Extension of the dissolution-precipitation model for kinetic elucidation of solvent-mediated polymorphic transformations

Extension of the dissolution-precipitation model for kinetic elucidation of solvent-mediated polymorphic transformations

Publication: Eur J Pharm Biopharm
Software: GastroPlus®

Thorough understanding and control of the different crystal forms of a drug product is key for fine chemistry and materials science; it ultimately determines the product's physicochemical properties and performance.

Structural and conformational determinants of macrocycle cell permeability

Structural and conformational determinants of macrocycle cell permeability

Publication: Nat Chem Biol

Macrocycles are of increasing interest as chemical probes and drugs for intractable targets like protein-protein interactions, but the determinants of their cell permeability and oral absorption are poorly understood.

Forecasting oral absorption across biopharmaceutics classification system classes with physiologically based pharmacokinetic models

Forecasting oral absorption across biopharmaceutics classification system classes with physiologically based pharmacokinetic models

Publication: J Pharm Pharmacol
Software: GastroPlus®

The aim of this study was (1) to determine how closely physiologically based pharmacokinetic (PBPK) models can predict oral bioavailability using a priori knowledge of drug-specific properties and (2) to...

In vitro and in silico investigation of electrospun terbinafine hydrochloride-loaded buccal nanofibrous sheets

In vitro and in silico investigation of electrospun terbinafine hydrochloride-loaded buccal nanofibrous sheets

Publication: J Pharm Biomed Anal

Terbinafine hydrochloride-loaded nanofibrous buccal films were formulated with the aim to improve the solubility and dissolution behavior; thus, the local effectiveness of the antifungal agent.

An in vitro and in silico study of the impact of engineered surface modifications on drug detachment from model carriers

An in vitro and in silico study of the impact of engineered surface modifications on drug detachment from model carriers

Publication: Int J Pharm

In silico modeling was used to predict the impact of carrier surface modifications on the in vivo plasma concentration of an active pharmaceutical ingredient (API) and as a tool to support formulation development.

Synthesis and structure-activity relationship study of tacrine-based pyrano[2,3-c]pyrazoles targeting AChE/BuChE and 15-LOX

Synthesis and structure-activity relationship study of tacrine-based pyrano[2,3-c]pyrazoles targeting AChE/BuChE and 15-LOX

Publication: Eur J Med Chem

A series of tacrine-based pyrazolo[4′,3′:5,6]pyrano[2,3-b]quinolines and related compounds were designed and synthesized for targeting AChE, BuChE and 15-LOX enzymes in the field of Alzheimer's disease therapy.

Physiologically Based Pharmacokinetic (PBPK) Modeling of Pharmaceutical Nanoparticles

Physiologically Based Pharmacokinetic (PBPK) Modeling of Pharmaceutical Nanoparticles

Authors: Li M, Zou P, Tyner K, Lee SL
Publication: AAPS J
Software: GastroPlus®

With the great interests in the discovery and development of drug products containing nanoparticles, there is a great demand of quantitative tools for assessing quality, safety, and efficacy of these products.

The Prediction of the Relative Importance of CYP3A/P-gp to the Non-linear Intestinal Absorption of Drugs by Advanced Compartmental Absorption and Transit (ACAT) Model

The Prediction of the Relative Importance of CYP3A/P-gp to the Non-linear Intestinal Absorption of Drugs by Advanced Compartmental Absorption and Transit (ACAT) Model

Publication: Drug Metab Dispos

Intestinal CYP3A and P-glycoprotein (P-gp) decrease the intestinal absorption of substrate drugs. Since substrate specificity of CYP3A often overlaps that of P-gp, and estimation of their saturability in the...

Using Physiologically Based Pharmacokinetic (PBPK) Modeling to Evaluate the Impact of Pharmaceutical Excipients on Oral Drug Absorption: Sensitivity Analyses

Using Physiologically Based Pharmacokinetic (PBPK) Modeling to Evaluate the Impact of Pharmaceutical Excipients on Oral Drug Absorption: Sensitivity Analyses

Publication: AAPS J

Drug solubility, effective permeability, and intestinal metabolism and transport are parameters that govern intestinal bioavailability and oral absorption.

Utilizing In Vitro Dissolution-Permeation Chamber for the Quantitative Prediction of pH-Dependent Drug-Drug Interactions with Acid-Reducing Agents: a Comparison with Physiologically Based Pharmacokinetic Modeling

Utilizing In Vitro Dissolution-Permeation Chamber for the Quantitative Prediction of pH-Dependent Drug-Drug Interactions with Acid-Reducing Agents: a Comparison with Physiologically Based Pharmacokinetic Modeling

Publication: AAPS J

For many orally administered basic drugs with pH-dependent solubility, concurrent administration with acid-reducing agents (ARAs) can significantly impair their absorption and exposure.

Folate-targeted amphiphilic cyclodextrin.siRNA nanoparticles for prostate cancer therapy exhibit PSMA mediated uptake, therapeutic gene silencing in vitro and prolonged circulation in vivo

Folate-targeted amphiphilic cyclodextrin.siRNA nanoparticles for prostate cancer therapy exhibit PSMA mediated uptake, therapeutic gene silencing in vitro and prolonged circulation in vivo

Publication: Nanomedicine

In this study, a folate targeted cyclodextrin (CD) nanoparticle was prepared by co-formulating CD.siRNA complexes with DSPE-PEG5000-folate to target the prostate specific membrane antigen (PSMA).

Predicting Exposure After Oral Inhalation of the Selective Glucocorticoid Receptor Modulator, AZD5423, Based on Dose, Deposition Pattern, and Mechanistic Modeling of Pulmonary Disposition

Predicting Exposure After Oral Inhalation of the Selective Glucocorticoid Receptor Modulator, AZD5423, Based on Dose, Deposition Pattern, and Mechanistic Modeling of Pulmonary Disposition

Publication: J Aerosol Med Pulm Drug Deliv

Exposure following oral inhalation depends on the deposition pattern of the inhaled aerosol, the extent and rate of oral and pulmonary absorption, as well as systemic distribution and clearance.

Application of Physiologically Based Absorption Modeling to Characterize the Pharmacokinetic Profiles of Oral Extended Release Methylphenidate Products in Adults

Application of Physiologically Based Absorption Modeling to Characterize the Pharmacokinetic Profiles of Oral Extended Release Methylphenidate Products in Adults

Authors: Yang X, Duan J, Fisher J
Publication: PLoS One

A previously presented physiologically-based pharmacokinetic model for immediate release (IR) methylphenidate (MPH) was extended to characterize the pharmacokinetic behaviors of oral extended release (ER) MPH formulations in adults for the first time.