ラットに

3H

-CU-

83

(S)を25μg/kgで静脈内あるいは経口投与し，血液中濃度および尿糞中排泄を検討した．
静脈内投与後の血液中濃度推移は投与後5分より上昇し，投与後45分に25.74ng eq./mlのC_maxを示し，それ以後t_1/2

3

.05時間とt_1/2 33.09時間の二相で減少した．投与後72時間までのAUCは135.42ng eq.·hr/mlであった．
経口投与では，投与後

3

時間でC_max

4

.10ng eq./mlに達し，以後t_1/2α

4

.46時間とt_1/2β 26.

83

時間の二相で減少した．投与後72時間までのAUCは48.62ng eq.·hr/mlであった．
静脈内投与と経口投与のいずれの場合も，尿および糞中への放射能の排泄は，投与後48時間でほぼ終了した．静脈内投与では，投与後72時間までに投与量の30.52%が尿中に，60.42%が糞中に排泄された．経口投与では，同じく72時間までに40.34%が尿中に，69.24%が糞中に排泄された．

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The numerical values of the intervals betrween optieal levels are competed for the configurations *⁹4s, 5s, 6s and s of Cu⁺, according to the general expression of energy-levels derived in the previous paper The self-consistent field radial functions computed by Hartree adn Hartree are used for1s, 2s, 2p, s, p and . Those of s, 5s, .s and are ealenlated from Hartree Hartree's core-functions by the numerical integrations. The calculated results are shown in Table I.The agreement with experiment is satisfactory

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A total of 176

E

. coli isolates were retrieved from 203 diarrheic fecal samples collected from Korean cattle on 117 different farms. The most frequently observed resistance in

E

. coli isolates was to tetracycline (.6%), followed by streptomycin (80.%) and ampicillin (64.%). Resistance to cefazolin, cefoperazone, cefepime and amikacin was very low. Of the 176

E

. coli strains, forty (.%) isolates from 30 farms showed resistance to fluoroquinolones (FQ). All the FQ-resistant strains possessed double mutations at codons and 87 in the gyrA gene, and a single mutation mostly at codon 80 in the parC gene, except in one isolate. The pulsed-field gel electrophoresis profiles of the FQ-resistant

E

. coli isolates were heterogeneous, but two or three isolates that showed an identical pattern originated from the same or different farms. This study demonstrates that FQ resistance is frequently observed in

E

. coli from diarrheic cattle and that mutations in the quinolone resistance-determining region are the same as those seen in

E

. coli originating from other animal species and humans. The FQ resistance in diarrheic cattle might have been mostly acquired independently, although the possibility of transmission of FQ-resistant

E

. coli within a farm or between farms is plausible.

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性周期における牛の末梢血中遊離estrogen測定にITTRICH螢光法を応用して次の成績を得た。
Ittrich colorの最大波長をspectrofluorometer Hitachi MPF-2AおよびType203で測定した結果,励起光538nm,螢光552.5nmであった。この螢光特性は, およびにそれぞれ共通であった。実際の測定では最大波長が接近しているので感度は若干低下するが510~520nmで励起し•螢光側552•5±•5nmを読み,ALLENの補正を行なった。この条件において,および-methyletherの最少検出量は1ngであった。回収率補正の目的で加えた6,-

3H

-

E₂

-17βの全過程における回収率は平均60.

3

±11.

7

%であった。正常性周期を示す黒毛和種2頭の頸静脈血についてestrogenを分画測定した。その結果,両牛共

E₁

,

E₂

の各消長型は性周期の全期間を通じてほぼ同じ傾向を示したが,

E₂

は

E₁

にくらべ全般に高値であった。また

E₃

は検出されなかった。これらの牛のtotalestrogenは発情前期に増加し,排卵前に鋭いピーク(35.

3

および

99.8ng

/l;

E₁5.9

および16.0ng/l,

E₂29.4

および

83.8ng

/l)を形成し,排卵後は急激に減少して最低値(

3

.

