Calcium Phosphate Particles as Pulmonary Delivery System for Interferon-α in Mice

Calcium Phosphate Particles as Pulmonary Delivery System for Interferon-α in Mice

Publication: AAPS PharmSciTech
Software: GastroPlus®

Systemically administered interferons are rapidly cleared from the circulation thus requiring frequent dosing to maintain the therapeutic levels of circulating interferon.

Utility of Physiologically Based Pharmacokinetic Absorption Modeling to Predict the Impact of Salt-to-Base Conversion on Prasugrel HCl Product Bioequivalence in the Presence of Proton Pump Inhibitors

Utility of Physiologically Based Pharmacokinetic Absorption Modeling to Predict the Impact of Salt-to-Base Conversion on Prasugrel HCl Product Bioequivalence in the Presence of Proton Pump Inhibitors

Authors: Fan J, Zhang X, Zhao L
Publication: AAPS J

Prasugrel HCl may convert to prasugrel base during manufacturing or storage. It was reported that formulations with different ratios of salt to base were bioequivalent in healthy subjects...

Synthesis and pharmacodynamics of ibuprofen-1-acetoxyethyl ester

Synthesis and pharmacodynamics of ibuprofen-1-acetoxyethyl ester

Publication: Chem Res Chin Univ
Software: ADMET Predictor®

Ibuprofen(IBU) and its derivatives are widely used in treating many diseases, such as depression, glomerulonephritis, fever caused by common cold or influenza, and rheumatoid arthritis.

In vitro–in vivo and pharmacokinetic evaluation of solid lipid nanoparticles of furosemide using Gastroplus™

In vitro–in vivo and pharmacokinetic evaluation of solid lipid nanoparticles of furosemide using Gastroplus™

Publication: RSC Adv
Software: GastroPlus®

In this work, we conducted pharmacokinetic studies and established the in vitro and in vivo correlation (IVIVC) of furosemide (FRS) loaded solid lipid nanoparticles (FSLN).

Prediction of efficacy for conversion from adjunctive therapy to monotherapy with eslicarbazepine acetate 800 mg once daily for partial-onset epilepsy.

Prediction of efficacy for conversion from adjunctive therapy to monotherapy with eslicarbazepine acetate 800 mg once daily for partial-onset epilepsy.

Publication: Clin Pharmacol

Eslicarbazepine acetate (ESL) is a once-daily (QD) oral antiepileptic drug (AED) indicated for partial-onset seizures (POS). Clinical studies of gradual conversion to ESL 1,200 and 1,600 mg QD...

Applications of Mechanistic Modeling and Simulations in Compound and Dosage Forms Selections

Applications of Mechanistic Modeling and Simulations in Compound and Dosage Forms Selections

Authors: Mintah EA
Publication: Mercer University College

Physiologically based pharmacokinetic (PBPK) modeling and simulation techniques have been adopted in the pharmaceutical industry to aid in compound selection and dosage form development in recent years.

Exploring the Feasibility of Biowaiver Extension of BCS Class III Drugs with Site-Specific Absorption Using Gastrointestinal Simulation Technology

Exploring the Feasibility of Biowaiver Extension of BCS Class III Drugs with Site-Specific Absorption Using Gastrointestinal Simulation Technology

Authors: Sun L, Sun J, He Z
Publication: Eur J Drug Metab Pharmacokinet

The US Food and Drug Administration, World Health Organization and European Medicines Agency have allowed biowaiver for some BCS class III drugs, but shortened the requisite dissolution time of BCS...

The impact of reduced gastric acid secretion on dissolution of salts of weak bases in the fasted upper gastrointestinal lumen: Data in biorelevant media and in human aspirates.

The impact of reduced gastric acid secretion on dissolution of salts of weak bases in the fasted upper gastrointestinal lumen: Data in biorelevant media and in human aspirates.

Publication: Eur J Pharm Biopharm
Software: GastroPlus®

To propose media for simulating the intragastric environment under reduced gastric acid secretion in the fasted state at three levels of simulation of the gastric environment and evaluate their...

Substrate and method dependent inhibition of three ABC-transporters (MDR1, BCRP, and MRP2)

Substrate and method dependent inhibition of three ABC-transporters (MDR1, BCRP, and MRP2)

Publication: Eur J Pharm Sci

Drug transport and drug-drug interactions (DDI) with human ABC transporters are generally investigated in mammalian cell lines or inverted membrane vesicles from insect cells (Sf9) overexpressing the transporter of interest.

Mechanistic Modelling of Drug-Induced Liver Injury: Investigating the Role of Innate Immune Responses

Mechanistic Modelling of Drug-Induced Liver Injury: Investigating the Role of Innate Immune Responses

Publication: Gene Regul Syst Bio
Software: DILIsym®

Drug-induced liver injury (DILI) remains an adverse event of significant concern for drug development and marketed drugs, and the field would benefit from better tools to identify liver liabilities early in development and/or to mitigate potential DILI risk in otherwise promising drugs.

Identification of neuron selective androgen receptor inhibitors

Identification of neuron selective androgen receptor inhibitors

Publication: World J Biol Chem

Aim: To identify neuron-selective androgen receptor (AR) signaling inhibitors, which could be useful in the treatment of spinal and bulbar muscular atrophy (SBMA)...

Comparison of oral absorption properties among different bisphosphonates by using a newly developed physiologically based pharmacokinetic model.

Comparison of oral absorption properties among different bisphosphonates by using a newly developed physiologically based pharmacokinetic model.

Authors: Nakai K, Nakamura M
Publication: Therapeutic Research
Software: GastroPlus®

Absorption of bisphosphonates(BPs)from the gastrointestinal tract is inhibited by forming a complex combined with multivalent cation in intake foods.

Comparing Dog and Human Intestinal Fluids: Implications on Solubility and Biopharmaceutical Risk Assessment

Comparing Dog and Human Intestinal Fluids: Implications on Solubility and Biopharmaceutical Risk Assessment

Publication: AAPS PharmSciTech

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

Quantitative analysis of lab-to-lab variability in Caco-2 permeability assays

Publication: Eur J Pharm Biopharm
Software: GastroPlus®

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

Mechanistic investigation of the negative food effect of modified release zolpidem

Publication: Eur J Pharm Sci
Software: GastroPlus®

When administered orally as either an immediate or modified release dosage form, zolpidem demonstrates a negative foodeffect, i.e. decrease in Cmax and AUC.

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 impact of supersaturation level for oral absorption of BCS class IIb drugs, dipyridamole and ketoconazole, using in vivo predictive dissolution system: Gastrointestinal Simulator (GIS)

Publication: Eur J Pharm Sci
Software: GastroPlus®

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

Studies on Core-Shell Nanocapsules of Felodipine: In Vitro-In Vivo Evaluations

Publication: AAPS PharmSciTech
Software: GastroPlus®

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

Identification of novel TACE inhibitors compatible with topical application

Publication: Bioorg Med Chem Lett.
Software: ADMET Predictor®

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...