pharmacy and Pharmacology

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Section: In Vitro Evaluation Of Drug Products For Paediatricsmentioning

confidence: 99%

Section: In Vitro Evaluation Of Drug Products For Paediatricsmentioning

confidence: 99%

Biopharmaceutical considerations in paediatrics with a view to the evaluation of orally administered drug products – a PEARRL review

Guimarães

Statelova

Holm

et al. 2018

Journal of Pharmacy and Pharmacology

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Integration of Biorelevant Pediatric Dissolution Methodology into PBPK Modeling to Predict In Vivo Performance and Bioequivalence of Generic Drugs in Pediatric Populations: a Carbamazepine Case Study

Pawar

Zhao

et al. 2023

AAPS J

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This study investigated the impact of gastro-intestinal fluid volume and bile salt (BS) concentration on the dissolution of carbamazepine (CBZ) immediate release (IR) 100 mg tablets and to integrate these in vitro biorelevant dissolution profiles into physiologically based pharmacokinetic modelling (PBPK) in pediatric and adult populations to determine the biopredictive dissolution profile. Dissolution profiles of CBZ IR tablets (100 mg) were generated in 50–900 mL biorelevant adult fasted state simulated gastric and intestinal fluid (Ad-FaSSGF and Ad-FaSSIF), also in three alternative compositions of biorelevant pediatric FaSSGF and FaSSIF medias at 200 mL. This study found that CBZ dissolution was poorly sensitive to changes in the composition of the biorelevant media, where dissimilar dissolution (F2 = 46.2) was only observed when the BS concentration was changed from 3000 to 89 μM (Ad-FaSSIF vs Ped-FaSSIF 50% 14 BS). PBPK modeling demonstrated the most predictive dissolution volume and media composition to forecast the PK was 500 mL of Ad-FaSSGF/Ad-FaSSIF media for adults and 200 mL Ped-FaSSGF/FaSSIF media for pediatrics. A virtual bioequivalence simulation was conducted by using Ad-FaSSGF and/or Ad-FaSSIF 500 mL or Ped-FaSSGF and/or Ped-FaSSIF 200 mL dissolution data for CBZ 100 mg (reference and generic test) IR product. The CBZ PBPK models showed bioequivalence of the product. This study demonstrates that the integration of biorelevant dissolution data can predict the PK profile of a poorly soluble drug in both populations. Further work using more pediatric drug products is needed to verify biorelevant dissolution data to predict the in vivo performance in pediatrics. Graphical Abstract

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Age related biorelevant dissolution testing for paediatric formulations

Cited by 2 publications

References 3 publications

Biopharmaceutical considerations in paediatrics with a view to the evaluation of orally administered drug products – a PEARRL review

Biopharmaceutical considerations in paediatrics with a view to the evaluation of orally administered drug products – a PEARRL review

Integration of Biorelevant Pediatric Dissolution Methodology into PBPK Modeling to Predict In Vivo Performance and Bioequivalence of Generic Drugs in Pediatric Populations: a Carbamazepine Case Study

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