8

~

5.3ng

/l;

E₁1.6

および1.9ng/l,

E₂2.2

および

3.4ng

/l)を示した。黄体期の最高値(10.1および27.0ng/l;

E₁2.4

および

3.4ng

/l,

E₂7.7

および23.6ng/l)は排卵後6~

8

日に認めた。すなわちestrogenの血中濃度は性周期の間に2つのピークを形成することを認めた。

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Chemical synthesis of (, 24R)- and (, 24S)-1, 24-dihydroxy--vitamin has been achieved starting with the commercially available dinorcholenic acid acetate. Synthesis involved introduction of the 1-hydroxy group by a reduction of the 1, 2-epoxide generated by epoxidation of the 1, , 6-trien--one. The side chain on the steroid was then constructed by means of a Wittig reaction followed by introduction of the bond by standard methods and its protection with 1-phenyl-1, 2, -triazoline-, 5-dione. Subsequent reduction of the hydroxy groups in the steroid side chain followed by reduction of the Diels-Alder addition products yielded the both 24-isomers. The 5, -dienes were irradiated and the corresponding vitamin compounds isolated. Nuclear magnetic resonance was used to identify individual isomers. The (, 24S)-1, 24-hydroxyvitamin compound bound equally well to the chick intestinal cytosol receptor as 1, 25-dihydroxyvitamin , while the 24R-isomer was approximately ten times less active. In vivo, both isomers were less active than 1, 25-dihydroxyvitamin ; however, the 24S-isomer was considerably more active than the 24R-isomer approaching the activity of 1, 25-dihydroxyvitamin .

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In the 1993 Kushiro-oki Earthquake of Richter magnitude ., simultaneous recording of earthquake motions was successfully made at the ground surface and at a depth of 77 meters in a dense saturated sand deposit. The peak horizontal acceleration was 0.47 g on the ground surface and 0.21 g at a depth of 77 meters. The acceleration record at the ground surface showed a distinctive ground response, which consisted of a cyclic motion having a period of about 1.5 seconds overlain by a spike at each peak of the motion. In order to study the mechanism of this peculiar ground response, effective stress analysis was conducted on the dense saturated sand deposit. The model used for this study was a strain space multiple mechanism model, which takes into account the effect of principal stress axis rotation. The recorded earthquake motion at a depth of 77 meters was used as the input earthquake motion for the analysis. Sampling after in-situ freezing was done in order to evaluate the properties of the sand. The results of the analysis indicated that the observed ground response was due to the effect of dilatancy of sand, which plays a significant role in the response of the dense saturated sand deposits during strong earthquake motions.

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本検討は, 経皮的冠動脈形成術 (PCI) 後の翌日血液透析 (HD) 時における透析中低血圧 (IDH) の発生因子について検討した. 対象は待機的PCI後, 翌日HDを施行した慢性HD患者連続

名 (年齢70±歳, 男性64名). IDHの定義は, 収縮期血圧20mmHg以上の低下で, 症状を伴いかつHD中断を要したものとした. また, HD記録よりIDHを後方視的に調査し, Logistic回帰分析にてIDHの予測因子を検討した. IDH群 (12名) は非IDH群 (71名) に比して, 有意に低体重 (52.0±. vs. 62.9±1.5kg; p=0.007), 造影剤量/体重が多く (2.5±0. vs. 1.±0.1mL/kg; p=0.018), 低左室駆出率で (45.±.2 vs. 56.0±1.% ; p=0.030), /’ が高値 (.9±. vs. 17.2±0.9cm/sec; p=0.038) であった. また, 冠動脈病変や侵襲的な治療について有意差は認めなかった. Logistic回帰分析では, 造影剤量/体重 (OR, 6.87; 95%CI, 1.-25.; p=0.004) がIDHの有意な予測因子であった. 造影剤使用量が多い症例は, IDHを生じる危険性が高いことが示唆された.

