Study methodologies of supersaturated state are fast developing as pharmaceutical industry is adopting supersaturating drug delivery systems (SDDS) to overcome the solubility issue of drugs.
Automated techniques in pKa determination: Low, medium and high-throughput screening methods
Drug discovery programs that generate hundreds of new molecular entities need efficient methodologies for physicochemical profiling.
The OECD Principles for (Q)SAR Models in the Context of Knowledge Discovery in Databases (KDD)
The steps followed in the knowledge discovery in databases (KDD) process are well documented and are widely used in different areas where exploration of data is used for decision making. In turn, while…
In vitro/in silico approach in the development of simvastatin-loaded self-microemulsifying drug delivery systems.
The aims of this study were to formulate simvastatin (SV)-loaded self-microemulsifying drug delivery systems (SMEDDS), and explore the potential of these drug delivery systems to improve...
Exposure-safety and efficacy response relationships and population pharmacokinetics of eslicarbazepine acetate
Eslicarbazepine acetate (ESL) is a once-daily (QD) oral antiepileptic drug (AED) for focal-onset seizures (FOS).
Pharmacokinetics and interspecies scaling of a novel, orally-bioavailable anti-cancer drug, SHetA2
SHetA2 is a small molecule drug with promising cancer prevention and therapeutic activity and a high preclinical safety profile. The study objectives were to perform interspecies scaling and...
Dissolution and Translational Modeling Strategies Enabling Patient-Centric Drug Product Development: the M-CERSI Workshop Summary Report
On May 15th–17th, 2017, the US FDA and the International Consortium for Innovation and Quality in Pharmaceutical Development (IQ) held a workshop at the University of Maryland’s Center of Excellence...
A strategy for early risk predictions of clinical drug-drug interactions involving the GastroPlusTM DDI module for time-dependent CYP inhibitors
A set of reference compounds for time-dependent inhibition (TDI) of cytochrome P450 with available literature data for kinact and KI was used to predict clinical implications using the GastroPlusTM software.
A Survey of the Regulatory Requirements for BCS-Based Biowaivers for Solid Oral Dosage Forms by Participating Regulators and Organisations of the International Generic Drug Regulators Programme
The Biopharmaceutics Classification System (BCS) based biowaiver is a scientific model which enables the substitution of in vivo bioequivalence studies with in vitro data as evidence of therapeutic equivalence subject to certain conditions.
Experimental versus theoretical log D7.4, pKa and plasma protein binding values for benzodiazepines appearing as new psychoactive substances
The misuse of benzodiazepines as new psychoactive substances is an increasing problem around the world. Basic physicochemical and pharmacokinetic data is required on these substances to interpret and predict their effects upon humans.
In silico prediction coupled with in vitro experiments and absorption modeling to study the inclusion complex of telmisartan with modified beta-cyclodextrin
Telmisartan (TEL) is a poorly bioavailable antihypertensive drug candidate owing to its low solubility in all the biofluids.
An Introduction to DILIsym® Software, a Mechanistic Mathematical Representation of Drug-Induced Liver Injury
Drug-induced liver injury (DILI) is one of the primary reasons why a new drug candidate may fail during development.
In Vitro, in Silico, and in Vivo Assessments of Intestinal Precipitation and Its Impact on Bioavailability of a BCS Class 2 Basic Compound
In this study, a multipronged approach of in vitro experiments, in silico simulations, and in vivostudies was developed to evaluate the dissolution, supersaturation, precipitation, and...
Absolute Oral Bioavailability of Creatine Monohydrate in Rats: Debunking a Myth
Creatine is an ergogenic compound used by athletes to enhance performance. Supplementation with creatine monohydrate (CM) has been suggested for musculoskeletal and neurological disorders.
Process optimization and in vivo performance of docetaxel loaded PHBV-TPGS therapeutic vesicles: A synergistic approach.
This research was motivated due to substantial requirement of improved treatment for breast cancer which accounts for over 0.52 million deaths annually worldwide.
Clinical Bioavailability of the Novel BACE1 Inhibitor Lanabecestat (AZD3293): Assessment of Tablet Formulations Versus an Oral Solution and the Impact of Gastric pH on Pharmacokinetics.
The relative bioavailability of lanabecestat administered as 2 tablet formulations versus an oral solution was investigated.
In vitro to in vivo extrapolation for high throughput prioritization and decision making
In vitro chemical safety testing methods offer the potential for efficient and economical tools to provide relevant assessments of human health risk.
Combining an In Vitro Kinetic Model with a Physiologically-Based Pharmacokinetic Model to Assess the Potential In Vivo Fate of Polyvinyl Pyrrolidone-Vinyl Acetate Copolymers
To understand hydrolysis and alcoholysis of polyvinylpyrrolidone-co-vinylacetate (PVPVA) during formulation and storage, elucidate the reaction mechanism, establish an intrinsic kinetic model, and apply...
The Role of Circulating Tumor DNA in Renal Cell Carcinoma
Next-generation sequencing (NGS) of circulating tumor DNA (ctDNA) is a novel technology that can complement tumor tissue NGS and has the potential to influence...
Monitoring of erlotinib in pancreatic cancer patients during long-time administration and comparison to a physiologically based pharmacokinetic model
In this study, a therapeutic drug monitoring (TDM) of erlotinib in pancreatic cancer patients was performed over 50 weeks to reveal possible alterations in erlotinib plasma concentrations.