From the fronds of Polystichum tripteron (KUNZE) P_R. a new norcarotenoid glycoside was isolated and shown to be (R, , R)--hydroxy-megastigma-, -dien--one--O-β--glucoside. The fronds of Dennstaedtia wilfordii (MOORE) CHRIST. contain the same glucoside.

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Repetitive liquefactions in angular and subangular gravels from an alluvial fan, in the case of two earthquakes with accelerations lower than that of a former which had caused liquefaction some months before, are described. The liquefaction took place from the surface, down to a depth of approximately 10 m. Water laden with sediments spouted out for some tens of minutes after the strong motion ceased. Knowledge of the grain size distribution of the sediments inside the body of the alluvial fan roughly defines the areas of the fan prone to future liquefaction. Non-repetitive liquefaction in overconsolidated fine fluvio-lacustrine sand of glacial origin at the unusual depth of 14 m to 16 m is also described. From the observation of sand lifted up for 10 m inside a large diameter well, and of that which spouted out from several microvents, it was estimated that extra-pore pressure was close to lithostatic conditions. Nevertheless, modeling of intrinsic pore pressure buildup on the DESRA2 programme gives lower values than the experimental one. Geotechnical characteristics of the 12 m-thick sandy stratum indicate that the upper part is unusually soft, either due to water circulation or past repetitive liquefactions which prevented reconsolidation. It is suggested that excess pore pressure generated by the earthquake was also due to redistribution of pressure from adjacent sediments.

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One method currently being considered for the disposal of high level radio-active waste is burial in the seabed. When a hot object is buried in soil, the temperature of the soil adjacent to the object is raised and there is transient heat flow away from the object. The rise in the temperature of the soil causes excess pore pressures to be generated and transient pore water diffusion also takes place. A finite element formulation of the coupled heat flow and consolidation problem is presented. The computer implementation of this formulation is found to compare favourably with analytical solutions based on the same physical principles.

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(,)-2,-エポキシ-,,11,11-テトラメチルシクロウンデカ-,-ジエン(2)をフムレン1((2,,)-,,11,11-テトラメチルシクロウンデカ-2,,-トリエン)より合成する既知の合成法は実際に牧率が低く合成的に問題がある.さらに,2の合成はその反応性や物性の研究のために簡単に高牧率で行われることが望まれる.今回,2の新たな合成法と簡便な精製法を見いだし,2を高牧率で1から合成することができたので報告する.1のジエポキシ化,続く再結晶により得られたジエポキシド()は二価のチタンにより還元されて,1(273%)と(25%)と少量のを含む2を主生成物(42.%)として与えた.1とは原料として再利用できる.2の精製は1と同様硝酸銀()錯体の結晶で行い,純粋な2は1から通算牧率32.0%で得られた.2の既知方法による合成は段階の反応と数回のカラム分離及び10%含浸シリカゲルカラム分離を必要とし牧率が極端に低い.今回,新しい2の合成法は2段階の反応で1回のカラム分離と再結晶により高い通算牧率を示す.

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Two new partially saturated tricyclic ring systems, , a, , , , 10, 10a, 11-octahydro-11-oxodibenz [, ] oxepins (a and ), and -thiepins (a and ) were synthesized. Compounds a and were desulfurized to give a pair of isomeric 2-methylbenzoylcyclohexanes (10a and 10). Deuterated a and (11a and 11) were prepared starting from butadiene- (12). The stereochemical features of a (trans), (cis), a (trans) and (cis) are compared with those of 10a, 10, 11a and 11 on the basis of proton nuclear magnetic resonance data.

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Nアルキル,:,10-ペリレンテトラカルボン酸モノアンヒドリド=モノイミド[a～]と芳香族アミン(アニリン,p-トルイジン,p-アニシジン,,-キシリジン,-アミノナゾベンゼン,およびo-フェニレンジアミン)を縮合して非対称型,:,10-ペリレンビス(ジカルボキシミド)誘導体-N-アルキル-N'-アリール-,:,10-ペリレンビス(ジカルボキシミド)(〔a～〕,〔a～〕,〔a～〕,〔a～〕,〔a～〕,および〔10a～〕)を合成した. これらの各誘導体はすべて赤色系の色相を示し, 顔料試験の結果N-ブチル-N'-アリール-,:,10-ペリレンビス(ジカルボキシミド)(たとえば〔〕や〔〕)がとくにすぐれた耐光性を示した.

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The correction factor (η_ie) for the ultimate bearing capacity of a footing placed adjacent to a slope, taking into account the combined effect of horizontal and vertical seismic loads, represented by horizontal and vertical seismic coefficients, k_h and k_v, respectively, was derived using a modified Janbu's slice method. The influence of slope angles ‘α’ on the values of ‘η_ie’ are studied here. It was found that the values of η_ie can be expressed as an exponential function of ‘k_h/(1-k_v)’ and ‘α’, with a measurable interdependency between ‘α’ and ‘η_ie’. The influence of ‘α’ on the value of ‘η_ie’ increases as the input value of ‘k_h/(1-k_v)’ increases. Equations derived based on the analytical results are proposed to account for this effect. Based on the analyses of 11 near-fault seismographers obtained in the 1999 Chi-Chi earthquake in Taiwan, a ratio between the vertical and the horizontal seismic coefficients, λ, of between ±0.25 is suggested for including the combined effect of vertical and horizontal seismic forces in evaluating the seismic bearing capacity of footings located in near-fault areas.

