Development of a stick-type transdermal eyelid delivery system of ketotifen fumarate for ophthalmic diseases

A transdermal eyelid delivery system for treating ocular diseases (eye-stick) has been developed. Ketotifen fumarate (KT) was used as a model drug. An in vivo study using rabbits showed that the eye-stick device maintained a constant conjunctival concentration of the drug for an extended period of time, which was equivalent or higher than the therapeutic level following eye drop administration. Moreover, the conjunctival concentration after eye-stick application was well predicted using the physicochemical parameters, diffusion coefficient and partition coefficient, obtained from in vitro hairless mouse skin permeation experiments.     

Effects of T-tubules on dielectric spectra of skeletal muscle simulated by boundary element method with two-dimensional models

In order to investigate the origin of large intensity the alpha-relaxation in skeletal muscles observed in dielectric measurements with extracellular electrode methods, effects of the interfacial polarization in the T-tubules on dielectric spectra were evaluated with the boundary-element method using two-dimensional models in which the structure of the T-tubules were represented explicitly. Each model consisted of a circular inclusion surrounded by a thin shell corresponding to the sarcolemma. The T-tubules were represented by simplified two types of invagination of the shell: straight invagination along the radial directions, and branched one. Each of the models was subjected to two kinds of calculations relevant to experiments with the extracellular and the intracellular electrode methods. Electrical interactions between the cells were omitted in the calculations. Both calculations showed that the dielectric spectra of the models contained two relaxation terms. The low-frequency relaxation term assigned to the alpha-relaxation depended on the structure of the T-tubules. Values of the relaxation frequency of the alpha-relaxation obtained from the two types of calculations agreed with each other. At the low-frequency limit, the permittivity obtained from the extracellular-electrode-type calculations varied in proportion to the capacitance obtained from the intracellular-electrode-type ones. These results were consistent with conventional lumped and distributed circuit models for the T-tubules. This confirms that the interfacial polarization in the T-tubules in a single muscle cell is not sufficient to explain the experimental results in which the intensity of the alpha-relaxation in the extracellular-electrode-type experiments exceeded the intensity expected from the results of the intracellular-electrode-type experiments. The high-frequency relaxation term that was assigned to the beta-relaxation was also affected by the T-tubule structure in the calculations relevant to the extracellular-electrode-type experiments.     

Dodecyl thioglycopyranoside sulfates: novel sugar-based surfactants for enantiomeric separations by micellar electrokinetic capillary chromatography

Four novel chiral anionic surfactants having carbohydrate hydrophilic heads, sodium n-dodecyl 1-thio-beta-D-glucopyranoside 6-hydrogen sulfate (6-betaGlcD), sodium n-dodecyl 1-thio-beta-L-glucopyranoside 6-hydrogen sulfate (6-betaGlcL), sodium n-dodecyl 1-thio-beta-L-fucopyranoside 3-hydrogen sulfate (3-betaFucL), and sodium n-dodecyl 1-thio-alpha-L-rhamnopyranoside 3-hydrogen sulfate (3-alphaRhaL), were synthesized by selective sulfation of the corresponding thioglycosides. Their CMC determined by fluorescence using pyrene as a probe in water was 1.3-2.7 mM. These surfactants found to be useful as chiral selectors for enantiomeric separation by MEKC. The enantiomeric separation was optimized with respect to pH, buffer concentration, and surfactant concentration. Under the optimized conditions (50 mM phosphate buffer at pH 6.5, 30 mM surfactant, 20 kV), the enantiomeric separations of five dansylated amino acids (Dns-AAs) were achieved within approximately 20 min with the migration order of Val相似文献   

Enantiomeric separation by MEKC using dodecyl thioglycoside surfactants: Importance of an equatorially oriented hydroxy group at C‐2 position in separation of dansylated amino acids

To investigate the influence of stereogenic centers of sugar‐based surfactants for enantiomeric separation, four n‐dodecyl thioglycoside sulfates (CMC 1.5–3.6 mM) were chosen as micelle‐forming surfactants and five dansylated hydrophobic amino acids were used as test analytes. The analytes were mutually separated by these micelles exhibiting almost similar migration times independent of the used surfactant. Baseline separations of all enantiomers were achieved using both β‐D ‐glucose and β‐D ‐galactose derivates that have an equatorially oriented hydroxy group at C‐2 position. In contrast, the ability of enantioseparation was markedly decreased in the case of β‐D ‐mannose and 2‐deoxy‐β‐D ‐glucose derivatives. These results suggested that the structure of C‐2 position of the sugar unit, namely presence of an equatorially oriented hydroxy group, is highly important for the enantiomeric separation of the chosen hydrophobic dansylated amino acids.     

