The solubility of bosentan in aqueous-2-propanol mixtures at several temperatures,measurement and data correlation

ABSTRACT

The solubilities of bosentan (BST) in binary aqueous mixtures of 2-propanol at temperatures ranging from 293.15 to 313.15 K were determined using a shake-flask method. The produced data were modelled with the Jouyban-Acree-van’t Hoff model and difference between the predicted data and experimental ones were illustrated by percent average relative deviations (%ARD). Moreover, the thermodynamic functions of dissolution for BST in the aqueous 2-propanol solutions were computed which suggest that the dissolution process is endothermic and not spontaneous.     

Solvatochromic Solvent Polarity Measurements In Analytical Chemistry: Synthesiss And Applications Of Et-30

Abstract

The E_T(30) scale of solvent polarity has been shown to be useful in examining many diverse analytical processes. It is based on the charge transfer absorption of 2,6-diphenyl-4-(2,4,6-triphenyl-N-pyridinio)phenolate (referred to as ET-30 in this paper). Unfortunately, use of the E_T(30) scale has been hindered by (a) the lack of a commercial source of the ET-30 dye and (b) the lack of an English language synthetic procedure. Here we discuss recent applications of the E_T(30) scale to analytical techniques, as well as a simplified procedure for the synthesis of ET-30.     

离子色谱法同时测定水中六种阳离子

研究了用抑制电导离子色谱法一次进样同时测定水中Li^ ,Na^ , NH4^ ,Mg^2 ,Ca^2 的色谱法条件,相对标准偏差小于0．5％,加标回收率在97．5％－104．0％。在水质分析中运用t检验法,比较了用钙、镁离子浓度计算和传统方法测定的总硬度之间是否存在显著性差异。     

Comparison of three methods for fractionation and enrichment of low molecular weight proteins for SELDI-TOF-MS differential analysis

In most diseases, the clinical need for serum/plasma markers has never been so crucial, not only for diagnosis, but also for the selection of the most efficient therapies, as well as exclusion of ineffective or toxic treatment. Due to the high sample complexity, prefractionation is essential for exploring the deep proteome and finding specific markers.In this study, three different sample preparation methods (i.e., highly abundant protein precipitation, restricted access materials (RAM) combined with IMAC chromatography and peptide ligand affinity beads) were investigated in order to select the best fractionation step for further differential proteomic experiments focusing on the LMW proteome (MW inferior to 40,000 Da). Indeed, the aim was not to cover the entire plasma/serum proteome, but to enrich potentially interesting tissue leakage proteins. These three methods were evaluated on their reproducibility, on the SELDI-TOF-MS peptide/protein peaks generated after fractionation and on the information supplied.The studied methods appeared to give complementary information and presented good reproducibility (below 20%). Peptide ligand affinity beads were found to provide efficient depletion of HMW proteins and peak enrichment in protein/peptide profiles.     

Structure and Photoelectric Characteristics of Functional Polymers and of Compositions Based on Them

The electronic processes in disordered organic solids were analyzed, classified, and summarized. They include the photogeneration of charge pairs, electron transport, geminal and bimolecular recombination, and the capture of charge carriers in local electronic states. General criteria were formulated for the targeted search for and the creation of new prospective polymers and their compositions with organic pigments and related compounds having specific photoelectric characteristics for electrographic and holographic media, photoelectric converters, and electroluminescent and photorefractive devices.     

Structure-Activity Relationship of Insecticidal Steroids. V. 3β-Benzoyloxystigmastan-6-ones

The toxicity of steroid benzoates 4-10 for Colorado beetle (Leptinotarsa decemlineata Say.) larvae was studied by a contact-intestinal method. The most active growth and development regulator for this insect is 3-benzoyloxy-5-hydroxy-⁷-6-ketosteroid 9a.     

A Comparative Study of Naproxen – Beta Cyclodextrin Complexes Prepared by Conventional Methods and Using Supercritical Carbon Dioxide

Naproxen is a poorly soluble anti-inflammatorydrug, the solubility of which canbe enhanced by complexation withbeta-cyclodextrin. Besides that, the inclusioncomplex reduces the incidence of gastrointestinal side effects of the drug. The aim of this work was to compare the physicochemical characteristics of the solid complexes prepared by traditional methods (kneading, freeze-drying and spray-drying) and using a supercritical fluid technology. The unusual solvent properties of carbon dioxide above their critical temperature and pressure were exploited in order to prepare inclusion compounds. Complexes prepared using supercritical fluid technology showed similar properties to those of freeze-drying andspray-drying complexes as proved by DSC, FT-IRand UV.     

Improvement in the Physicochemical Properties of Ketoconazole through Complexation with Cyclodextrin Derivatives

Highly-soluble cyclodextrin derivatives, such as hydroxypropyl--cyclodextrin(HP--CD) and methyl--cyclodextrin (MEB), were tested as solubilizingagents for ketoconazole, with the aim of improving the physicochemical andbiopharmaceutical properties of this lipophilic imidazole antifungal agent. Productswere prepared in four molecular ratios by physical mixing, kneading and spray-dryingmethods. The kneaded products in a ratio of 1:2 and the spray-dried products exhibitedthe highest dissolution rates. The phase solubility diagrams of ketoconazole with thesecyclodextrins at 25 °C in water and in simulated intestinal medium wereconstructed. A solubility diagram of A_L type was obtained with HP--CD, and one of A_P type with MEB. The complexes were characterized by thermal methods(DSC, TG, DTG and DTA). Multicomponent systems were prepared with tartaric acid.The effects of water-soluble polymers, e.g., polyvinylpyrrolidone, on the aqueous solubility of ketoconazole were investigated. Particle size distribution, surface area, partition coefficient, heat of dissolution and wettability studies were also carried out. The formation of inclusion complexes was observed by means of thermoanalytical studies.     

Convenient preparative method for synthesis of methyl (Z)-3-aryl-2-(carbobenzoxyamino)acrylates by Wittig—Horner reaction with the use of Et3N as a base

The Wittig—Horner reaction of CbzNHCH(CO₂Me)P(O)(OMe)₂ (1) with ArCHO (2) in the presence of Et₃N as a base affords methyl (Z)-3-aryl-2-(carbobenzoxyamino)acrylates (3) with high degrees of diastereoselectivity (Z)/(E) > 101. One recrystallization of the crude product is sufficient to obtain isomerically and chemically pure (Z)-3.Translated fromIzyestiya Akademii Nauk. Seriya Khimicheskaya, No. 11, pp. 2218-2220, November, 1995.The authors are grateful to the Dupont company (USA) for financing this study     

The inclusion complex of piromidic acid with dimethyl-β-cyclodextrin in aqueous solution and in the solid state

Inclusion complex formation of piromidic acid (PA) with dimethyl--cyclodextrin (DM--CD) in aqueous solution and in the solid state was confirmed by the solubility method, differential scanning calorimetry (DSC) and proton nuclear magnetic resonance (¹H-NMR) spectroscopy. The apparent stability constant,K _c , of the complex was estimated to be 244 M^–1. The stoichiometry of the complex was given as the ratio 1:2 of PA to DM--CD. The dissolution rate of the PA/DM--CD complex was much greater than that of intact PA.Presented at the Fourth International Symposium on Inclusion Phenomena and the Third International Symposium on Cyclodextrins, Lancaster, U.K., 20–25 July 1986.