Effect of surface covering of lactose carrier particles on dry powder inhalation properties of salbutamol sulfate

The effect of the surface covering of lactose carrier particles on the dry powder inhalation properties of salbutamol sulfate was investigated. Lactose carrier surfaces were covered with sucrose tristearate (J-1803F) by a high-speed elliptical-rotor-type powder mixer (Theta-Composer). In the present study, drug/carrier powder mixtures were prepared consisting of micronized salbutamol sulfate and lactose carriers with various particle surface conditions prepared by surface covering. These powder mixtures were aerosolized by a Jethaler), and the in vitro inhalation properties of salbutamol sulfate were evaluated by a twin impinger. Compared with the powder mixed with uncovered lactose carrier, the in vitro inhalation properties of the powder mixture prepared using the surface covering lactose carrier were significantly different, showing that the in vitro inhalation properties of salbutamol sulfate were improved. In vitro inhalation properties increased with the percentage of J-1803F added. Using this surface covering system would thus be valuable for increasing the inhalation properties of dry powder inhalation with lactose carrier particles.     

Inhibition of acetylcholinesterase activity by essential oil from Citrus paradisi

Inhibition of acetylcholinesterase (AChE) activity by essential oils of Citrus paradisi (grapefruit pink in USA) was studied. Inhibition of AChE was measured by the colorimetric method. Nootkatone and auraptene were isolated from C. paradisi oil and showed 17-24% inhibition of AChE activity at the concentration of 1.62 microg/mL.     

Influence of storage humidity on the in vitro inhalation properties of salbutamol sulfate dry powder with surface covered lactose carrier

The influence of storage humidity on the in vitro inhalation properties of salbutamol sulfate dry powder with surface covered lactose carrier was investigated. In the present study, drug/carrier powder mixtures were prepared consisting of micronized salbutamol sulfate and lactose carriers with different particle surface conditions prepared by surface covering. Lactose carrier surfaces were covered with vegetable magnesium stearate (Mg-St-V) by a high-speed elliptical-rotor-type powder mixer (Theta-Composer). These powder mixtures were aerosolized by a Jethaler), and the in vitro inhalation properties of salbutamol sulfate were evaluated by a twin impinger. Compared with the powder mixed with uncovered lactose carrier, the in vitro inhalation properties of the powder mixture prepared using the surface covered lactose carrier were little decreased with increased in relative humidity (RH), showing that the in vitro inhalation properties of salbutamol sulfate were improved at high RH. Using this surface covering technique would thus be valuable for storage humidity of dry powder inhalation (DPI) with lactose carrier particles.     

Electrodeposition of manganese and molybdenum mixed oxide thin films and their charge storage properties

Manganese and molybdenum mixed oxides in a thin film form were deposited anodically on a platinum substrate by cycling the electrode potential between 0 and +1.0 V vs Ag/AgCl in aqueous manganese(II) solutions containing molybdate anion (MoO(4)2-). A possible mechanism for the film formation is as follows. First, electrooxidation of Mn2+ ions with H2O yields Mn oxide and protons. Then, the protons being accumulated near the electrode surface react with MoO(4)2- to form polyoxomolybdate through a dehydrated condensation reaction (by protonation and dehydration). The condensed product coprecipitates with the Mn oxide. Cyclic voltammetry of the Mn/Mo oxide film-coated electrode in aqueous 0.5 M Na2SO4 solution exhibited a pseudocapacitive behavior with higher capacitance and better rate capability than that of the pure Mn oxide prepared similarly, most likely as a result of an increase in electrical conductivity of the film. Electrochemical quartz crystal microbalance and X-ray photoelectron spectroscopy clearly demonstrated that the observed pseudocapacitive behavior results from reversible extraction/insertion of hydrated protons to balance the charge upon oxidation/reduction of Mn3+/Mn4+ in the film.     

Lewis acid-activated chiral leaving group: enantioselective electrophilic addition to prochiral olefins

A new strategy using a BINOL derivative as a chiral leaving group and Lewis acid has been developed for enantioselective alkylation of prochiral olefins. (R)-2,2'-Bis[2-(trimethylsilyl)ethoxymethyl]-1,1'-binaphthol is demonstrated to be an effective reagent for enantioselective hydroxymethylation of silyl enol ethers and trisubstituted alkenes. Electrophilic addition to prochiral olefins is accompanied by cleavage of an acetal that is dual activated by SnCl4 and the delta-effect of silicon through the S(N)2 substitution process. Enantioselective synthesis of cyclic terpenes is also described using this strategy.     

A convenient preparation of 3,3,3-trifluoro-1-propynylamines and their Lewis acid catalyzed reaction with carbonyl compounds leading to (z)-alpha-(trifluoromethyl)-alpha,beta-unsaturated amides

N,N-Dialkyl(3,3,3-trifluoro-1-propynyl)amines were readily prepared by a three-step procedure starting from commercially available 2,2,3,3,3-pentafluoropropanol. These fluorinated alkynylamines reacted smoothly with a variety of aldehydes or ketones in the presence of a catalytic amount of Lewis acid and molecular sieves 4A at ambient temperature to produce the corresponding alpha-(trifluoromethyl)-alpha,beta-unsaturated amides in good to excellent yields with high Z-stereoselectivity.