Effect of the interaction of drug-beta-cyclodextrin complex with bile salts on the drug absorption from rat small intestinal lumen

This investigation was concerned with the change of the bioavailability of a drug owing to the interaction of the drug-beta-cyclodextrin complex with bile salts in rat intestinal lumen. The absorption of sulfamethizole (SMZ) from rat intestinal lumen after administration of SMZ-beta-cyclodextrin complex was determined by a closed-loop method in the presence or absence of bile. The blood level of SMZ after administration of SMZ-beta-cyclodextrin complex was significantly decreased in comparison with that after administration of SMZ alone in bile duct-ligated rats. On the other hand, the blood level of SMZ after SMZ-beta-cyclodextrin administration in intact rats (bile duct non-ligated) or on the addition of sodium cholate was similar to the level in the case of SMZ alone. Thus, bile salts were found to act as a competing agent in the gastrointestinal tract.     

Effects of α-tocopherol and its acetate on the hydrolytic activity of phospholipase D in egg yolk phosphatidylcholine bilayers

Effects of -tocopherol (Toc) and -tocopherol acetate (TocA) on the hydrolysis activity of phospholipase D (fromStreptomyces chromofuscus) were studied in small unilamellar vesicles (SUV) of egg yolk phosphatidylcholine (PC). Choline produced in the reaction was monitored by use of a choline oxidase — oxygen electrode. Addition of 18 mol% Toc into SUV (2 mM PC) brought about a twofold rate of choline production. On the other hand, the effect of 18 mol% TocA in SUV was very small. The apparent maximum velocity,V _max(app), increased by addition of Toc in SUV. The apparent Michaelis constant,K _m(app), was unchanged by addition of Toc and TocA in SUV. The Toc and TocA molecules did not have significant effects when PC was solubilized in the micelles of heptaethylene glycol dodecyl ether. The effects of Toc and TocA are, therefore, not due to specific ones on the enzyme itself, but rather upon the bilayer-organization of the substrate. Measurements of spreading pressure showed complete miscibility of PC and Toc, and limited mutual solubility of PC and TocA, suggesting stronger attractive interactions between Toc and PC than those between TocA and PC in the bilayers.     

Retro-ene reactions in heterocyclic synthesis,III. A new route to 4,5-dihydrooxazoles and 5,6-dihydro-4H-1,3-oxazines

Methyl (E)-4,4-dimethyl-5-oxo-2-pentenoate ( 1 , X = O) reacted with 1,2- or 1,3-aminoalcohols 3 to yield oxazolidines 4a-c or tetrahydro-1,3-oxazines 4d,e. The corresponding imino ester 1 (X = NBu-t) also gave 4 on reaction with 3 . Compounds 4 on heating at 230° yielded 4,5-dihydrooxazoles 5a-c or 5,6-dihydro-4H-1,3-oxazines 5d,e along with methyl 4-methyl-3-pentenoate ( 6 ).     

On the protonation equilibria of sephadex C-25 and C-50

The system H(+)Na(+) has been studied on Sephadex C-25 and C-50 at two ionic strengths by potentiometry. The data have been fitted by the H?gfeldt three-parameter model. For ionic strength 0.100 M (Na)ClO(4) an excellent fit is obtained with a standard deviation of +/-0.013 for both gels. For ionic strength 0.010 M (Na)ClO(4) a satisfactory fit could only be obtained by excluding the lowest and highest pH-value for each gel.     

Pilot-plant for NOx, SO2 and HC removal from flue-gas of municipal waste incinerator by electron beam irradiation

According to the basic research performed using a small size reactor at TRCRE of JAERI, the electron beam irradiation process was proved to be very effective for NO_x, SO₂ and HC removals from flue-gas of municipal waste incinerators. Based on this result, a pilot-plant was constructed for the demonstration of NO_x, SO₂ and HC removal performance using electron accelerator of maximum energy 0.95 MeV and maximum power 15kW.The pilot-plant was constructed at Matsudo City waste Disposal Center. The flue-gas of 1,000 Nm³/hr is guided from the waste incinerator flue-gas line of 30,000Nm³/hr to the pilot-plant to be processed by spraying Ca(OH)₂ slurry or powder and irradiation with high-energy electron beam of the accelerator. NO_x, SO₂ and HC are removed simultaneously from the flue-gas by the enhanced reaction with Ca (OH)₂ under irradiation.A brief explanation of the pilot-plant and preliminary results of the experiments are introduced in this paper.     

