PEGylated y-tocotrienol isomer of vitamin E: Synthesis, characterization, in vitro cytotoxicity, and oral bioavailability

PEGylated y-tocotrienol isomer of vitamin E: Synthesis, characterization, in vitro cytotoxicity, and oral bioavailability

Publication: Eur J Pharm Biopharm
Software: GastroPlus®

Vitamin E refers to a family of eight isomers divided into two subgroups, tocopherols and the therapeutically active tocotrienols (T3).

Modeling and Simulation to Support Clinical Development of Eslicarbazepine Acetate in Partial-Onset Epilepsy

Modeling and Simulation to Support Clinical Development of Eslicarbazepine Acetate in Partial-Onset Epilepsy

Conference: ACCP

Eslicarbazepine acetate (ESL) is a once-daily (QD) oral antiepileptic drug (AED) approved by the US Food and Drug Administration for the treatment of partial-onset seizures (POS) as monotherapy or…

Preclinical pharmacokinetic studies of 3-deazaneplanocin A, a potent epigenetic anticancer agent, and its human pharmacokinetic prediction using GastroPlus™

Preclinical pharmacokinetic studies of 3-deazaneplanocin A, a potent epigenetic anticancer agent, and its human pharmacokinetic prediction using GastroPlus™

Publication: Eur J Pharm Sci
Software: GastroPlus®

DZNep is a potential epigenetic drug, and exerts potent anti-proliferative and pro-apoptotic effects on broad-spectrum carcinomas via disruption of the EZH2 pathway.

Regulatory Considerations for Approval of Generic Inhalation Drug Products in the US, EU, Brazil, China, and India

Regulatory Considerations for Approval of Generic Inhalation Drug Products in the US, EU, Brazil, China, and India

Publication: AAPS J
Division: PBPK

This article describes regulatory approaches for approval of "generic" orally inhaled drug products (OIDPs) in the United States, European Union, Brazil, China and India.

Deciphering nifedipine in vivo delivery from modified release dosage forms: Identification of food effect

Deciphering nifedipine in vivo delivery from modified release dosage forms: Identification of food effect

Publication: ACTA Pharm
Software: GastroPlus®

With the increased reliance on in vitro dissolution testing as an indicator of in vivo drug behavior and the trend towards the in silico modeling of dosage form performance, the need for bioperformance...

Prospective Predictions of Human Pharmacokinetics for Eighteen Compounds

Prospective Predictions of Human Pharmacokinetics for Eighteen Compounds

Publication: J Pharm Sci
Software: GastroPlus®

Quantitative predictions of pharmacokinetics (PKs) and concentration-time profiles using in vitro and in vivo preclinical data are critical to estimate systemic exposures for first-in-human studies.

Application of Absorption Modeling in Rational Design of Drug Product Under Quality-by-Design Paradigm

Application of Absorption Modeling in Rational Design of Drug Product Under Quality-by-Design Paradigm

Authors: Kesisoglou F, Mitra A
Publication: AAPS J
Software: GastroPlus®

Physiologically based absorption models can be an important tool in understanding product performance and hence implementation of Quality by Design (QbD) in drug product development.

Application of Physiologically Based Absorption Modeling for Amphetamine Salts Drug Products in Generic Drug Evaluation

Application of Physiologically Based Absorption Modeling for Amphetamine Salts Drug Products in Generic Drug Evaluation

Authors: Babiskin AH, Zhang X
Publication: J Pharm Sci
Software: GastroPlus®

Amphetamine (AMP) salts-based extended-release (ER) drug products are widely used for the treatment of attention deficit hyperactivity disorder.

Discovery of new acetylcholinesterase inhibitors with small core structures through shape-based virtual screening

Discovery of new acetylcholinesterase inhibitors with small core structures through shape-based virtual screening

Authors: Chen Y, Liu Z, Fu T, Li W, Xu X, Sun H
Publication: Bioorg Med Chem Lett.
Software: ADMET Predictor®

Targeting acetylcholinesterase (AChE) using small molecule inhibitors is considered to be the most successful therapeutic strategy in the treatment of Alzheimer’s disease (AD).

Prediction of pH dependent absorption using in vitro, in silico, and in vivo rat models: Early liability assessment during lead optimization

Prediction of pH dependent absorption using in vitro, in silico, and in vivo rat models: Early liability assessment during lead optimization

Publication: Eur J Pharm Sci
Software: GastroPlus®

Weakly basic compounds which have pH dependent solubility are liable to exhibit pH dependent absorption. In some cases, a subtle change in gastric pH can significantly modulate the plasma concentration of...