Design of a rate- and time-programming drug release device using a hydrogel: pulsatile drug release from κ-carrageenan hydrogel device by surface erosion of the hydrogel

We have found that a repetitive pulsatile drug release with a certain time interval is observed from a monolithic hydrogel device by surface erosion of the hydrogel. As a model system of pulsatile drug release, dibucaine hydrochloride and κ-carrageenan hydrogel were chosen as a drug and a device, respectively. Electrostatic interactions between dibucaine hydrochloride and κ-carrageenan polymer segments are strong, since dibucaine hydrochloride is positively charged and each disaccharide repeating unit of κ-carrageenan chains has one sulfate group. Dibucaine hydrochloride was loaded into the hydrogel by immersing dry κ-carrageenan hydrogel disks in a dibucaine hydrochloride solution for 24 h. The pulsed release of dibucaine hydrochloride from the device was observed every 50 min between 30 and 250 min after the release starts. The weight of κ-carrageenan hydrogel decreases in an oscillatory manner with time in distilled water. The oscillatory changes observed in the hydrogel weight in distilled water are considered to be caused by influx and efflux of water molecules into and from the surface and core of the hydrogel and by polymer liberation from the hydrogel. This phenomenon was well explained by our kinetic model [Colloids and Surfaces B 8 (1996) 93–100]. The time interval between pulses observed in drug release coincides with that observed in the oscillatory weight change of the hydrogel. From these, it was concluded that the pulsatile release of dibucaine hydrochloride from the device was caused by the pulsatile liberation of swollen κ-carrageenan hydrogel from the surface of the device.     

Deformation of a singularity of type E8 and Mordell‐Weil lattices in characteristic 2

In this paper, we study the Mordell‐Weil lattices of the family of elliptic surfaces which is arising from the E₈⁴ singularity, one of the ADE singularities in characteristic 2. And we construct a subfamily of the universal family of supersingular K 3 surfaces in characteristic 2 as an application (© 2010 WILEY‐VCH Verlag GmbH & Co. KGaA, Weinheim)     

Degradation of triphenyltin compounds in sea water by pyoverdins from Pseudomonas chlororaphis

The yellow compound species pyoverdin was isolated from Pseudomonas chlororaphis. Degradation of triphenyltin (TPT) by pyoverdin (20 mg) was carried in distilled water (30 ml) containing a 6 µg l^?1 concentration of TPT at 20 °C for 96 h in aerobic conditions. The organotins in water and sea water were analyzed by gas chromatograph–mass spectrometry in selected ion mode. TPT and diphenyltin (DPT) in sea water were degraded to monophenyltin (MPT) with pyoverdins isolated from P. ­chlororaphis. Degradation of TPT in sea water increased with increasing temperature between 4 and 37 °C. Optimum degradation of TPT in sea water was at pH 7–8.5. Degradation of TPT and DPT in distilled water can be faster than in sea water. Also, degradation of TPT in both water and sea water was faster than that of DPT. Tributyltin, dibutyltin, monobutyltin and MPT in water and sea water were not degraded by pyoverdins isolated from P. chlororaphis. Copyright © 2001 John Wiley & Sons, Ltd.     

Synthesis and recognition of amino acids by binaphthyl-crown receptors

Two binaphthyl crown receptors containing phenylboric acid 2 and 2,4-dinitrophenylurea 3 as lariat parts were prepared from the optically active binaphthyl crown alcohol 1 in two and four steps, respectively. Host 2 showed a 30% extraction efficiency for GABA by a solid-liquid extraction method in DMSO. Chromogenic Host 3 discriminated the guest linear amino acid by molecular length and the information was revealed through color changes.     

Revised structure of tetrapetalone A and its absolute stereochemistry

The chemical structure of tetrapetalone A (1), a novel lipoxygenase inhibitor from Streptomyces sp., was revised by using the ¹H-¹⁵N HMBC technique. Furthermore, the absolute stereochemistry of all the asymmetric carbons in 1 was determined based on the detailed NOE data of 1 and its derivative.     

Doubly N-confused hexaphyrin: a novel aromatic expanded porphyrin that complexes bis-metals in the core

Meso-hexakis(pentafluorophenyl)-substituted doubly N-confused hexaphyrins and their metal complexes were synthesized for the first time, and the structures were elucidated by X-ray single-crystal analyses. The free base form of oxidized hexaphyrin (5) had two preorganized N3O pockets in the macrocyclic core, where a hydrogen-bonding network was formed to keep the molecule planar (the mean plane deviation is 0.054 A). The formation of a planar bis-Cu(II) complex was confirmed by UV/vis, magnetic susceptibility measurements, and X-ray crystallography. The bis-Ni(II) complex (7), on the other hand, was distored from planarity, but it changed to the planar structure upon solvent (acetonitrile) coordination as judged by the observation of a sharp Soret-like band in absorption spectra and the X-ray structures of the complexes.