Practical Anticipation of Human Efficacious Doses and Pharmacokinetics Using In Vitro and Preclinical In Vivo Data

Practical Anticipation of Human Efficacious Doses and Pharmacokinetics Using In Vitro and Preclinical In Vivo Data

Authors: Heimbach T, Lakshminarayana SB, Hu W, He H
Publication: AAPS J
Keywords: dose-response, drug design, drug relationship, humans, in vitro techniques, pharmacokinetics
Software: GastroPlus®

Accurate predictions of human pharmacokinetic and pharmacodynamic (PK/PD) profiles are critical in early drug development, as safe, efficacious, and "developable" dosing...

The use of gastrointestinal intubation studies for controlled release development

The use of gastrointestinal intubation studies for controlled release development

Authors: Sutton SC
Publication: Br J Clin Pharmacol
Keywords: administration and dosage, animals, colon physiology, dogs, gastrointestinal, humans, intestinal absorption, permeability, solubility
Software: GastroPlus®

This review describes clinical results of gastrointestinal intubation studies of eight controlled release (CR) candidates under development during the 1990s and offer

Population pharmacokinetic analysis of linezolid in patients with infectious disease: application to lower body weight and elderly patients

Population pharmacokinetic analysis of linezolid in patients with infectious disease: application to lower body weight and elderly patients

Authors: Abe S, Chiba K, Cirincione B, Grasela TH, Ito K, Suwa T
Publication: J Clin Pharmacol
Keywords: 80 and over, Acetamides, adolescent, adult, Age Factors, aged, analysis, anti-bacterial agents, Asian Continental Ancestry Group, body weight, clinical trials, Communicable Diseases, drug therapy, Phase II as Topic, Phase III as Topic
Division: Clinical Pharmacology and Pharmacometrics (CPP)

Linezolid (Zyvox), belonging to oxazolidinone antibiotics, is commonly used for the treatment of patients infected with methicillin-resistant Staphylococcus aureus and vancomycin-resistant enterococci.

Simulation of Food Effect on Cilostazol Exposure in Human

Simulation of Food Effect on Cilostazol Exposure in Human

Authors: Lukacova V, Crison JR, Bolger MB, Woltosz WS
Conference: CRS
Keywords: Cp-Time, dissolution, fed, food effect, PBPKPlus, solubility, tissue:plasma
Software: ADMET Predictor®, GastroPlus®
Division: PBPK

For certain drugs, the time of administration respective to meal times can have a significant impact on exposure. The effect of food is usually attributed to increased solubility/dissolution rate and/or…

Improving the Efficiency and Ensuring the Quality of Data Assembly for Pharmacometric Analysis

Improving the Efficiency and Ensuring the Quality of Data Assembly for Pharmacometric Analysis

Authors: Grasela TH, Fiedler-Kelly J, Hitchcock D
Conference: PAGE
Keywords: assembly, communications, creation, data, data assembly, dataassembly, dataset, dataset requirements, efficiency, forensic pharmacometrics, forms, informatics, PKPD methodology, process, programming, quality, specifications, team, wiki
Division: Clinical Pharmacology and Pharmacometrics (CPP)

Better tools and processes can improve the efficiency of data assembly and the quality of analysis-ready datasets for pharmacometric analyses.

Modeling and Simulation Approach to Pediatric Drug Development

Modeling and Simulation Approach to Pediatric Drug Development

Authors: Grasela TH, Passarell JA, Ludwig E, Fiedler-Kelly J
Conference: PAGE
Keywords: breakpoint model, children, clinical trial, dose, dosing regimens, exposure, PD, Pediatric, pediatrics, pharmacodynamic, pharmacokinetic, PK, PK/PD, PKPD methodology, simulation, strategy, study design
Division: Clinical Pharmacology and Pharmacometrics (CPP)

Describe a process for determining pediatric drug doses using pharmacokinetic/pharmacodynamic (PK/PD) modeling and simulation.

Celebrating Globalization

Celebrating Globalization

The word “globalization” can be interpreted many ways, both positive and negative. In these uncertain economic times, many people think globalization is equivalent to job loss and trade protectionism.

Prediction of Dose-Dependent Intestinal and Liver First Pass Extraction for CYP3A4 Substrates

Prediction of Dose-Dependent Intestinal and Liver First Pass Extraction for CYP3A4 Substrates

Authors: Lukacova V, Bolger MB, Woltosz WS
Conference: PharmSci Fair
Keywords: absorption, Cilostazol, gut, liver, midazolam, PBPK, PEAR, Population Estimates for Age-Related (PEAR™) Physiology™
Software: GastroPlus®
Division: PBPK

Cilostazol and midazolam absorption and pharmacokinetics were simulated using GastroPlus™. The program’s Advanced Compartmental and Transit model described the absorption and intestinal metabolism of both…

Role of physiological intestinal water in oral absorption

Role of physiological intestinal water in oral absorption

Authors: Sutton SC
Publication: AAPS J
Keywords: animals, biological models, biopharmaceutics, humans, intestinal absorption, metabolism, permeability, pharmaceutical preparations, pharmacokinetics, solubility
Software: GastroPlus®

Water volume has impact when the compound has low aqueous solubility. For example, the absorption of compounds with a Biopharmaceutics Classification System...