4.6 Article

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

相关参考文献

注意:仅列出部分参考文献,下载原文获取全部文献信息。
Article Pharmacology & Pharmacy

Performance Evaluation of Montelukast Pediatric Formulations: Part II - a PBPK Modelling Approach

Mariana Guimaraes et al.

Summary: This study aimed to develop a physiologically based pharmacokinetic (PBPK) model coupled with age-appropriate in vitro dissolution data to describe drug performance in adults and pediatric patients. Through two case studies, the study demonstrated how a PBPK absorption modeling strategy can facilitate decision-making and enhance understanding of drug performance in the pediatric population during drug development.

AAPS JOURNAL (2022)

Article Pharmacology & Pharmacy

Proof of Concept in Assignment of Within-Subject Variability During Virtual Bioequivalence Studies: Propagation of Intra-Subject Variation in Gastrointestinal Physiology Using Physiologically Based Pharmacokinetic Modeling

Margareta Bego et al.

Summary: The concept of 'Virtual Bioequivalence' (VBE) is growing using modeling, in vitro tests, and integration of pre-existing data to predict the effects of drugs on the human body. However, building confidence in VBE outcomes requires considering the degree of population variability. Researchers have shown the feasibility of this approach by capturing the confidence interval of pharmacokinetic parameters using physiological pharmacokinetic modeling, but it requires a diverse set of drugs and formulations to determine the variability of physiological parameters.

AAPS JOURNAL (2022)

Review Pharmacology & Pharmacy

Review of paediatric gastrointestinal physiology relevant to the absorption of orally administered medicines

Erik Wollmer et al.

Summary: Despite progress in paediatric drug development, there is a need for better medications for children. This review provides comprehensive data on the ontogeny of gastrointestinal conditions in children, emphasizing the importance of addressing existing data gaps and conducting further research.

ADVANCED DRUG DELIVERY REVIEWS (2022)

Article Pharmacology & Pharmacy

A Physiologically Based Pharmacokinetic Model for Studying the Biowaiver Risk of Biopharmaceutics Classification System Class I Drugs With Rapid Elimination: Dexketoprofen Trometamol Case Study

Xian Zhang et al.

Summary: Biowaiver based on the biopharmaceutics classification system (BCS) is widely used for the approval of new generic drug products. However, some formulations of dexketoprofen trometamol (DEX) tablets failed the first bioequivalence (BE) study. In this study, a physiologically based pharmacokinetic (PBPK) model for DEX was established, and the effects of dissolution, permeability, and gastric emptying time on DEX absorption were examined using sensitivity analyses. The results showed that dissolution rate, permeability, and gastric emptying time were sensitive parameters of C-max. Virtual BE studies conducted on DEX formulations within the biowaiver range showed that dissolution rate changes did not lead to high non-BE ratio, indicating that the risk of C-max is low when generic products satisfy the requirements of biowaiver guideline.

FRONTIERS IN PHARMACOLOGY (2022)

Article Pharmacology & Pharmacy

Gastrointestinal Fluid Volumes in Pediatrics: A Retrospective MRI Study

Matthias Van der Veken et al.

Summary: This study analyzed clinical MRI data of pediatric patients and found that fluid volumes in the stomach, duodenum, jejunum, and small intestine increase with age. Body height and weight were identified as the best estimators for these fluid volumes, but no method performed ideally.

PHARMACEUTICS (2022)

Article Pharmacology & Pharmacy

Characterisation of fasted state gastric and intestinal fluids collected from children

Gopal Pawar et al.

Summary: This study characterized gastric and intestinal fluid from paediatric populations, finding large inter-individual variability in pH, buffer capacity, osmolality, and bile acid concentration. Further research is needed to develop simulated paediatric media and explore their impact on drug solubility and dissolution.

EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS (2021)

Article Pharmacology & Pharmacy

Physiologically Based Pharmacokinetic Modeling Framework to Predict Neonatal Pharmacokinetics of Transplacentally Acquired Emtricitabine, Dolutegravir, and Raltegravir

Xiaomei I. Liu et al.

