Despite many documented differences in gut physiology compared to humans, the beagle dog has been successfully used as a preclinical model for assessing the relative bioavailability of dosage forms during formulation development.
Quantitative analysis of lab-to-lab variability in Caco-2 permeability assays
In this study, Caco-2 permeability results from different laboratories were compared. Six different sets of apparent permeability coefficient (Papp) values reported in the literature were...
Mechanistic investigation of the negative food effect of modified release zolpidem
When administered orally as either an immediate or modified release dosage form, zolpidem demonstrates a negative foodeffect, i.e. decrease in Cmax and AUC.
Exploring Canine – Human Differences in Product Performance. Part II: Use of Modeling and Simulation to Explore the Impact of Formulation on Ciprofloxacin In Vivo Absorption and Dissolution in Dogs
This study explored the in vivo performance of three oral ciprofloxacin formulations (oral solution, fast, or slow dissolving tablets) in beagle dogs.
The impact of supersaturation level for oral absorption of BCS class IIb drugs, dipyridamole and ketoconazole, using in vivo predictive dissolution system: Gastrointestinal Simulator (GIS)
The development of formulations and the assessment of oral drug absorption for Biopharmaceutical Classification System (BCS) class IIb drugs is often a difficult issue due to the potential for...
Studies on Core-Shell Nanocapsules of Felodipine: In Vitro-In Vivo Evaluations
The present study aimed for in vitro-in vivo-in silico simulation studies of experimentally designed (32-factorial) Capmul PG-8-cored, Eudragit RSPO-Lutrol F 127 nanocapsules to ferry felodipine using GastroPlus™.
Identification of novel TACE inhibitors compatible with topical application
Targeting the Tumor Necrosis Factor α signalling with antibodies has led to a revolution in the treatment of psoriasis. Locally inhibiting Tumor Necrosis Factor α Converting Enzyme...
Evolution of Circulating Tumor DNA Profile from First-line to Subsequent Therapy in Metastatic Renal Cell Carcinoma
Background: Treatment of metastatic renal cell carcinoma (mRCC) typically entails mechanistically distinct agents across the first- and second-line setting.
Prediction of Losartan Active Carboxylic Acid Metabolite Exposure Following Losartan Administration Using Static and Physiologically-Based Pharmacokinetic Models.
The aim of this study was to evaluate a strategy based on static and dynamic physiologically based pharmacokinetic (PBPK) modeling for the prediction of metabolite and parent drug area under...
Development and qualification of physiologically based pharmacokinetic models for drugs with atypical distribution behavior: A desipramine case study.
Desipramine is a secondary tricyclic amine, which is primarily metabolized by cytochrome 2D6. It shows a high volume of distribution (Vss) (10–50 L/kg) due to its high lipophilicity, unspecific phospholipid binding, and lysosomal trapping.
Food effect: The combined effect of media pH and viscosity on the gastrointestinal absorption of ciprofloxacin tablet
The clinical implications of food-drug interactions may have to be taken seriously into account with oral drugs administration in order to minimize variations in drug bioavailability.
Influence of different proton pump inhibitors on the pharmacokinetics of voriconazole
This study aimed to determine the influence of proton pump inhibitors (PPIs) on the pharmacokinetics of voriconazole and to characterise potential drug-drug interactions (DDIs)...
Systems pharmacology modeling of drug-induced hyperbilirubinemia: Differentiating hepatotoxicity and inhibition of enzymes/transporters
Elevations in serum bilirubin during drug treatment may indicate global liver dysfunction and a high risk of liver failure.
In vitro dissolution models for the prediction of in vivo performance of an oral mesoporous silica formulation
Drug release from mesoporous silica systems has been widely investigated in vitro using USP Type II (paddle) dissolution apparatus.
Mechanistic prediction of food effects for Compound A tablet using PBPK model
Physiologically based pharmacokinetic (PBPK) modeling has been extensively used to study the factors of effect drug absorption, distribution, metabolize and extraction progress in human.
Biopharmaceutics data management system for anonymised data sharing and curation: First application with orbito IMI project
The OrBiTo IMI project was designed to improve the understanding and modelling of how drugs are absorbed.
In silico-in vitro-in vivo studies of experimentally designed carvedilol loaded silk fibroin-casein nanoparticles using physiological based pharmacokinetic model
The study aimed to design and develop carvedilol loaded silk fibroin-casein nanoparticles using 32 full factorial design.
Design and evaluation of an extended-release matrix tablet formulation; the combination of hypromellose acetate succinate and hydroxypropylcellulose
The purpose of this study was to develop an extended-release (ER) matrix tablet that shows robust dissolution properties able to account for the variability of pH and mechanical stress in the GI tract using...
Synthesis, spectral characterization, crystal structure, cytotoxicity and apoptosis—Inducing activity of two derivatives of 2-hydroxy-1,4-naphthaquinone
A phenaxazone compound [5H-Benzo[a]phenoxazin-5-one (BP)] along with an aminoquinone[2-[(o-hydroxyphenyl)amino]-1,4-naphthaquinone (HAN)] derivatives were synthesized from...