In vivo in silico pharmacokinetic simulation studies of carvedilol-loaded nanocapsules using GastroPlus™

In vivo in silico pharmacokinetic simulation studies of carvedilol-loaded nanocapsules using GastroPlus™

Publication: Ther Deliv
Software: GastroPlus®

The study aimed at in vivo pharmacokinetic evaluation of carvedilol loaded nanocapsules (CLN) followed by in silico predictions and establishment of IVIVC. 

Using Physiologically Based Pharmacokinetic (PBPK) Modelling to Gain Insights into the Effect of Physiological Factors on Oral Absorption in Paediatric Populations

Using Physiologically Based Pharmacokinetic (PBPK) Modelling to Gain Insights into the Effect of Physiological Factors on Oral Absorption in Paediatric Populations

Publication: AAPS J

Paediatric pharmaceutics has become an important topic, but currently, there is an incomplete knowledge of paediatric gastrointestinal physiology and adequate biopharmaceutical tools still have to be developed.

Limits of rapid log P determination methods for highly lipophilic and flexible compounds

Limits of rapid log P determination methods for highly lipophilic and flexible compounds

Publication: Analytica Chimica Acta

Lipophilicity is of crucial importance in many fields including pharmaceutical, environmental, cosmetic and food industries.

Integrating Predictions from Complementary Cytochrome P450 (CYP) Models

Integrating Predictions from Complementary Cytochrome P450 (CYP) Models

Conference: BioIT
Software: ADMET Predictor®
Division: PBPK

Many structure-activity classification models have been published for predicting whether a given compound is likely to inhibit and/or be subject to metabolism by a given cytochrome P450 (CYP) isoform, and...

Febrifugine analogues as Leishmania donovani trypanothione reductase inhibitors: binding energy analysis assisted by molecular docking, ADMET and molecular dynamics simulation

Febrifugine analogues as Leishmania donovani trypanothione reductase inhibitors: binding energy analysis assisted by molecular docking, ADMET and molecular dynamics simulation

Publication: J Biomol Struct Dyn

Visceral leishmaniasis affects people from 70 countries worldwide, mostly from Indian, African and south American continent. The increasing resistance to antimonial, miltefosine and frequent toxicity of...

pH-Dependent Solubility and Dissolution Behavior of Carvedilol-Case Example of a Weakly Basic BCS Class II Drug

pH-Dependent Solubility and Dissolution Behavior of Carvedilol-Case Example of a Weakly Basic BCS Class II Drug

Publication: AAPS PharmSciTech
Software: GastroPlus®

The objective of this study was to investigate the pH-dependent solubility and dissolution of weakly basic Biopharmaceutical Classification Systems (BCS) class II drugs, characterized by low solubility...

Simulated rat intestinal fluid improves oral exposure prediction for poorly soluble compounds over a wide dose range

Simulated rat intestinal fluid improves oral exposure prediction for poorly soluble compounds over a wide dose range

Publication: ADMET DMPK
Software: ADMET Predictor®

Solubility can be the absorption limiting factor for drug candidates and is therefore a very important input parameter for oral exposure prediction of compounds with limited solubility.

Advantage of the Dissolution / Permeation System for Estimating Oral Absorption of Drug Candidates in the Drug Discovery Stage

Advantage of the Dissolution / Permeation System for Estimating Oral Absorption of Drug Candidates in the Drug Discovery Stage

Publication: Mol Pharm

In order to increase the success rate in the development of oral drugs, an in vitro method, which can accurately estimate human oral absorption of a large variety of compounds from solid formulations...

Novel nonquaternary reactivators showing reactivation efficiency for soman-inhibited human acetylcholinesterase

Novel nonquaternary reactivators showing reactivation efficiency for soman-inhibited human acetylcholinesterase

Publication: Toxicol Lett

Soman is a highly toxic nerve agent with strong inhibition of acetylcholinesterase (AChE), but of the few reactivators showing antidotal efficiency for soman-inhibited AChE presently are all...

Software and Web Resources for Computer-Aided Molecular Modeling and Drug Discovery

Software and Web Resources for Computer-Aided Molecular Modeling and Drug Discovery

Publication: Chemometrics Applications and Research: QSAR in Medicinal Chemistry

Computer-aided molecular modeling and drug design plays a crucial role in drug discovery and has become an essential tool in the pharmaceutical industry.

Synthesis and Evaluation of Novel Radioligands Based on 3-[5-(Pyridin-2-yl)-2H-tetrazol-2-yl]benzonitrile for Positron Emission Tomography Imaging of Metabotropic Glutamate Receptor Subtype 5

Synthesis and Evaluation of Novel Radioligands Based on 3-[5-(Pyridin-2-yl)-2H-tetrazol-2-yl]benzonitrile for Positron Emission Tomography Imaging of Metabotropic Glutamate Receptor Subtype 5

Publication: J Med Chem

We found out 3-[5-(pyridin-2-yl)-2H-tetrazol-2-yl]benzonitrile analogues as the candidate for positron emission tomography (PET) imaging agents of metabotropic glutamate receptor subtype 5 (mGluR5).