Journal ArticleDOI
Cyclodextrin-water soluble polymer ternary complexes enhance the solubility and dissolution behaviour of poorly soluble drugs. Case example: Itraconazole
TLDR
The newly developed physiologically based pharmacokinetic (PBPK) in silico model predicted that the bioavailability of itraconazole is likely to be increased after oral administration of ternary complex formulations, especially when it raconazoles is formulated as a ternARY complex comprising HP-β-CD or HBen-β -CD and Soluplus®.About:
This article is published in European Journal of Pharmaceutics and Biopharmaceutics.The article was published on 2013-04-01. It has received 106 citations till now. The article focuses on the topics: Solubility & Itraconazole.read more
Citations
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Journal ArticleDOI
PBPK models for the prediction of in vivo performance of oral dosage forms
Edmund Kostewicz,Leon Aarons,Martin Bergstrand,Michael B. Bolger,Aleksandra Galetin,Oliver Hatley,Masoud Jamei,Richard Lloyd,Xavier Pepin,Amin Rostami-Hodjegan,Erik Sjögren,Christer Tannergren,David B. Turner,Christian Wagner,Werner Weitschies,Jennifer B. Dressman +15 more
TL;DR: It is expected that the "innovative" integration of in vitro data from more appropriate in vitro models and the enhancement of the GI physiology component of PBPK models, arising from the OrBiTo project, will lead to a significant enhancement in the ability of P BPK models to successfully predict oral drug absorption and advance their role in preclinical and clinical development, as well as for regulatory applications.
Journal ArticleDOI
Cyclodextrins in pharmaceutical formulations I: structure and physicochemical properties, formation of complexes, and types of complex
TL;DR: The physical chemical properties of various cyclodextrins are discussed, including the effects of substitutions on these properties, as well as the regulatory status of their use, commercial products containing cyclodeXTrins, toxicological considerations, and the forces involved in complex formation.
Journal ArticleDOI
Cyclodextrins in pharmaceutical formulations II: solubilization, binding constant, and complexation efficiency.
TL;DR: This work focuses on the solubilization of drugs by complexation, and discusses the determination and significance of binding constants for cyclodextrin complexes, and the determination of complexation efficiency and factors that influence it.
Journal ArticleDOI
Paediatric oral biopharmaceutics: key considerations and current challenges.
TL;DR: It is demonstrated that further work is required to adequately characterise the paediatric gastrointestinal tract to ensure that biopharmaceutics tools are appropriate to predict performance within this population.
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PBPK Models for CYP3A4 and P-gp DDI Prediction: A Modeling Network of Rifampicin, Itraconazole, Clarithromycin, Midazolam, Alfentanil, and Digoxin.
Nina Hanke,Sebastian Frechen,Daniel Moj,Hannah Britz,Thomas Eissing,Thomas Wendl,Thorsten Lehr +6 more
TL;DR: This study provides whole‐body P BPK models of rifampicin, itraconazole, clarithromycin, midazolam, alfentanil, and digoxin within the Open Systems Pharmacology (OSP) Suite and lays a cornerstone for the qualification of the OSP platform with regard to reliable PBPK predictions of enzyme‐mediated and transporter‐mediated DDIs during model‐informed drug development.
References
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Journal ArticleDOI
A Theoretical Basis for a Biopharmaceutic Drug Classification: The Correlation of in Vitro Drug Product Dissolution and in Vivo Bioavailability
TL;DR: A biopharmaceutics drug classification scheme for correlating in vitro drug product dissolution and in vivo bioavailability is proposed based on recognizing that drug dissolution and gastrointestinal permeability are the fundamental parameters controlling rate and extent of drug absorption.
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Improving drug solubility for oral delivery using solid dispersions.
TL;DR: The historical background and definitions of the various systems including eutectic mixtures, solid dispersions and solid solutions, as well as the production, the different carriers and the methods used for the characterization of solid dispersion are outlined.
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Pharmaceutical Applications of Cyclodextrins. 1. Drug Solubilization and Stabilization
TL;DR: The effects of substitution on various cyclodextrins properties and the forces involved in the drug-cyclodextrin complex formation are discussed, and methods which are useful in the optimization of complexation efficacy are reviewed.
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Characteristics and Significance of the Amorphous State in Pharmaceutical Systems
Bruno C. Hancock,George Zografi +1 more
TL;DR: The amorphous state is critical in determining the solid-state physical and chemical properties of many pharmaceutical dosage forms and some of the most common methods that can be used to measure them are described.
Journal ArticleDOI
Cyclodextrin Inclusion Compounds in Research and Industry
TL;DR: As cyclodextrins catalyze several chemical reactions they and their functionalized derivatives provide useful enzyme models and can be used to advantage in the production of pharmaceuticals, pesticides, foodstuffs, and toilet articles.