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At present, analytical or empirical formula for seismic bearing capacity of footings adjacent to slopes is not available. This study uses a pseudo-static-based approach in conjunction with rigorous Janbu's slice method to derive analytical values of seismic bearing capacity factors (N_γ) and correction factors for the effects of inertia of soil mass and load inclinations for a rigid footing adjacent to cohesionless slopes. It is shown that both the bearing capacity factors (N_γ) and the correction factors for the seismic bearing capacity of footings placed on level ground derived herein are comparable with those reported in the literature. Empirical equations regarding the effects of slope angles and load inclinations, expressed using generalized forms of those proposed in the literature, are also derived. It is also found that the empirical equations derived in the present study provide values of correction factors in good agreements with the analytical ones, indicating the validity of using these empirical equations for assessing the bearing capacity of rigid footings situated on the slope subjected to pseudo-static seismic loading.

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Background

The differences in conditions of enteric-coated acid-labile drug release and absorption between healthy subjects in bioequivalence studies and gastrointestinal patients in clinical practice can lead to significant differences in gastric stability of original PPIs and generics. Thus, pathologic duodenogastric reflux (PDGR) and the pH increasing within PPIs administration still remain unaccounted for.

Methods

Two-stage modified comparative dissolution testing of original omeprazole (OO) and four generics (G1;2;

;) was performed. At first, we moved drugs from solution with pH 1.2 (1.2±0.05) to pH .0 (.0±0.05) and measure concentration of omeprazole in solution by high-performance liquid chromatography. According to our self-developed formula, pH exposure time of resistance to PDGR for omeprazole is minutes, i.. the active substance should not be released within minutes at pH . The exposure at the second stage was conducted with pH (.0±0.05), that imitated gastric pH after PPI administration. And then we also moved drugs to pH with the subsequent measurement of omeprazole concentration.

Results

Omeprazole concentrations after

, 10, 15, 20, 30, 45, 60 minutes in pH solution at the first stage were different for OO and generics. For OO, these values were ,±0,%; 41,±,0%; 62,±,0%; 79,±2,%; ,±2,%; 81,±2,%; 80,±,%; for Generic1 - 0; 49,±,%; 88, ±2,%; 90,±,%; 88, 2±2,2%; 87,±2,0%; 85,±1,1%; for Generic2 - 0; 30,±,%; 66,±,2%; 76,±,%; ,±,%; 86,0±,%; ,±,%: for Generic - 80,±,%; ,±1,%; , ±,2%; ,±2,%; 81,±2,1%; ,1±2,0%; ,0±2,%; for Generic - ,±1,%; ,±0,%; ,2±1,2%; , ±0,%; ,±0,%; ,±0,%; ,±1,1%, respectively.

An analysis of the omeprazole concentration in pH

solution at the second stage revealed the following parameters after the same time: for OO - ,±0,%; 40, ±,0%; 62,±2,0%; 80,0±,1%; 85,±2,%; ,±,%; 80,±,%; for Generic1 - 0; 67,0±,%; 89,±2,%; 91, ±,%; 89,1±1,%; 88,±1,%; 87,±1,2%; for Generic2 - 0; 42,2±,%; 75,1±,%; 81,0±,0%; 88,±,2%; 88, ±1,%; 87,±1,0%; for Generic - 85,±0,%; 85,±0,%; ,±0,%; ,±,0%; ,±0,%; ,±0,%; ,±0,%, respectively. Generic release and degradation were completely realized at pH .

Conclusion

Decreased gastric stability of Generic

and Generic makes PDGR and inhibited gastric acid secretion due to PPIs administration the potential causes of decreased enteric-coated acid-labile drugs stability.

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11-Amino-, a, , , , 10, 10a, 11-octahydrodibebenzo[, ]thiepines (a-) and -oxepines (a-) were synthesized by the Leuckart reaction of , a, , , , 10, 10a, 11-octahydro-11-oxodibenzo[, ]thiepines (1a, )and -oxepines (2a, ) followed by hydrolysis of the reaction products a- and a-, respectively. The four diastereomers, cis(a-H, 10a-H)-cis(10a-H, 11-H) a and a, cis(a-H, 10a-H)-trans(10a-H, 11-H) and , trans(a-H, 10a-H)-trans(10a-H, 11a-H) and , and trans(a-H, 10a-H)-cis(10a-H, 11-H) and , were isolated and their configurations and conformations were elucidated by chemical methods together with ¹H-nuclear magnetic resonance spectroscopic and X-ray crystallographic analyses.

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Stereoselective synthesis of , - and , Z-β-ionylideneacetaldehydes was accomplished from the β-ionone tricarbonyl iron complex, and the latter was converted to Z-retinoic acid.