Revisiting thiol-yne chemistry: Selective and efficient monoaddition for block and graft copolymer formation

The untapped potential of radical thiol-yne mono-addition chemistry is exploited to overcome the known limitations of thiol-ene chemistry in polymer coupling and block copolymer formation. By careful choice of alkyne, the reaction can selectively lead to the mono-addition product with efficiencies surpassing those achieved by traditional thiol-ene chemistry. This improvement is illustrated by the nearly quantitative synthesis of a variety of diblock and graft copolymers. © 2014 Wiley Periodicals, Inc. J. Polym. Sci., Part A: Polym. Chem. 2015 , 53, 319–326     

Inconsistency in the Stability Constants of Inorganic Polyphosphate Anions Determined by Potentiometry and Spectroscopy

Compared with cyclo -triphosphate anions, cyclo -tri- w -imidotriphosphate anions (Figure 1), cP 3 (NH) 3 3 m , form stable complexes with transition metal ions. Two experimental procedures, potentiometry and spectroscopy, have been applied to determine the stability constants of the complexes with Co 2+ , Ni 2+ , and Cu 2+ ions at 25;C and at I = 0.10 (NaClO 4 ). One-to-one (ML) complex formation has been assumed for the analyses. In the presence of sufficiently high concentration of metal ions, the log g 1 values determined by both methods are consistent with each other, whereas the log g 1 value determined by spectroscopy decreases with the decrease in metal ion concentration. This peculiar phenomenon cannot be explained by the presence of additional complexes, that is, ML 2 or M 2 L. One possible reasoning is agglomeration formation of ligand molecules mediated by countercations in aqueous solution.     

α,α′‐Diarylacenaphtho[1,2‐c]phosphole P‐Oxides: Divergent Synthesis and Application to Cathode Buffer Layers in Organic Photovoltaics

A divergent method for the synthesis of α,α′‐diarylacenaphtho[1,2‐c]phosphole P‐oxides has been established; α,α′‐dibromoacenaphtho[c]phosphole P‐oxide, which was prepared through a Ti^II‐mediated cyclization of 1,8‐bis(trimethylsilylethynyl)naphthalene, underwent a Stille coupling with three different kinds of aryltributylstannanes to afford the α,α′‐diarylacenaphtho[c]phosphole P‐oxides in moderate to good yields. X‐ray crystallographic analyses and UV/Vis absorption/fluorescence measurements have revealed that the degree of π‐conjugation, the packing motif, the electron‐accepting ability, and the thermal stability of the acenaphtho[c]phosphole π‐systems are finely tunable with the α‐aryl substituents. All the P?O and P?S derivatives exhibited high stability in their electrochemically reduced state. To use this class of arene‐fused phosphole π‐systems as n‐type semiconducting materials, we evaluated device performances of the bulk heterojunction organic photovoltaics (OPV) that consist of poly(3‐hexylthiophene), an indene‐C₇₀ bisadduct, and a cathode buffer layer. The insertion of the diarylacenaphtho[c]phosphole P‐oxides as the buffer layer was found to improve the power conversion efficiency of the polymer‐based OPV devices.     

Hepatic parenchymal enhancement at Gd-EOB-DTPA-enhanced MR imaging: correlation with morphological grading of severity in cirrhosis and chronic hepatitis

The aim was to clarify whether enhancement effects of the liver parenchyma in the hepatobiliary phase (HP) of gadolinium-ethoxybenzyl-diethylenetriamine pentaacetic acid (Gd-EOB-DTPA)-enhanced MR imaging were correlated with the morphological grading of the severity in cirrhosis. A total of 62 patients with chronic hepatitis or cirrhosis underwent Gd-EOB-DTPA-enhanced MR imaging. Relative enhancement (RE) of liver parenchyma was calculated from signal intensity (SI) measurements obtained at precontrast images (SIpre) and 20-min postcontrast HP images (SIpost) as: (SIpost-SIpre)/SIpre. Morphological MR grades of severity in cirrhosis were divided into four groups. Then, RE of liver parenchyma and morphologic MR grading were correlated. Regarding the morphologic severity of cirrhosis, the numbers of patients with MR grade 1, 2, 3 and 4 were 14 (23%), 7 (11%), 28 (45%) and 13 (21%), respectively. The mean REs of liver parenchyma in each group of MR morphologic grade 1, 2, 3 and 4 were 0.71±0.21, 0.62±0.16, 0.70±0.22 and 0.77±0.18, respectively. There was no significant correlation between the MR grading of morphologic severity and the RE of liver parenchyma at 20-min HP. Hepatic parenchymal enhancement in the HP of Gd-EOB-DTPA-enhanced MR imaging did not necessarily decrease according to the severity of morphologic changes in cirrhosis. This fact may suggest that the hepatic uptake of Gd-EOB-DTPA depends on the preserved hepatocytes function rather than the severity of morphologic changes in cirrhosis.