Spin‐Torque Manipulation for Hydrogen Sensing

External manipulation of spin‐orbit torques (SOTs) promises not only energy‐efficient spin‐orbitronic devices but also versatile applications of spin‐based technologies in diverse fields. However, the external electric‐field control, widely used in semiconductor spintronics, is known to be ineffective in conventional metallic spin‐orbitronic devices due to the very short screening length. Here, an alternative approach to control the SOTs by using gases is shown. It is demonstrated that the spin‐torque generation efficiency of a Pd/Ni₈₁Fe₁₉ bilayer can be reversibly manipulated by the absorption and desorption of H₂ gas, which appears concomitantly with the change of the electrical resistance. It is found that compared with the change of the Pd resistance induced by the H₂ absorption, the change of the spin‐torque generation efficiency is almost an order of magnitude larger. This result provides a new method to externally manipulate the SOTs and paves a way for developing more sensitive hydrogen sensors based on the spin‐orbitronic technology.     

Terahertz Oscillating Devices Based Upon the Intrinsic Josephson Junctions in a High Temperature Superconductor

Recent developments of coherent terahertz (THz) oscillators based on the intrinsic Josephson junctions (IJJs) in mesas of the high temperature superconductor Bi₂Sr₂CaCu₂O_8+δ are reviewed. Experimental and theoretical studies of the emission from equilateral, right-angled isosceles, and acute isosceles triangular mesas are compared with those obtained from rectangular, square, and disk mesas, in order to determine the role of the mesa geometry. The superconducting properties and emission frequency f spectra are presented for a variety of triangular mesa geometries. Analytic and finite difference time domain numerical calculations of the emissions from the internal electromagnetic (EM) cavity modes of triangular mesas are compared with experiment. The experimental f always satisfies the ac Josephson relation, and its narrow linewidth arises from the synchronized emissions from many IJJs. For some mesa geometries, f also strongly locks onto an EM cavity mode frequency, enhancing the emission’s stability and output power. For other geometries, such cavity mode locking is weak, and f is highly tunable.     

Elastic properties of filled-Skutterudite compounds probed by Mössbauer nuclei

We have carried out Mössbauer spectroscopy and nuclear resonant inelastic scattering to elucidate the lattice dynamics in filled-Skutterudite compounds, especially phosphides. The second-order Doppler shift obeys the Debye model in RFe₄P₁₂. Nuclear quadrupole interaction reveals an unusual temperature dependence in these compounds. An anomaly is observed in ⁵⁷Fe nuclear resonant inelastic scattering of these compounds. The energy where the anomaly observed in SmFe₄P₁₂ agrees with the phonon excitation energy observed by ¹⁴⁹Sm nuclear resonant inelastic scattering. We have also performed the ⁹⁹Ru Mössbauer measurements of SmRu₄P₁₂.     

Synthesis of polyethylene and polypropylene containing fluorene units in the side chain

Copolymerizations of ethylene or propylene and allyl monomers containing 9‐fluorenyl group, diallyl‐di‐9‐fluorenylsilane (DAFS), 9,9‐diallylfluorene (DAF), and 9‐allylfluorene (AF), were investigated with various zirconocene catalysts using methylaluminoxane as a cocatalyst. The bridged zirconocene catalysts, especially a syndioselective catalyst, showed a higher reactivity for all the comonomers than the nonbridged catalysts. DAFS was mainly incorporated into the polymer chain via cyclization insertion, whereas DAF was copolymerized via both 1,2‐ and cyclization insertions. Cyclization selectivity, ratio of cyclized insertion unit, of DAF in the copolymerization with propylene was higher than that in the copolymerization with ethylene. Copolymerization with AF yielded low‐molecular weight copolymer because of frequent chain transfer reaction. Optical properties of the propylene based‐copolymers were investigated by UV‐vis and photoluminescence spectroscopy, and absorption‐ and emission‐derived from fluorenyl groups were detected in the copolymers. © 2010 Wiley Periodicals, Inc. J Polym Sci Part A: Polym Chem 48: 3542–3552, 2010     

Measurement of reduction in SHG coefficient of LiNbO/sub 3/ by proton exchanging

The SHG coefficient of a proton-exchanged layer of LiNbO/sub 3/, relative to the bulk value, has been measured for the first time by non-phase-matched SHG using a grating sample. It was found that the d/sub 33/ coefficient is reduced to approximately 0.5 of the bulk value by proton exchanging in pure benzoic acid.<>