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41.
Zoltán-István Szabó Réka Gál Zsolt Gáll Szende Vancea Emőke Rédai Ibolya Fülöp Emese Sipos Gabriella Donáth-Nagy Béla Noszál Gergő Tóth 《Journal of inclusion phenomena and macrocyclic chemistry》2017,88(1-2):43-52
Rufinamide (RUF) was characterized in terms of cyclodextrin (CD) complexation in order to improve its aqueous solubility. Binary systems of RUF with three CDs—β-cyclodextrin (β-CD), randomly methylated-β-cyclodextrin (RAMEB) and sulfobutylether-β-cyclodextrin (SBE-β-CD)—were characterized with a wide variety of analytical techniques. Liquid state characterization was carried out by complementary techniques such as nuclear magnetic resonance spectroscopy (NMR), capillary electrophoresis (CE), mass spectrometry (MS) and phase solubility studies. The latter revealed that the stability of the complexes decreased in the order of RAMEB?>?β-CD?>?SBE-β-CD. AL-type diagrams were obtained in all cases, characteristic of 1:1 stoichiometry, with a maximum of over 15-fold increase in RUF solubility, when complexed with RAMEB. NMR Job plot and MS studies confirmed phase solubility results, regarding the binding stoichiometry. 1H NMR and 2D ROESY investigations revealed the inclusion of the triazole moiety of RUF, confirmed by molecular modeling. Solid state complexation in 1:1 molar ratio was carried out by kneading method and investigated by differential scanning calorimetry (DSC) and infrared spectroscopy (IR). Comparative dissolution studies indicated an over two-fold improvement in dissolution efficacy of the kneaded products, when compared to the pure drug. Results of the present study might pave the way for a drug formulation with improved bioavailability. 相似文献
42.
Don Page 《Physics letters. [Part B]》1978,79(3):235-238
A compact rotating gravitational instanton (a positive-definite metric solution of the Einstein equations with Λ term) is presented. The manifold is the nontrivial S2 fibre bundle over S2 and has χ = 4, τ = 0, but no spinor structure. The metric can be obtained from a special limit of the positive-definite analytic extension of the Kerr-de Sitter metric or alternatively from the Taub-NUT metric with Λ term. The action is about less negative than that of the Einstein metric on the trivial bundle S2 × S2. 相似文献
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Brainstem electrical responses (BSER) to 60-dB-SL click in noise high passed at various cutoff frequencies separated b 1/2-octave steps were recorded in normal-hearing adult subjects. By applying a derived response technique, narrow-band contributions to the BSER from specific portions of the basilar membrane were revealed. Latencies and amplitudes of the various waves in the derived BSER were recorded. Results indicate that nearly the whole cochlear partition can contribute to the brainstem response. The shifts in latency of waves I, III, and V and amplitude changes of waves I and III as a function of CF appear to be fully comparable to those of the AP. In contrast, the amplitude behavior of wave V as a function of CF is different from waves I and III depending upon frequency range. The discrepency in the behavior of wave V with respect to the earlier waves suggests some sort of neural reorganization at the level where was V is generated. The fact that there are contributions to the brainstem response from apical portions of the cochlea opens the possibility for extending the brainstem technique in assessing the higher cochlear turn function. 相似文献
46.
Don Weingarten 《Nuclear Physics B》1974,70(3):501-533
We will define a sequence of functions called density correlations which measure statistical correlations between momentum space densities of particles in the ensemble of inelastic final states produced by scattering a pair of hadrons. Then we will show that early multiplicity scaling of the distribution of charged particles produced by pp collisions can primarly be explained by the assumption that fluctuations of the density of charged particles are quite random and therefore higher correlation functions are small in an appropriate sense, combined with the assumption that the first three density correlations fulfill an approximate form of Feyman scaling at small values of x. These assumptions will aslo be used to derive an expression for the scaling function Ψ(η) which is completely determined by <N2>S/<N>S2 and <N3>S/<N>S3, and recursion relation to calculate <Nm>S/<N>Sm, m ? 4, from <N2>S/<N>S2 and <N3>S/<N>S3. The prediction for Ψ(η) accurately reproduces data in the interval 0.2 ? η ? 3.1, 50 GeV/c ? pL ? 303 GeV/c, and the predictions for <NS>m/<N>Sm, 4 ? m ? 10, agree with observed values in the interval 50 GeV/c ? pL ? 303 GeV/c. 相似文献
47.
Don N. Page 《Physics letters. A》1982,91(2):57-60
Quantum mechanics can completely describe what may actually be predicted about any system, contrary to the argument of Einstein, Podolsky, and Rosen. One does not however need to restric predictions to specified experimental arrangements as Bohr did. 相似文献
48.
Partial fluorination overcomes herringbone crystal packing in small polycyclic aromatics 总被引:1,自引:0,他引:1
[structure: see text] We report the synthesis and characterization of partially fluorinated condensed tetracyclic aromatic compounds. Typical edge-to-face/herringbone packing of nonfluorinated analogues is replaced here by columnar stacks with disk planes orthogonal to the columnar axes. Enhanced pi-overlap results with overlaid electron-poor and -rich regions. 相似文献
49.
Bunch J Clench MR Richards DS 《Rapid communications in mass spectrometry : RCM》2004,18(24):3051-3060
Matrix-assisted laser desorption/ionisation (MALDI) quadrupole time-of-flight mass spectrometry (Q-TOFMS) has been used to detect and image the distribution of a xenobiotic substance in skin. Porcine epidermal tissue was treated with 'Nizoral', a medicated shampoo containing ketoconazole (+/-)-1-acetyl-4-[p-[[(2R,4S)-2-(2,4-dichlorophenyl)-2-(imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]piperazine) as active ingredient. Following incubation for 1 h at 37 degrees C all excess formulation was washed from the surface. A cross-section of the drug-treated tissue was then blotted onto a cellulose membrane, precoated in matrix (alpha-cyano-4-hydroxycinnamic acid (CHCA)), by airspray deposition. In separate experiments the tissue surface was treated with Nizoral within a triangular former, and subsequently blotted onto a matrix-coated membrane. Sample membranes were then mounted into the recess of specialised MALDI targets with adhesive tape. All samples were analysed by MALDI-TOFMS using an Applied Biosystem 'Q-star Pulsar i' hybrid Q-TOF mass spectrometer fitted with an orthagonal MALDI ion source and imaging software. Detection of the protonated molecule was readily achievable by this technique. Treatment of the tissue within a template gave rise to images depicting the expected distribution of the drug, demonstrating that this technique is capable of producing spatially useful data. Ion images demonstrating the permeation of the applied compound into the skin were achieved by imaging a cross-sectional imprint of treated tissue. A calibration graph for the determination of ketoconazole was prepared using the sodium adduct of the matrix ion as an internal standard. This enabled construction of a quantitative profile of drug in skin. Conventional haematoxylin and eosin staining and microscopy methods were employed to obtain a histological image of the porcine epidermal tissue. Superimposing the mass spectrometric and histological images appeared to indicate drug permeation into the dermal tissue layer. 相似文献
50.