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Kenji Sugibayashi: Influence Statistics

Purpose. Simultaneous skin transport and metabolism of ethyl nicotinate (EN), a model drug, were measured and theoretically analyzed.Methods. Several permeation studies of EN or its metabolite nicotinic acid (NA) were done on full-thickness skin or stripped skin with and without an esterase inhibitor. Permeation parameters such as partition coefficient of EN from the donor solution to the stratum corneum and diffusion coefficients of EN and NA in the stratum corneum and the viable ...

The effects of the concentration and molecular weight of poly-L-arginine (poly-L-Arg) on the in vivo nasal absorption of fluorescein isothiocyanate-labeled dextran (MW, 4 kDa, FD-4) in rats were studied. When poly-L-Arg with a range of different molecular weights (MW, 8.9, 45.5 and 92.0 kDa) was applied intranasally at various concentrations, the bioavailability (F(0-9 h)) of FD-4 increased with the increasing concentration of poly-L-Arg. The enhanced absorption was also dependent on the ...

Bucolome, a nonsteroidal anti-inflammatory drug, has often been coadministered to patients who take warfarin as an anticoagulant. This combination increases the anticoagulant effect, which is most likely due to the interaction of bucolome with the pharmacokinetics (PK) or pharmacodynamics (PD) of warfarin. More than 30 years ago the mechanism of this interaction was reported to be inhibition of warfarin protein binding by bucolome, and the inhibition of warfarin metabolism by bucolome ...

PurposeTo calculate the skin concentration of active ingredients in cosmetics and topical pharmaceuticals using silicone membrane permeation.MethodsA series of parabens were used as model ingredients. Skin concentration of parabens was calculated using silicone membrane permeability. Their partition coefficient from formulations to the silicone membrane was determined by the membrane permeation profiles, and used to calculate their silicone membrane concentration, under an assumption ...

Several cationic compounds were screened as potential nasal absorption enhancers to increase intranasal absorption of a model drug, fluorescein isothiocyanate labeled dextran (MW 4.4 kDa, FD-4), without nasal membrane damage in rats. Their effects were compared with those of classical enhancers. Various cationic compounds (poly-L-arginines with different molecular weights (MW 8.9, 45.5 and 92.0 kDa, poly-L-Arg (10), (50) and (100), respectively), L-arginine (L-Arg), L-lysine (L-Lys), and ...

A combination of microneedle pretreatment and iontophoresis was evaluated for the potential to increase skin permeation of drugs. Two model compounds with low and high molecular D(2)O and fluorescein isothiocyanate (FITC)-dextrans (FD-4, FD-10, FD-40, FD-70 and FD-2000; average molecular weight of 3.8, 10.1, 39.0, 71.2 and 200.0 kDa), respectively, were used and the effect of microneedle pretreatment and iontophoresis on their in vitro permeability was evaluated using excised hairless ...

An in vitro permeation study of ethyl nicotinate (EN) was carried out using excised hairless rat skin, and simultaneous skin transport and metabolism of the drug were kinetically followed. Fairly good steady-state fluxes of EN and its metabolite nicotinic acid (NA) through the skin were obtained after a short lag time for all the concentrations of EN applied. These steady-state fluxes were not proportional to the initial donor concentration of EN: EN and NA curves were concave and ...

The objectives of the present study are to clarify the relationship between the physicochemical properties and the nail permeability of drugs through human nail plates. Homologous p-hydroxybenzoic acid esters were used to investigate the relationship between the octanol/water partition coefficient and the permeability coefficient of several drugs. The nail permeability was found to be independent of the lipophilicity of a penetrating drug. However, the nail permeability of several model ...

The stability of flavin adenin dinucleotide (FAD) in plasma was studied under a low-intensity light and FAD was found to be converted to flavin mononucleotide (FMN) and riboflavin (RF) in both human and rat plasma. The hydrolysis rates of FAD in plasma at 4 degrees C were lower than those at 37 degrees C. In addition, the hydrolysis rates were markedly inhibited when EDTA, known as an anticoagulant, was added to plasma. These results indicated that plasma samples in pharmacokinetic ...

A predictive method for skin permeability of drugs from polyethylene glycol 400 (PEG)-water and ethanol (EtOH)-water binary solvents is proposed. The method is based on a permeation model, in which the stratum corneum is assumed to be a membrane having two parallel permeation pathways: lipid and pore pathways. Skin permeability of several drugs with a variety of physicochemical properties from various PEG-water and EtOH-water solvents was tested. In PEG-water solvents, almost the same ...

The species difference in skin permeability, Kp, of nicorandil was determined by using excised skin samples from hairless mouse, hairless rat, guinea-pig, dog, pig, and human. The Kp value of nicorandil in hairless mice was the greatest among the six species, and those in pigs and humans were in good agreement. To clarify the reasons for the species difference, various skin characteristics in each species were measured. It was suggested that the difference of skin surface lipids in each ...

The cytochrome P450 (CYP) isoforms that catalyze the oxidation metabolism of 6-methoxy-2-napthylacetic acid (6-MNA), an active metabolite of nabumetone, were studied in rats and humans. Using an extractive reversed-phase HPLC assay with fluorescence detection, monophasic Michaelis-Menten kinetics was obtained for the formation of 6-hydroxy-2-naphthylacetic acid (6-HNA) in liver microsomes of rats and humans, and kinetic analysis showed that the K(m) and V(max) values for the formation of ...

Pressure sensitive adhesive (PSA) matrices containing amorphous ketotifen were prepared and evaluated for enhanced skin permeability of the drug. A solvent casting method using silicone-typed PSA was employed, and n-hexane, an original solvent for the PSA and one more solvent, dichloromethane, tetrahydrofuran, acetone, ethyl acetate or toluene, were used for complete dissolution of ketotifen and high dispersion in an amorphous state of the drug. Presence of the amorphous form was judged ...