Journal of Pharmaceutical Sciences
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Radar Chart Array Analysis to Visualize Effects of Formulation Variables on IgG1 Particle Formation as Measured by Multiple Analytical Techn...
We found that the environmental/mechanical stress condition (e.g., heat vs. agitation) was the most important factor in influencing the particle size and morphology distribution with this IgG1 mAb. Additionally, the presence of NaCl exhibited a pH and stress-dependent behavior resulting in promotion...
Aminoalkylmethacrylate copolymer E improves oral bioavailability of YM466 by suppressing drug-bile interaction.
The aim of this study was to find out polymeric compounds that can inhibit the interaction between YM466, a novel anticoagulant, and bile to improve its oral bioavailability. In vitro ultrafiltration method using extract gall powder was useful to detect the formation of insoluble complex of YM466 wi...
Precise comparison of protein localization among OCT, OAT, and MATE in human kidney.
Organic anion transporters (OATs) and organic cation transporters (OCT) play pivotal roles in the uptake of drugs into epithelial cells at the basolateral membranes, and multidrug and toxin extrusion (MATE) mediates drug secretion into urine at the brush-border membranes. In this study, the expressi...
When is protein binding important?
The present paper is an ode to a classic citation by Benet and Hoener (2002. Clin Pharm Ther 71(3):115-121). The now classic paper had a huge impact on drug development and the way the issue of protein binding is perceived and interpreted. Although the authors very clearly pointed out the limitation...
Quantitative atlas of blood-brain barrier transporters, receptors, and tight junction proteins in rats and common marmoset.
The purpose of this study was to determine the protein amounts of blood-brain barrier (BBB) permeability-related transporters, receptors, and tight junction proteins in Sprague Dawley and Wistar rats and common marmoset, and also to investigate inter-species and inter-strain differences across roden...
Establishment of novel prediction system of intestinal absorption in humans using human intestinal tissues.
The objective of this study was to establish a novel prediction system of drug absorption in humans by utilizing human intestinal tissues. Based on the transport index (TI), a newly defined parameter, calculated by taking account of the change in drug concentrations because of precipitation on the a...
Adapalene microemulsion for transfollicular drug delivery.
The aim of this study was to develop a microemulsion formulation of adapalene for transfollicular delivery. A pseudoternary phase diagram was developed for microemulsion consisting of oleic acid as oil phase, tween 20 as surfactant, Transcutol® as cosurfactant, and deionized water. Differential tape...
A prediction model for monitoring ribbed roller compacted ribbons.
The application of near infrared (NIR) spectroscopy for real-time monitoring of the critical quality attributes of ribbed roller compacted ribbons was studied. Three NIR probes (QR 200, QR 400, and QR 600) of lens diameters, 200, 400, and 600 μm, respectively were used at various fixed distances fro...
Conjugation to polymeric chains of influenza drugs targeting M2 ion channels partially restores inhibition of drug-resistant mutants.
We endeavored to recover their potency in inhibiting drug-resistant influenza viruses. Depending on loading densities, as well as the nature of the drug, the polymer, and the spacer arm, polymer-conjugated drugs were up to 30-fold more potent inhibitors of drug-resistant strains than their monomeric...
Asparagine deamidation dependence on buffer type, pH, and temperature.
The deamidation of asparagine into aspartate and isoaspartate moieties is a major pathway for the chemical degradation of monoclonal antibodies (mAbs). It can affect the shelf life of a therapeutic antibody that is not formulated or stored appropriately. A new approach to detect deamidation using io...