Synthesis and In Vitro Properties of Dexamethasone 21-Sulfate Sodium as a Colon-Specific Prodrug of Dexamethasone

ABSTRACT

We synthesized dexamethasone 21-sulfate sodium (DS) as a colon-specific prodrug of dexamethasone and investigated its properties. Introduction of a sulfate group to dexamethasone lowered the apparent partition coefficient from 52.5 to 0.27 in 1-octanol/pH 6.8 phosphate buffer at 37°C. DS was stable on incubation with buffer solutions of varied pH or with the upper intestinal contents of rats at 37°C for 24 h. On incubation with the cecal contents, DS was hydrolyzed by producing dexamethasone over 80% of the dose at 10 h. When DS was incubated with the cecal contents collected from trinitrobenzenesulfonic acid (TNBS)-induced colitic rats, the degree of prodrug hydrolysis and production of dexamethasone amounted to 70% of healthy rats. In comparison with prednisolone, hydrocortisone, and cortisone, dexamethasone was stable against bioinactivation by the cecal contents, a desirable property for the development of a colon-specific prodrug. These results demonstrated that DS might be delivered specifically to the colon as an intact form to produce dexamethasone in high yield, suggesting DS as a potential colon-specific prodrug of dexamethasone.     

Neural network-based prediction of the long-term time-dependent mechanical behavior of laminated composite plates with arbitrary hygrothermal effects

Journal of Mechanical Science and Technology - Recurrent neural network (RNN)-based accelerated prediction was achieved for the long-term time-dependent behavior of viscoelastic composite laminated...     

Determination of atomistic deformation of tricalcium silicate paste with high-volume fly ash

We examined the effect of incorporating high-volume fly ash on the atomic arrangement and interatomic deformation behavior of calcium silicate hydrates in tricalcium silicate paste upon exposure to external forces. The interatomic structural changes and strains under compressive load were assessed using synchrotron in situ high-energy X-ray scattering-based atomic pair distribution function analysis. Three different types of strains, which were (a) macroscopic strains from gauges on the surfaces of specimen, (b) strains in a reciprocal space (Bragg peak shift), and (c) strains in real space (PDF peak shift), were compared to each other. All monitored and calculated strains for tricalcium silicate-fly ash (50 wt% fly ash) paste were compared with the counterparts of the pure tricalcium silicate paste. Pair distribution function analysis in the range of r < 10 Å indicated that the atomic arrangement of tricalcium silicate-fly ash was similar to that of synthetic calcium silicate hydrates followed by that of pure tricalcium silicate paste. Moreover, the pair distribution function refinement results revealed that the calcium silicate hydrate structure in tricalcium silicate-fly ash paste was similar to tobermorite 11 Å, unlike that in pure tricalcium silicate paste. The interatomic strain of tricalcium silicate-fly ash in the real space (r < 20 Å) was smaller than that of tricalcium silicate under compression, which suggested that the incompressibility of calcium silicate hydrates at atomistic scale was enhanced by the incorporation of fly ash into it. This was likely to be caused by the increased silicate polymerization of calcium silicate hydrates, which was attributed to the increase in the amount of silicate in their structure via the addition of fly ash.     

System analysis study for Korean fusion DEMO reactor

A conceptual design study for a steady-state Korean fusion DEMO reactor (K-DEMO) has been initiated. Two peculiar features need to be noted. First, the major radius is designed to be just below 6.5 m, considering practical engineering feasibilities. But still, high magnetic field at the plasma center around 8 T is expected to be achieved by using current state-of-the-art high performance Nb₃Sn strand technology. Second, a two-stage development plan is being considered. In the first stage, K-DEMO will demonstrate a net electricity generation but will also act as a component test facility. Then, after a major upgrade, K-DEMO is expected to show a net electric generation on the order of 300 MWe and the competitiveness in cost of electricity (COE). Feasibility of such a practical, near-future demonstration reactor is studied in this paper, based on a zero dimensional system analysis code study. It was shown that a net electric generation on the order of 300 MWe can be achieved below the optimistic β_N limit of 5. The elongation of K-DEMO is around 1.8 with single null configuration. Detailed optimization process and the resultant various plasma parameters are described.     

Antioxidant activities and nutritional properties of Jeonyak prepared with beef bone stock and gelatin

The antioxidant activities and nutritional properties of Jeonyak made with beef bone stock and gelatin were investigated. Traditional Jeonyak (J1) was prepared with beef bone stock, whereas modified Jeonyak was made with gelatin and honey (J2) or with gelatin and oligosaccharides (J3). All 3 kinds of Jeonyak had antioxidant activities and J1 had the highest activity. The α-glucosidase inhibitory activity was measured to investigate the antidiabetic effect and J3 had the highest inhibitory activity of 80.47%. Glycine was the most abundant amino acid in all 3 kinds of Jeonyak. Both traditional and modified Jeonyaks have antioxidative and antidiabetic effects, suggesting that Jeonyak can be used as an effective traditional functional food.     

