In Vitro–In Vivo Correlation of Tianeptine Sodium Sustained-Release Dual-Layer Tablets

Tianeptine tablets are currently marketed to be designed for immediate-release tablets. The tianeptine has a short half-life, making it difficult to design for sustained-release tablets and achieve bioequivalence with the tianeptine immediate-release tablet (Stablon^®). We established the in vitro–in vivo correlation (IVIVC) of three formulations of tianeptine sustained-release tablets according to their granule size. To evaluate sustained drug release, in vitro tests were performed in pH 1.2 media for 24 h. In vivo pharmacokinetic analysis was performed following oral administration of reference drug and test drug to beagle dogs. The dissolution profile revealed delayed release as the size of the granules increased. The dissolution results were confirmed in pharmacokinetic analysis, showing that the half-life was delayed as granule size increased. The final formulation and reference drug showed an equivalent area under the curve (AUC). Through this, IVIVC was established according to the size of the tianeptine sodium granules, which is the purpose of this study, and was used to predict in vivo pharmacokinetics from the formulation composition. This approach may be useful for determining optimal formulation compositions to achieve the desired pharmacokinetics when developing new formulations.     

Improvement of Biological Effects of Root-Filling Materials for Primary Teeth by Incorporating Sodium Iodide

Therapeutic iodoform (CHI₃) is commonly used as a root-filling material for primary teeth; however, the side effects of iodoform-containing materials, including early root resorption, have been reported. To overcome this problem, a water-soluble iodide (NaI)-incorporated root-filling material was developed. Calcium hydroxide, silicone oil, and NaI were incorporated in different weight proportions (30:30:X), and the resulting material was denoted DX (D5~D30), indicating the NaI content. As a control, iodoform instead of NaI was incorporated at a ratio of 30:30:30, and the material was denoted I30. The physicochemical (flow, film thickness, radiopacity, viscosity, water absorption, solubility, and ion releases) and biological (cytotoxicity, TRAP, ARS, and analysis of osteoclastic markers) properties were determined. The amount of iodine, sodium, and calcium ion releases and the pH were higher in D30 than I30, and the highest level of unknown extracted molecules was detected in I30. In the cell viability test, all groups except 100% D30 showed no cytotoxicity. In the 50% nontoxic extract, D30 showed decreased osteoclast formation compared with I30. In summary, NaI-incorporated materials showed adequate physicochemical properties and low osteoclast formation compared to their iodoform-counterpart. Thus, NaI-incorporated materials may be used as a substitute for iodoform-counterparts in root-filling materials after further (pre)clinical investigation.     

Ein Vergleich zwischen radioaktiver Markierung und Indikator-Aktivierungsanalyse bei der Messung von Verweilzeitspektren

An VK-Z-Rohren zur Herstellung von Polyamid wurden Verweilzeitspektren mit der Methode der radioaktiven Markierung und der Methode der Indikatoraktivierungsanalyse gemessen. Die nach den beiden Methoden ermittelten Verweilzeitspektren werden miteinander verglichen. Die Übereinstimmung der Verweilzeitspektren wird durch Gegenüberstellung der statistischen Momente und durch einen Test nach Kolmogoroff-Smirnov geprüft. Es wird der experimentelle Aufwand beider Verfahren diskutiert und eine Fehlerabschätzung durchgeführt.     

Zur Anreicherung der stabilen Isotope des Schwefels durch Fest-Flüissig-Austausch unter Verwendung von Ionenaustauschern

An verschiedenen Systemen chemischer Verbindungen wurden Versuche zur Anreicherung des stabilen Isotopes ³⁴S unter Verwendung der Ionenaustauscher Wofatit L 150, SBW und SBK nach den Methoden der Frontalchromatographie und der Bandenverdrāngungschromatographie ausgeführt. Beim Isotopenaustauschsystem Hydrogensulfit (am Ionenaustauscher)/Schwefeldioxid (in wäβriger Lösung) wurden Verfahrensweise und Betriebsparameter hinsichtlich des Anreicherungsgrades optimiert. Mit Hilfe einer einfachen Methode gelang es, aus den Versuchsergebnissen Werle für den elementaren Trennfaktor und die Trennstufenhöhe zu berechnen.     