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We screened the differentiation-inducing activities of 39 mushroom extracts from Akita prefecture, Japan, on the mouse osteoblastic cell line, MCT-1. Sixteen phosphate buffered saline (PBS), boiled PBS, 14 ethanol and 12 methanol extracts induced alkaline phosphatase (ALP) activities, an indicator of MCT-1 cell differentiation. The enzyme activities were markedly induced by extracts of Tricholoma auratum, and we isolated the active compound from methanol extracts of this mushroom. Physical data for the isolated active compound were identical to those for (,24R)-ergosta-,-diene-,5α,6β-triol (1). 1 induced ALP activities of MCT-1 cells and promoted cell proliferation. To investigate the relationships between the chemical structure and differentiation-inducing activity of the compound, ALP-inducing activities of MCT-1 cells by 1, ergosterol (2), ergocalciferol (), cholesta-,5α,6β-triol (), -dehydrocholesterol (5) and cholecalciferol (6) were tested. The enzyme activities of MCT-1 cells were increased .0-fold by 10 μM 1 and 2.-fold by 10 μM . However, 2, , 5 and 6 did not induce MCT-1 cell ALP activity at 0.1—10 μM. These results suggested that the OH groups at C-5 and/or C-6 of 1 and played an important role in their differentiation-inducing activities on MCT-1 cells. Furthermore, 1 suppressed induction of MCT-1 cell apoptosis by serum starvation.

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Stress wave theory is applied to open-ended pipe piles to clarify the effects of soil plug on the behaviour of piles during driving and static loading. Measured field data and various numerical models are reviewed ; methods are presented to calculate wave propagation in both the pile and the soil plug ; modelling is presented which takes into account the interaction between the soil plug and the pile ; also presented is simplified method to estimate the loadsettlement relation of the pipe pile in static loading. By correlating observed and calculated values in two analytical cases, the authors demonstrate that incorporation of the soil plug (modelled as a series of masses and springs) is required to correctly predict pile behaviour during driving and static loading.

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In this paper, centrifuge shaking table tests were conducted in order to understand the performance of seawalls during a seismic event. The model tests showed that the displacement of the caisson was much affected by the seaward shear deformation of the sand seabed beneath it during shaking. It was also confirmed that an armored embankment played an important role in the displacement of the caisson during shaking. Based on these test results, a two-dimensional DEM-FEM coupled analysis method was newly developed to numerically predict the deformation of seawalls covered with armored embankments during earthquakes. The movements of the armor units were calculated by DE analysis and deformations of the caisson, rubble mound, sand seabed and backfill were calculated by FE analysis considering the non-linearity of the soil materials based on the effective stress. Dynamic interaction was taken into account by delivering the nodal displacements of the finite elements or the nodal forces converted from the contact forces through the imaginary distinct elements defined at the boundaries between the DE and FE domain. The applicability of this method to the prediction of the deformation of seawalls was verified through numerical simulations of the centrifuge model test.

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Seismic records obtained from a seismometer array located in downtown Tokyo Japan for about ten years were inversely analyzed to estimate the dynamic soil parameters. Due to the illposed nature of the problem, the simple and often used "least square method" does not properly estimate the parameters. The Extended Bayesian Method combined with the Akaike Bayesian Information Criterion was introduced to overcome this difficulty. The results obtained were compared with dynamic triaxial test results obtained at the time of the seismometer installation. The shear moduli agree quite well with the estimated results, however the damping ratios estimated are slightly higher than the ones obtained in the laboratory.

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The acetone extracts from three samples of the hepatopancreas of the poisonous scallops obtained on the Okhotsk Coast of Hokkaido Island were fractionated into two parts, hexane soluble fraction (fraction H) and 85% aqueous ethanol soluble fraction (fraction ) by partition to two layers. The majortoxic components in the mouse assay of “diarrheic shellfish toxin” by intra-peritoneal injection were found to be free unsaturated fatty acids showed the following toxicity in MU per g, 18:1 n-9 35, 18:2 n-6 , 18: n- 167, 18: n- , 20:5 n- 167, and :6 n- , respectively. Toxicity of the fraction Hin MUper g was much lower than that of the fraction . However, the toxicity of the fraction H per 1 g of the hepatopancreas was about twice that of the fraction , since the fraction Hwas much more abundant than the fraction in the hepatopancreas. The method for the assay of the diarrhetic shellfish toxin must be reexamined by considering the toxic effect of the free unsaturated fatty acids.

