Requirements to Establishing Confidence in Physiologically Based Pharmacokinetic (PBPK) Models and Overcoming Some of the Challenges to Meeting Them

Requirements to Establishing Confidence in Physiologically Based Pharmacokinetic (PBPK) Models and Overcoming Some of the Challenges to Meeting Them

Authors: Peters SA, Dolgos H
Publication: Clin Pharmacokinet
Software: GastroPlus®

When scientifically well-founded, the mechanistic basis of physiologically based pharmacokinetic (PBPK) models can help reduce the uncertainty and increase confidence in extrapolations outside the studied scenarios or studied populations.

Overview of Brazilian Requirements for Therapeutic Equivalence of Orally Inhaled and Nasal Drug Products

Overview of Brazilian Requirements for Therapeutic Equivalence of Orally Inhaled and Nasal Drug Products

Publication: AAPS PharmSciTech
Division: PBPK

Brazil has established a framework for provision of generic pharmaceuticals including for orally inhaled and nasal drug products (OINDP) to its populace.

Stability behaviour of antiretroviral drugs and their combinations. 10: LC-HRMS, LC-MSn, LC-NMR and NMR characterization of fosamprenavir degradation products and in silico determination of their ADMET properties

Stability behaviour of antiretroviral drugs and their combinations. 10: LC-HRMS, LC-MSn, LC-NMR and NMR characterization of fosamprenavir degradation products and in silico determination of their ADMET properties

Publication: Eur J Pharm Biopharm
Software: ADMET Predictor®

The present study focused upon the forced degradation behaviour of fosamprenavir (FPV), an antiretroviral drug. A total of six degradation products (DPs) were separated on a non-polar stationary phase by high performance liquid chromatography (HPLC).

Impact of Intracellular Concentrations on Metabolic Drug-Drug Interaction Studies

Impact of Intracellular Concentrations on Metabolic Drug-Drug Interaction Studies

Publication: AAPS J
Software: ADMET Predictor®

Accurate prediction of drug-drug interactions (DDI) is a challenging task in drug discovery and development. It requires determination of enzyme inhibition in vitro which is highly system-dependent for many compounds.

A focus on riociguat in the treatment of pulmonary arterial hypertension

A focus on riociguat in the treatment of pulmonary arterial hypertension

Publication: Basic Clin Pharmacol Toxicol
Software: ADMET Predictor®

Current treatment of pulmonary arterial hypertension (PAH) targets three signalling pathways: the nitric oxide (NO) pathway, the endothelin pathway and...

“Development of Fixed Dose Combination Products” Workshop Report: Considerations of Gastrointestinal Physiology and Overall Development Strategy

“Development of Fixed Dose Combination Products” Workshop Report: Considerations of Gastrointestinal Physiology and Overall Development Strategy

Publication: AAPS J
Software: GastroPlus®

The gastrointestinal (GI) tract is one of the most popular and used routes of drug product administration due to the convenience for better patient compliance and reduced costs to the patient compared to other routes.

Investigation of potent inhibitors of cholinesterase based on thiourea and pyrazoline derivatives: Synthesis, inhibition assay and molecular modeling studies

Investigation of potent inhibitors of cholinesterase based on thiourea and pyrazoline derivatives: Synthesis, inhibition assay and molecular modeling studies

Publication: Bioorg Chem
Software: ADMET Predictor®

Owing to the desperate need of new drugs development to treat Alzheimer's ailment the synthesis of 1-aroyl-3-(5-(4-chlorophenyl)-1,2,4-triazole-3-thioneaminylthioureas (2–6)...

In Silico Design of Dapsone Analogues Effective Towards Enoyl Acyl Carrier Protein Reductase Enzyme of Mycrobacterium Leprae

In Silico Design of Dapsone Analogues Effective Towards Enoyl Acyl Carrier Protein Reductase Enzyme of Mycrobacterium Leprae

Publication: World J Pharm Res
Software: ADMET Predictor®

A series of new antileprotic drugs targeting enoyl acyl carrier protein reductase (ENR) enzyme of Mycobacterium lepraewere designed by in silico techniques.

Insights into DPI sensitivity to humidity: An integrated in-vitro-in-silico risk-assessment

Insights into DPI sensitivity to humidity: An integrated in-vitro-in-silico risk-assessment

Publication: J Drug Deliv Sci Technol
Software: GastroPlus®

Dry powder inhalers (DPIs) are known to be sensitive to humidity. Erroneous storage of these products by patients in high humidity environments, could present a potential risk.

Toward the establishment of a standardized pre-clinical porcine model to predict food effects – Case studies on fenofibrate and paracetamol

Toward the establishment of a standardized pre-clinical porcine model to predict food effects – Case studies on fenofibrate and paracetamol

Publication: Int J Pharm
Software: GastroPlus®, PKPlus™

A preclinical porcine model that reliably predicts human food effect of fenofibrate was developed. Fenofibrate was administered to pigs as model compound with a positive food effect.

Solidified SNEDDS for the oral delivery of rifampicin: Evaluation, proof of concept, in vivo kinetics, and in silico GastroPlusTM simulation

Solidified SNEDDS for the oral delivery of rifampicin: Evaluation, proof of concept, in vivo kinetics, and in silico GastroPlusTM simulation

Publication: Int J Pharm

The present investigation was performed to develop a rifampicin (RIF)-loaded solidified self-nanoemulsifying drug delivery system (SNEDDS) (solidified RIF-OF1) for in vitro and in vivo evaluations.