To visualize fatty acid amide hydrolase (FAAH) in brain in vivo, we developed a novel positron emission tomography (PET) ligand N-(3,4-dimethylisoxazol-5-yl)piperazine-4-[4-(2-fluoro...
Provenance of Computers in Pharmacy
Computers in pharmacy are used for the information of drug data, records and files, drug management (creating, modifying, adding and deleting data in patient files to generate reports), business details.
Utility of PBPK Absorption Modeling to Guide Modified Release Formulation Development of Gaboxadol, a Highly Soluble Compound with Region-Dependent Absorption
Given the complexity of controlled release (CR) formulations, selecting the right preclinical tools is important to enable decision making on the in vivo performance of these formulations during development.
Effects of Cytochrome P450 3A4 Inhibitors – Ketoconazole and Erythromycin – on Bitopertin Pharmacokinetics and Comparison with Physiologically Based Modelling Predictions
To assess the effect of strong and moderate cytochrome P450 (CYP) 3A4 inhibition on exposure of bitopertin, a glycine reuptake inhibitor primarily metabolized by CYP3A4, and to...
Development of In Vitro In Vivo Correlation Models For Clopidogrel Tablets To Describe Administration Under Fasting And Fed Conditions
The dissolution profiles of clopidogrel 75 mg tablets in compendial gastric and intestinal media as well as in biorelevant simulated gastric and intestinal media mimicking fasting and fed conditions were determined.
Sandwich-Cultured Hepatocytes as a Tool to Study Drug Disposition and Drug-Induced Liver Injury
Sandwich-cultured hepatocytes (SCH) are metabolically competent and have proper localization of basolateral and canalicular transporters with functional bile networks.
In vitro anticancer properties and biological evaluation of novel natural alkaloid jerantinine B
Natural products play a pivotal role in medicine especially in the cancer arena. Many drugs that are currently used in cancer chemotherapy originated from or were inspired by nature.
Absorption, distribution, metabolism, excretion, and kinetics of 2,3,3,3-tetrafluoro-2- (heptafluoropropoxy) proprionic acid ammonium salt following a single dose in rat, mouse, and cynomolgus monkey
Ammonium, 2,3,3,3-tetrafluoro-2-(heptafluoropropoxy)-propanoate has been developed as a processing aid used in the manufacture of fluoropolymers.
Simulations Plus Reports First Quarter FY2016 Financial Results
Consolidated net revenues up 18.4%; net income increased 109%
Evaluations of imidazolium ionic liquids as novel skin permeation enhancers for drug transdermal delivery
In this work, imidazolium ionic liquids (imidazolium ILs) were employed as the novel chemical permeation enhancers (CPEs) and their performances and mechanisms of action were deeply investigated.
Simulations Plus Sets Date for 1st Quarter 2016 Earnings Release and Conference Call
Conference Call to be on Thursday, January 14, at 4:15 PM ET
Some factors that can lead to poor peak shape in hydrophilic interaction chromatography, and possibilities for their remediation
Some factors which present difficulties for obtaining good peak shape in hydrophilic interaction chromatography (HILIC) were studied.
Identification of Novel Potential Inhibitors of Aldose Reductase: A Multistage Computational Filtering Approach
The aldose reductase (AR) is a rate limiting enzyme in the polyol pathway, for the conversion of glucose to sorbitol. The identification of a potent inhibitor is the need of the hour.
A Workflow to Investigate Exposure and Pharmacokinetic Influences on High-Throughput in Vitro Chemical Screening Based on Adverse Outcome Pathways
Adverse outcome pathways (AOPs) link adverse effects in individuals or populations to a molecular initiating event (MIE) that can be quantified using in vitro methods.
Comparison of biorelevant simulated media mimicking the intestinal environment to assess the solubility profiles of poorly soluble drugs
During the discovery stage in lead identification/optimization, compounds are characterized for their solubilities in biorelevant media and these data are often used to model the in vivo behavior of...
Using Physiologically Based Pharmacokinetic Modeling for in vitro – in vivo Extrapolation to Predict Chemical Exposure
Mechanistic absorption and physiologically based pharmacokinetic (MA/ PBPK) models are useful tools in risk assessment. These models incorporate complex processes related to a compound’s disposition...
Absorption, Metabolism, Excretion, and the Contribution of Intestinal Metabolism to the Oral Disposition of [14C]Cobimetinib, a MEK Inhibitor, in Humans
The pharmacokinetics, metabolism, and excretion of cobimetinib, a MEK inhibitor, were characterized in healthy male subjects (n = 6) following a single 20 mg (200 μCi) oral dose.