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Synthesis and pharmacodynamics of ibuprofen-1-acetoxyethyl ester
Ibuprofen(IBU) and its derivatives are widely used in treating many diseases, such as depression, glomerulonephritis, fever caused by common cold or influenza, and rheumatoid arthritis.
In vitro–in vivo and pharmacokinetic evaluation of solid lipid nanoparticles of furosemide using Gastroplus™
In this work, we conducted pharmacokinetic studies and established the in vitro and in vivo correlation (IVIVC) of furosemide (FRS) loaded solid lipid nanoparticles (FSLN).
Prediction of efficacy for conversion from adjunctive therapy to monotherapy with eslicarbazepine acetate 800 mg once daily for partial-onset epilepsy.
Eslicarbazepine acetate (ESL) is a once-daily (QD) oral antiepileptic drug (AED) indicated for partial-onset seizures (POS). Clinical studies of gradual conversion to ESL 1,200 and 1,600 mg QD...
Applications of Mechanistic Modeling and Simulations in Compound and Dosage Forms Selections
Physiologically based pharmacokinetic (PBPK) modeling and simulation techniques have been adopted in the pharmaceutical industry to aid in compound selection and dosage form development in recent years.
Population Pharmacokinetic Analysis of Compound A and Its Metabolite in Healthy Subjects and Patients with Diabetic Nephropathy
Compound A is a potent and highly selective non-steroidal mineralocorticoid receptor (MR) antagonist being developed for the treatment of diabetic nephropathy and other potential indications.
Exploring the Feasibility of Biowaiver Extension of BCS Class III Drugs with Site-Specific Absorption Using Gastrointestinal Simulation Technology
The US Food and Drug Administration, World Health Organization and European Medicines Agency have allowed biowaiver for some BCS class III drugs, but shortened the requisite dissolution time of BCS...
The impact of reduced gastric acid secretion on dissolution of salts of weak bases in the fasted upper gastrointestinal lumen: Data in biorelevant media and in human aspirates.
To propose media for simulating the intragastric environment under reduced gastric acid secretion in the fasted state at three levels of simulation of the gastric environment and evaluate their...
Substrate and method dependent inhibition of three ABC-transporters (MDR1, BCRP, and MRP2)
Drug transport and drug-drug interactions (DDI) with human ABC transporters are generally investigated in mammalian cell lines or inverted membrane vesicles from insect cells (Sf9) overexpressing the transporter of interest.
Mechanistic Modelling of Drug-Induced Liver Injury: Investigating the Role of Innate Immune Responses
Drug-induced liver injury (DILI) remains an adverse event of significant concern for drug development and marketed drugs, and the field would benefit from better tools to identify liver liabilities early in development and/or to mitigate potential DILI risk in otherwise promising drugs.
Identification of neuron selective androgen receptor inhibitors
Aim: To identify neuron-selective androgen receptor (AR) signaling inhibitors, which could be useful in the treatment of spinal and bulbar muscular atrophy (SBMA)...
Estimating Predictive Uncertainty for Artificial Neural Net Ensembles
The performance of QSAR models has traditionally been evaluated in terms of aggregate statistics – sensitivity, specificity, root mean square error (RMSE), R2, etc. – for some kind of test set.
Comparison of oral absorption properties among different bisphosphonates by using a newly developed physiologically based pharmacokinetic model.
Absorption of bisphosphonates（BPs）from the gastrointestinal tract is inhibited by forming a complex combined with multivalent cation in intake foods.
Applying Physiologically-Based Pharmacokinetic (PBPK) Modeling & Simulation to Assist with Pharmaceutical Research and Regulatory Submissions
Open communication between regulatory agencies, pharmaceutical companies, universities, and software providers will help identify new M&S applications.
Comparing Dog and Human Intestinal Fluids: Implications on Solubility and Biopharmaceutical Risk Assessment
Despite many documented differences in gut physiology compared to humans, the beagle dog has been successfully used as a preclinical model for assessing the relative bioavailability of dosage forms during formulation development.