One-step synthesis ofα,β-unsaturated arylsulfones by a novel multicomponent reaction of aromatic aldehydes,chloroacetonitrile, benzenesulfinic acid sodium salt

A new and green method for the synthesis of α,β-unsaturated arylsulfones had been achieved through the condensation of aromatic aldehydes,chloroacetonitrile,benzenesulfinic acid sodium salt in the presence of l-butyl-3-methyl imidazolium hydroxide([bmim]OH) in EtOH under reflux.The ionic liquid was recovered and recycled for subsequent reactions.The advantages of this protocol were non-toxic,easy work-up and good yields.     

Effect of Surfactant Type and Concentration on Surfactant Migration,Surface Tension,and Adhesion of Latex Films

The effect of surfactant type and concentration on the migration behavior of surfactant in a latex film was investigated. Two types of surfactant, including an anionic (sodium lauryl sulfate, SLS) and a non-ionic (nonylphenol ethoxylate, average number of ethylene oxide units = 40, NP-40) surfactant, were used in an emulsion polymerization of methyl methacrylate butyl acrylate copolymer (MMA–BA). The total amount of surfactant was varied in three levels, i.e., 1.5, 3, and 4.5 wt%, and the surfactants were used both pure and in a mixture state. The surfactant migration to the film–air (F–A) and film–substrate (F–S) interfaces of the latex films was determined by using an attenuated total reflection-Fourier transform infrared (ATR-FTIR) method. In addition, the adhesion of the latex films to glass substrates was measured by a pull-off test. The results showed that the migration of anionic surfactant to the interfaces was greater than the non-ionic one. It was also found that the use of non-ionic surfactant along with anionic surfactant could decrease the migration of the anionic surfactant to the interfaces.     

荧光法研究对-二甲氨甲基-杯[8]芳烃与二苯胺磺酸钠包结作用

用荧光法研究了水溶性对-二甲氨甲基-杯[8]芳烃与二苯胺磺酸钠的相互作用。发现当对-二甲氨甲基-杯[8]芳烃加入到二苯胺磺酸钠溶液时,二苯胺磺酸钠的荧光峰发生了明显的蓝移,荧光增强,可能的作用机理是二苯胺磺酸钠中的磺酸根与对-二甲氨甲基-杯[8]芳烃中带正电的氮原子之间有较强的静电作用,二苯胺磺酸钠进入了对-二甲氨甲基-杯[8]芳烃的疏水空腔。同时研究了几种有机溶剂对包结物的荧光强度的影响,初步探讨了其作用机理。     

Preparation and characterization of titania based nanowires

A new method for preparation of titania nanowires with diameter around 10 nm and length up to 2–3 μm is described. The precursor was prepared from sodium titanate by adding ethylene glycole (EG) and heating at temperature of 198°C for 6 h under reflux. The sodium titanate glycolate formed by this way aggregated into 1D nanostructures and was subsequently transformed into titania glycolate during a chemical treatment with 98% sulfuric acid. Titania nanowires with variable amount of anatase and rutile were prepared by heating to temperatures in the range 350–1000°C. The precursor as well as titania based samples were characterized by X-ray diffraction, Infrared spectroscopy, Scanning electron microscopy, High resolution transmission microscopy, Thermogravimetry, Differential thermal analysis, Evolved gas analysis and Emanation thermal analysis. The nitrogen adsorption/desorption was used for surface area and porosity determination. The photoactivity of the prepared titania samples was assessed by the photocatalytic decomposition of 4-chlorophenol in an aqueous slurry under UV irradiation of 365 nm wavelength.