Summary: This study developed and evaluated a physiologically based pharmacokinetic modeling workflow to predict the disposition of antiretroviral drugs in neonates exposed in utero to pregnant women living with HIV. The models generally captured initial plasma concentrations after birth but underestimated concentrations in the terminal phase. Sensitivity analysis indicated specific enzyme activities in newborns compared to adults.

CLINICAL PHARMACOKINETICS (2021)

Review Chemistry, Medicinal

Biowaiver Monograph for Immediate-Release Solid Oral Dosage Forms: Carbamazepine

Mauricio A. Garcia et al.

Summary: Carbamazepine is a BCS Class 2 drug with high permeability but a narrow therapeutic index, not recommended for a BCS-based biowaiver; USP dissolution conditions effectively differentiate between bioinequivalent products, potentially aiding in predicting bioequivalence of formulations.

JOURNAL OF PHARMACEUTICAL SCIENCES (2021)

Article Pharmacology & Pharmacy

Evaluation of Physiologically Based Pharmacokinetic Models to Predict the Absorption of BCS Class I Drugs in Different Pediatric Age Groups

Xiaomei I. Liu et al.

Summary: This study applied physiologically based pharmacokinetic (PBPK) models to investigate the absorption and pharmacokinetics of BCS class I drugs in pediatric patients, confirming that gastric emptying time is a key factor affecting drug absorption in children.

JOURNAL OF CLINICAL PHARMACOLOGY (2021)

Article Chemistry, Medicinal

Establishing the Bioequivalence Safe Space for Immediate-Release Oral Dosage Forms using Physiologically Based Biopharmaceutics Modeling (PBBM): Case Studies

Tycho Heimbach et al.

Summary: This article discusses five case studies on using physiologically based biopharmaceutics modeling (PBBM) to establish safe spaces for oral drug products. It explores the challenges and methods in developing safe spaces and highlights the need for more case studies to drive the development of best practices.

JOURNAL OF PHARMACEUTICAL SCIENCES (2021)

Article Chemistry, Medicinal

In Vitro Biopharmaceutical Equivalence of Carbamazepine Sodium Tablets Available in Lima, Peru

Angel T. Alvarado et al.

Summary: In this study, the biopharmaceutical equivalence of carbamazepine sodium tablets in Peru was evaluated through in vitro testing, revealing that while the samples met official specifications for quality control tests, they did not demonstrate in vitro biopharmaceutical equivalence with the innovator brand.

DISSOLUTION TECHNOLOGIES (2021)

Article Pharmacology & Pharmacy

Impact of gastrointestinal physiology on drug absorption in special populations – An UNGAP review

Cordula Stillhart et al.

EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES (2020)

Review Pharmacology & Pharmacy

Physiologically-based pharmacokinetic models for children: Starting to reach maturation?

Laurens F. M. Verscheijden et al.

PHARMACOLOGY & THERAPEUTICS (2020)

Article Pharmacology & Pharmacy

Biopharmaceutical implications of excipient variability on drug dissolution from immediate release products

P. Zarmpi et al.

EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS (2020)

Article Medicine, Research & Experimental

Topography of Simulated Intestinal Equilibrium Solubility

Claire Dunn et al.

MOLECULAR PHARMACEUTICS (2019)

Review Pharmacology & Pharmacy

Impact of regional differences along the gastrointestinal tract of healthy adults on oral drug absorption: An UNGAP review

Maria Vertzoni et al.

EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES (2019)

Article Medicine, Research & Experimental

Magnetic Resonance Imaging Quantification of Gastrointestinal Liquid Volumes and Distribution in the Gastrointestinal Tract of Children

Eleni Papadatou-Soulou et al.

MOLECULAR PHARMACEUTICS (2019)

Article Pharmacology & Pharmacy

Gastric fluid composition in a paediatric population: Age-dependent changes relevant for gastrointestinal drug disposition

Jens Van Den Abeele et al.

EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES (2018)

Article Pharmacology & Pharmacy

Interindividual and intraindividual variability of fasted state gastric fluid volume and gastric emptying of water

Michael Grimm et al.

EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS (2018)

Meeting Abstract Pharmacology & Pharmacy

Age related biorelevant dissolution testing for paediatric formulations

G. Mencarelli et al.

INTERNATIONAL JOURNAL OF PHARMACEUTICS (2018)

Article Pharmacology & Pharmacy

Ability of gelatin and BSA to stabilize the supersaturated state of poorly soluble drugs

Timothy Pas et al.

EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS (2018)

Editorial Material Chemistry, Medicinal

FIP Guidelines for Dissolution Testing of Solid Oral Products

Horst Dieter Friedel et al.

JOURNAL OF PHARMACEUTICAL SCIENCES (2018)

Article Pharmacology & Pharmacy

Mathematical prediction of pharmacokinetic parameters-an in-vitro approach for investigating pharmaceutical products for IVIVC

Vaibhav Rastogi et al.

FUTURE JOURNAL OF PHARMACEUTICAL SCIENCES (2018)

Article Medicine, Research & Experimental

Validation of Dissolution Testing with Biorelevant Media: An OrBiTo Study

James Mann et al.

MOLECULAR PHARMACEUTICS (2017)

Article Pharmacology & Pharmacy

Investigating Oral Absorption of Carbamazepine in Pediatric Populations

Philip Kohlmann et al.

AAPS JOURNAL (2017)

Article Chemistry, Multidisciplinary

Assessment of Age-Related Changes in Pediatric Gastrointestinal Solubility

Anil R. Maharaj et al.

PHARMACEUTICAL RESEARCH (2016)

Article Pharmacology & Pharmacy

Advances in the design of fasted state simulating intestinal fluids: FaSSIF-V3

Alexander Fuchs et al.

EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS (2015)

Article Pharmacology & Pharmacy

Development and validation of an HPLC-UV method for the quantification of carbamazepine in rabbit plasma

Hammam A. Mowafy et al.

SAUDI PHARMACEUTICAL JOURNAL (2012)

Article Pharmacology & Pharmacy

Physico-mechanical and Stability Evaluation of Carbamazepine Cocrystal with Nicotinamide

Ziyaur Rahman et al.

AAPS PHARMSCITECH (2011)

Article Immunology

Pharmacokinetics of Lopinavir/Ritonavir Crushed Versus Whole Tablets in Children

Brookie M. Best et al.

JAIDS-JOURNAL OF ACQUIRED IMMUNE DEFICIENCY SYNDROMES (2011)

Article Chemistry, Multidisciplinary

Dissolution media simulating conditions in the proximal human gastrointestinal tract: An update

Ekarat Jantratid et al.

PHARMACEUTICAL RESEARCH (2008)

Article Biochemistry & Molecular Biology

Ontogeny of human hepatic cytochromes P450

Ronald N. Hines

JOURNAL OF BIOCHEMICAL AND MOLECULAR TOXICOLOGY (2007)

Article Chemistry, Medicinal

Towards a universal dissolution medium for carbamazepine

M. A. EL-Massik et al.

DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY (2006)

Review Pharmacology & Pharmacy

Prediction of the clearance of eleven drugs and associated variability in neonates, infants and children

Trevor N. Johnson et al.

CLINICAL PHARMACOKINETICS (2006)

Article Pharmacology & Pharmacy

Simulation of fasting gastric conditions and its importance for the in vivo dissolution of lipophilic compounds

M Vertzoni et al.

EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS (2005)

Article Chemistry, Medicinal

Surfactant-facilitated crystallization of dihydrate carbamazepine during dissolution of anhydrous polymorph

N Rodríguez-Hornedo et al.

JOURNAL OF PHARMACEUTICAL SCIENCES (2004)

Article Pharmacology & Pharmacy

Solution-mediated phase transformation of anhydrous to dihydrate carbamazepine and the effect of lattice disorder

D Murphy et al.

INTERNATIONAL JOURNAL OF PHARMACEUTICS (2002)