Solid-state interactions and drug release of teicoplanin in binary combinations with peracetylated α-, β-, and γ-cyclodextrins

Triacetyl α-cyclodextrin, triacetyl β-cyclodextrin and triacetyl γ-cyclodextrin were tested as possible hydrophobic carriers to prolong the release of hydrophilic teicoplanin (TCP). Physical–chemical characterization of individual components, drug-carrier physical mixtures at 0.5, 0.67 and 0.75 mass fraction of carrier, and the respective interaction products by kneading or evaporative crystallization under microwave irradiation was carried out using differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA). In vitro drug release in pH 7.4 phosphate buffer at 37 °C was determined by intrinsic dissolution rate (IDR) measurements on non disintegrating compressed discs. Solid-state interactions of TCP with triacetyl α-cyclodextrin by evaporative crystallization and kneading and with triacetyl β-cyclodextrin by evaporative crystallization (probably resulting in carrier amorphization) were demonstrated. The role of carrier hydrophobicity, carrier mass fraction and preparation method of solid drug-carrier combinations on solid-state drug-carrier interactions and slowing down of TCP release was assessed. Modulation of drug release can be achieved using TCP-triacetyl γ-cyclodextrin combinations at 0.5 mass fraction of carrier.     

Reactions of organomercury fulminates with acetylene derivatives

Organomercury fulminates react with acetylene derivatives to give unstable 3-(organomercurio)isoxazoles, which isomerize to 2-cyanoenolates. These are hydrolyzed with hydrochloric acid to the corresponding enols and are cleaved by water at the double bond. With monosubstituted acetylenes, substitution at the free position by the organomercury residue is predominant.     

FLUORESCENCE OF Euglena gracilis PHOTORECEPTOR PIGMENT: AN in vivo MICROSPECTROFLUOROMETRIC STUDY

Abstract— The spectroscopic characterization of the photoreceptor pigment is one of the main questions in the study of the photosensory transduction chains in photomotile microorganisms. One of the possible techniques that can be used is in vivo microspectrofluorometry. By means of a tunable dye-laser microspectrofiuorometer developed by us, we have investigated some of the spectroscopic properties of the photoreceptor pigment of the green flagellate Euglena gracilis. The in vivo fluorescence excitation spectrum has been determined and the fluorescence quantum yield has been measured. The results show that flavins are indeed present in the paraflagellar body of E. gracilis and that their fluorescence quantum yield is much lower than that of a free flavin. An estimate of the order of magnitude of the rate constants for primary molecular reactions is tentatively given.     

Researches on pyridodiazepines. Behavior of 7,8,9,10-tetrahydro-5-methylcyclopenta[e]pyrido[3,2-b][1,4]-diazepin-6(5H)-one with chloroacetyl chloride

Following a previous experiment, an original heteropolycyclic structure 4 was obtained by a reaction of chloroacetyl chloride with compound 3 bearing a conjugated double bond system. The condensation develops with an initial NH-chloroacetylation and ring closure by quaternarization of the pyridine nitrogen. This is achieved through an 1,4 -cycloaddition of chloroketene to make a pyranone ring.     

Hemithio-analogues of meisenheimer complexes and sulphide group activation of aromatic substitution by alkoxides

EtO^? in DMSO adds to ethylthiopicrate at C-3 to generate an ephemeral

-adduct which ends into 1-ethylthio-4-ethoxy-2,5-dinitrobenzene, whilst ethyl picrate gives two adducts of attack of EtS^? at C-3 or C-1.     

PHOTOMORPHOGENIC RESPONSES TO UV RADIATION. II: A COMPARATIVE STUDY OF UV EFFECTS ON HYPOCOTYL ELONGATION IN A WILD-TYPE AND AN aurea MUTANT OF TOMATO (Lycopersicon esculentum Mill.)

Hypocotyl growth in etiolated seedlings of wild-type and an aurea mutant of tomato (Lycopersicon esculenturn Mill.), that appears to be deficient in labile phytochrome, is strongly inhibited by UV radiation in the region of 300–400 nm. The role of phytochrome in the UV-mediated inhibition of hypocotyl growth was studied using different experimental approaches: (1) by comparing the effectiveness of treatments of increasing duration of exposure to 692 nm and UV radiation; (2) by modifying the UV spectral range with specific cut-off filters. The experimental results suggest that the UV-induced inhibition of growth in wild-type tomato is mediated to a large extent by the longer wavelengths of the UV-A region and is mediated mainly by phytochrome. In contrast, at wavelengths < 305 nm a strong UV-B effect was found in the aurea mutant, suggesting a preeminent action of a specific UV-B absorbing photoreceptor that displays less action in the wild-type.