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The mechanism of wave-induced instability in a permeable seabed have been studied for more than two decades. The distinction between shear failure and liquefaction, however, has not been clearly defined. This paper presents a fundamental study on the differences in two failure modes for a fully saturated seabed of both finite and infinite thickness. The wave-induced effective stresses and pore pressure, obtained from an analytical solution of Biot's pore-elastic consolidation theory, were employed to examine the failure modes under a two-dimensional plane strain condition. A case study is presented to examine the failure modes with respect to several parameters, such as excess pore pressure, seepage flow, seepage force, failure areas and stress path in the seabed. The conclusions obtained from this study were as follows ; (1) the thickness of a permeable seabed affects the pore pressure and effective stress response to ocean waves and the failure mode of the seabed, (2) either a liquefaction or shear failure, or both, occur in the seabed, even in the saturated seabed, () the Mohr-Coulomb's failure criterion, when combined with elastic stresses, can not be employed to estimate the liquefaction failure in the seabed, () the liquefaction can be evaluated by a criterion in terms of the excess pore pressure, (5) The liquefied zone in the seabed is significantly different from the shear failure zone. The shape beneath the seabed surface for the former is almost identical to the contour where the upward seepage flow is concentrated.

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Realization of a - TV system using the present day HDTV is proposed. This system is based on the stereoscopic principles transmitting the left and right eye view images of the object on multiplexed video lines. In the receiver, the video lines are demultiplexed, the missing lines are interpolated and the stereo pair of images are reconstructed in two picture tubes. By means of a bicircularily polarized viewing system, these stereo pair of images are made to offer a true - vision. This system takes the advantage of high resolution offered by teh HDTV system and at the same time adds only a minimal complexity to the circuitry of the HDTV transmitter and the receiver for converting the HDTV into - TV.

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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%; 79,5±2,9%; ,5±2,9%; 81,6±2,9%; 80,6±,%; for Generic1 - 0; 49,±9,9%; , ±2,%; 90,±,%; , 2±2,2%; 87,±2,0%; 85,9±1,1%; for Generic2 - 0; 30,6±6,%; 66,±,2%; 76,±,%; ,±5,%; 86,0±,%; 84,6±,%: for Generic - 80,±,6%; ,5±1,9%; , ±,2%; ,±2,%; 81,9±2,1%; ,1±2,0%; ,0±2,%; for Generic - ,5±1,%; 84,±0,%; 84,2±1,2%; , 9±0,9%; ,9±0,9%; ,9±0,9%; ,±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 - ,±0,6%; 40, 5±,0%; 62,±2,0%; 80,0±,1%; 85,±2,9%; ,±,%; 80,9±,5%; for Generic1 - 0; 67,0±,%; 89,±2,%; 91, 9±,%; 89,1±1,6%; ,±1,%; 87,±1,2%; for Generic2 - 0; 42,2±5,6%; 75,1±,%; 81,0±6,0%; ,±,2%; , 6±1,%; 87,9±1,0%; for Generic - 85,5±0,5%; 85,6±0,5%; 84,±0,9%; ,±,0%; 84,±0,%; 84,±0,%; 84,±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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Two new polyacetylene compounds (, 6, 12)-1-acetoxy--isovaleryloxytetradeca-, 6, 12-trien-, 10-diyn-14-ol (), and (, 6, 12)-1-acetoxy--(2-methylbutyryloxy)tetradeca-, 6, 12-trien-, 10-diyn-14-ol (C) have been isolated along with (, 6, 12)-1-acetoxy--senecioyloxytetradeca-, 6, 12-trien-, 10-diyn-14-ol (A) from Atractylodes Rhizome (Karabyakujutu). The structures of these compounds were determined on the basis of their spectral data.

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  The distribution of sarcophytol-A in the Sarcophyton genus was investigated in seven samples belonging to S. glaucum ( samples), S. infundibulifurme (2 samples), S. crassocaule (1 sample) and S. trocheliophorum (1 sample) that were collected on Ishigaki Island in Okinawa Prefecture. Sarcophytol-A was present in one sample each of S. glaucum and S. infundibulifurme. This study indicates that the composition of cembranoids in the Sarcophyton genus is not related with the respective species, but with the individual samples collected.

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