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 The stability of

‒tetrahydrocannabinol acetate (‒THC‒OAc) and ‒tetrahydrocannabinol acetate (‒THC‒OAc) in -liquid during storage was investigated. ‒THC‒OAc liquids in cartridges were stored at 80℃ or 30℃ for 28 days. The relative concentrations of cannabinoids in the liquids were measured by gas chromatography with flame ionization detection. ‒THC‒OAc decreased during storage at either temperature. ‒THC, a minor impurity, also decreased. ‒THC‒OAc liquid in a cartridge was stored at 80℃ for 57 days. The concentration of ‒THC‒OAc and ‒THC, a minor impurity, did not change during that time. Cannabinol acetate increased in all liquids, and unknown products were also detected by gas chromatography/mass spectrometry (GC/MS). The ‒THC‒OAc and ‒THC‒OAc liquids were subjected to GC/MS to detect representative diluents, glycerol, propylene glycol, and polyethylene glycol 400, but none of these were detected.

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The small strain stiffness and anisotropic nature of two sands with different geological origin have been determined via laboratory seismic tests performed in a triaxial cell. Dry triaxial reconstituted specimens of Ticino river silica sand (TS) and of Kenya carbonatic sand (KS) were subjected to isotropic and anisotropic states of effective stress ; then both shear and constrained compression waves were propagated in vertical, horizontal and oblique directions by means of five couples of piezoelectric transducers especially arranged in the specimens. The propagated compression and shear waves allow the assessment of the constrained M₀ and shear G₀ moduli respectively, at very small strains where, as a first approximation many soils can be assumed, from an engineering point of view, to behave as an elastic cross-anisotropic medium with a vertical axis of symmetry. This paper, after a brief description of the novel measuring technique adopted and of the tested materials, summarises the test results and their interpretation in order to separate the effects of the fabric anisotropy from those produced by the state of effective stresses on soil stiffness. The stiffness and anisotropic response of the two tested sands are compared. Finally the results enable us to establish five independent constants of the cross-anisotropic elasticity model, which appears to be appropriate to reproduce the behaviour at small strain of the two sands.

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A full account is given of the chemical behavior observed for , -dialkyladeninium salts (16). On treatment with boiling 1N aqueous NaOH for 60min, 16a, , , (X=I), 16 (X=Br), and 16 (X=) rearranged to isomeric , -dialkyladenines (21a-) in 50-91% yields. Treatment of the salts with 0.N aqueous at room temperature for 30-90min or with Amberlite CG-400 (OH^-) in H₂O at room temperature gave the ring-opened derivatives a- (in the trans-formamide form) in 56-% yields, and rate constants for the ring-opening reactions of 16a, , -g (X=) and 16 (X=Br) leading to a-g were determined in H₂O at pH . and ionic strength 0.50 at 25°. Cyclization of a with NaH in AcNMe₂ at room temperature or with boiling 1N aqueous NaOH produced 21a in % or 72% yield, respectively.In solution, the trans-formamides seemed to transform slowly into the cis-formamides 23, attaining equilibria. The existence of such an equilibrium in or Me₂SO- at 25° or in H₂O at pH . and ionic strength 0.50 at 25° was kinetically confirmed in the case of a, and the mechanism of the rearrangement of 16 to 21 through is discussed on the basis of the above kinetic results and Deslongchamps' theory of stereoelectronic control. On treatment with in MeOH at room temperature, 16a (X=I) furnished the , -dihydro derivative 28 (% yield), which slowly decomposed in H₂O at 60° to give a in 49% yield.The , -dialkyladeninium salts (16) were found to be obtainable from N'-alkoxy-1-alkyl--formamidoimidazole--carboxamidines () through an alternative synthetic route : Alkylations of with alkyl halides in HCONMe₂ in the absence of base, followed by hydrogenolysis of the N'-alkoxy group and cyclizatio (or vice versa) produced 16 in acceptable yields. In order to interpret the proton nuclear magnetic resonance spectrum of a, the 2-deuterated species 26 was also synthesized from 24 via 25 and 27.

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Circuit techniques to enhance the linearity of input-voltage-to-current (V/I) conversion and to increase the output impedance of a current source by compensating for the low intrinsic gain of a transistor were introduced to realize a high-frequency operational transconductance amplifier (OTA) for a low supply voltage using sub-100-nm CMOS processes. Applying these techniques, a MOS th-order Gm- linear-phase low-pass filter (LPF) was realized using a 65nm CMOS process. A simplified biquad LPF that can serve as a component of a th-order LPF was newly developed by replacing OTAs with resistors. As a result, the -dB frequency bandwidth, group delay ripple, rd-order distortion, and rd-order input intercept point (IIP) were 200MHz, 2.2%, ≤ -55dB with a 100MHz input, and +10.dBm, respectively, all with a ±0.1Vp-p input signal at each input terminal in the pseudodifferential configuration. The LPF including an output buffer dissipated 60mW in the case of a 1.2V supply. Wide spurious-free dynamic range (SFDR) characteristics were confirmed up to high frequencies.

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