Challenges in translational drug research in neuropathic and inflammatory pain: the prerequisites for a new paradigm

Challenges in translational drug research in neuropathic and inflammatory pain: the prerequisites for a new paradigm

Publication: Eur J Clin Pharmacol
Division: PBPK

Despite an improved understanding of the molecular mechanisms of nociception, existing analgesic drugs remain limited in terms of efficacy in chronic conditions, such as neuropathic pain.

Looking to the future of drug-induced liver injury: an interview with Paul B Watkins

Looking to the future of drug-induced liver injury: an interview with Paul B Watkins

Authors: Watkins PB
Publication: Future Sci OA
Software: DILIsym®

Paul Watkins talks to Francesca Lake, Head of Open Access Publishing: Paul is The Howard Q Ferguson Professor in the Eshelman School of Pharmacy at The University of North Carolina at Chapel Hill (UNC, NC, USA), and an expert in drug safety and drug-induced liver injury (DILI).

Population Pharmacokinetic Evaluation and Missed-Dose Simulations for Eslicarbazepine Acetate Monotherapy in Patients With Partial-Onset Seizures

Population Pharmacokinetic Evaluation and Missed-Dose Simulations for Eslicarbazepine Acetate Monotherapy in Patients With Partial-Onset Seizures

Publication: Clin Pharmacol Drug Dev

Given the potential consequences of antiepileptic therapy nonadherence, missed-dose scenarios of 12- to 48-hour dose delays (4-hour intervals) for eslicarbazepine acetate monotherapy...

In vitro and in vivo evaluation of gastro-retentive carvedilol loaded chitosan beads using GastroPlus™

In vitro and in vivo evaluation of gastro-retentive carvedilol loaded chitosan beads using GastroPlus™

Publication: Int J Biol Macromol
Software: GastroPlus®

The objective of present investigation was to develop gastro-retentive controlled release system of carvedilol using biological macromolecule, chitosan. 32 full factorial design was adopted for...

Population Pharmacokinetic and Pharmacodynamic Modeling of LY2510924 in Patients with Advanced Cancer.

Population Pharmacokinetic and Pharmacodynamic Modeling of LY2510924 in Patients with Advanced Cancer.

Publication: CPT Pharmacometrics Syst Pharmacol

The objectives of this study were to characterize the pharmacokinetics (PK) of LY2510924, a potent peptide antagonist of the CXCR4 receptor, after subcutaneous administration in patients with...

Biorelevant Dissolution Models for a Weak Base To Facilitate Formulation Development and Overcome Reduced Bioavailability Caused by Hypochlordyria or Achlorhydria.

Biorelevant Dissolution Models for a Weak Base To Facilitate Formulation Development and Overcome Reduced Bioavailability Caused by Hypochlordyria or Achlorhydria.

Publication: Mol Pharm
Software: GastroPlus®

In this study, two dissolution models were developed to achieve in vitro–in vivo relationship for immediate release formulations of Compound-A, a poorly soluble weak base with pH-dependent...

Synthesis, antioxidant, antifungal, molecular docking and ADMET studies of some thiazolyl hydrazones

Synthesis, antioxidant, antifungal, molecular docking and ADMET studies of some thiazolyl hydrazones

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

Some thiazolyl hydrazones were synthesized by one pot reaction of thiophene-2-carbaldehyde or 2, 4-dichlorobenzaldehyde, thiosemicarbazide and various phenacyl bromides which were preliminarily...

Mathematical model reveals role of nucleotide signaling in airway surface liquid homeostasis and its dysregulation in cystic fibrosis

Mathematical model reveals role of nucleotide signaling in airway surface liquid homeostasis and its dysregulation in cystic fibrosis

Publication: Proceedings of the National Academy of Sciences
Division: PBPK
Therapeutic Areas: Pulmonary

Mucociliary clearance is composed of three components (i.e., mucin secretion, airway surface hydration, and ciliary-activity) which function coordinately to clear inhaled microbes and other foreign particles from airway surfaces.

In Silico Absorption Analysis of Valacyclovir in Wildtype and Pept1 Knockout Mice Following Oral Dose Escalation

In Silico Absorption Analysis of Valacyclovir in Wildtype and Pept1 Knockout Mice Following Oral Dose Escalation

Authors: Yang B, Smith DE
Publication: Pharm Res
Software: GastroPlus®

We developed simulation and modeling methods to predict the in vivo pharmacokinetic profiles of acyclovir, following escalating oral doses of valacyclovir, in wildtype and Pept1knockout mice.

Lipophilic salts of poorly soluble compounds to enable high-dose lipidic SEDDS formulations in drug discovery

Lipophilic salts of poorly soluble compounds to enable high-dose lipidic SEDDS formulations in drug discovery

Publication: Eur J Pharm Biopharm
Software: GastroPlus®

Self-emulsifying drug delivery systems (SEDDS) have been used to solubilize poorly water-soluble drugs to improve exposure in high-dose pharmacokinetic (PK) and toxicokinetic (TK) studies.

In silico prediction of skin metabolism and its implication in toxicity assessment

In silico prediction of skin metabolism and its implication in toxicity assessment

Publication: Computational Toxicology
Software: ADMET Predictor®

Skin, being the largest organ of the body, represents an important route of exposure, not only for the abundance of chemicals present in the environment, but also for...

Integrating in vitro, modeling, and in vivo approaches to investigate warfarin bioequivalence

Integrating in vitro, modeling, and in vivo approaches to investigate warfarin bioequivalence

Publication: CPT Pharmacometrics Syst Pharmacol
Software: GastroPlus®

We demonstrate the use of modeling and simulation to investigate bioequivalence concerns raised about generic warfarin products.

Identification and characterisation of a salt form of Danirixin with reduced pharmacokinetic variability in patient populations

Identification and characterisation of a salt form of Danirixin with reduced pharmacokinetic variability in patient populations

Publication: Eur J Pharm Biopharm
Software: GastroPlus®

The natural variability of gastric pH or gastric acid reducing medications can result in lower and more variable clinical pharmacokinetics for basic compounds in patient populations.