Recent Progress of Innovative Perovskite Hybrid Solar Cells

Recently, innovative perovskite hybrid solar cells have attracted great interest in solar cell research fields, such as dye-sensitized solar cells, organic photovoltaics, thin-film solar cells, and silicon solar cells, because their device efficiencies are gradually approaching those of crystalline Si solar cells, and they can be fabricated by cheap low-temperature solution processes. Here, we review the recent progress of innovative perovskite hybrid solar cells. The introduction includes the general concerns about solar cells and why we need innovative solar cells. The second part explains the structure and the material properties of hybrid perovskite materials. We focus on why the hybrid perovskite materials can exhibit excellent solar cell properties, such as high open-circuit voltage. The third part introduces recent progress in innovative perovskite hybrid solar cells, in terms of device architecture and deposition methods for dense perovskite thin films with full surface coverage. The device architecture is important in attaining high power conversion efficiency; the device operating mechanism is dependent on the device structure; and the pinhole-free dense perovskite thin films with full surface coverage are crucial for achieving high efficiency. Finally, we summarize the recent progress in perovskite hybrid solar cells, and the issues to be solved, in the summary and outlook section.     

A novel method of making PVF porous foam without using the pore forming agent

Different with the conventional method of manufacturing poly(vinyl formal) (PVF) porous foam by using the pore‐forming agents such as wheat or potato starches, a novel method without using the pore‐forming agent is introduced in this article. Through the help of images taken by a scanning electron microscope, the formation process of the present PVF foam will be discussed in terms of the spinodal decomposition (SD) phase separation principle. Additionally, the effect of poly(vinyl alcohol) concentration and reaction temperature on the pore structure of the PVF foam will be investigated. Moreover, the water adsorption capacities of the PVF foams obtained by the present method will be studied in details through the analyses of pore‐size distribution, mechanical modulus, and thermal property. © 2014 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2015 , 132, 41270.     

A Surface Tailoring Method of Ultrathin Polymer Gate Dielectrics for Organic Transistors: Improved Device Performance and the Thermal Stability Thereof

Tailoring the surface of the dielectric layer is of critical importance to form a good interface with the following channel layer for organic thin film transistors (OTFTs). Here, a simple surface treatment method is applied onto an ultrathin (<15 nm) organosilicon‐based dielectric layer via the initiated chemical vapor deposition (iCVD) to make it compatible with organic semiconductors without degrading its insulating property. A molecular‐thin oxide capping layer is formed on a 15 nm thick poly(1,3,5‐trimetyl‐1,3,5‐trivinyl cyclotrisiloxane) (pV3D3) by a brief oxygen plasma treatment. The capping layer greatly enhances the thermal stability of the dielectrics, without degrading the original mechanical flexibility and insulating performance of the dielectrics. Moreover, the surface silanol functionalities formed by the plasma treatment can also be utilized for the surface modification with silane compounds. The surface‐modified dielectrics are applied to fabricate low‐voltage operating (<5 V) pentacene‐based OTFTs. The highest field‐effect mobility of the device with the surface‐treated 15 nm thick pV3D3 is 0.59 cm² V^?1 s^?1, which is improved up to two times compared to the TFT with the pristine pV3D3. It is believed that the simple surface treatment method can widely extend the applicability of the highly robust, ultrathin, and flexible pV3D3 gate dielectrics to design the surface of the dielectrics to match well various kinds of organic semiconductors.     

Effects of K2O Evaporation on the Structural Properties of KSbO3 Compounds

A specimen having a stoichiometric composition of KSbO₃·(KSb) calcined at 800°C has an R rhombohedral structure (RS), and changes to a Pn cubic structure (CS) when calcined at 1100°C. Finally, a <111>‐oriented rhombohedral phase is formed in the specimen calcined at 1230°C. K/Sb ratio decreases from 1.0 in RS, 0.93 in CS, and finally to 0.85 in <111>‐oriented rhombohedral phases. On the other hand, a specimen having a K‐excess composition of K_1.1SbO₃ calcined at 800°C shows a RS that is maintained in the K‐excess specimen calcined at 1230°C. The composition of these specimens is very close to KSb. Therefore, the RS with a space group of R is a stable form of KSbO₃. The formation of Pn cubic and <111>‐oriented R phases can be explained by the evaporation of K₂O during the calcination process at temperatures above 1100°C.