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

t₁

/2

3

.05時間と

t₁

/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

t₁

/2α 4.46時間と

t₁

/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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It has been shown after mathematical and mechanical investigation that Limit Equilibrium Method (LEM) can be considered as a method to obtain the necessary condition of Slip Line Method (SLM), and that the solution can be obtained under the condition that F_s= and ∂F_s/∂θ=O, where F_s is the safety factor and θ is the inclination of the plane on which the safety factor is defined. Next, the generalized LEM (GLEM) is proposed, dealing with the following points : () Triangular or quadrangular blocks can be treated; (2) Safety factors are defined also on interblock planes; and () All types of plastic problems, slope stability, bearing capacity, and earth pressure are identically formulated. Two situations regarding treatment of the moment equilibrium condition are discussed. GLEM is applied to well-known problems. The results agree well with those obtained by theoretical methods. GLEM can be used to obtain the distribution of earth pressure or bearing capacity. GLEM, Iike ordinary LEM, is very effective for the practical problems, but GLEM is more theoretical and it can result in more accurate solutions.

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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-. Sixteen phosphate buffered saline (PBS), boiled PBS, 14 ethanol and 12 methanol extracts induced alkaline phosphatase (ALP) activities, an indicator of MCT- 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-,,6β-triol (). induced ALP activities of MCT- 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- cells by , ergosterol (2), ergocalciferol (), cholesta-,,6β-triol (4), -dehydrocholesterol () and cholecalciferol (6) were tested. The enzyme activities of MCT- cells were increased .-fold by 10 μM and 2.4-fold by 10 μM 4. However, 2, , and 6 did not induce MCT- cell ALP activity at .—10 μM. These results suggested that the OH groups at C- and/or C-6 of and 4 played an important role in their differentiation-inducing activities on MCT- cells. Furthermore, suppressed induction of MCT- cell apoptosis by serum starvation.

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The Tsukuba Challenge is a competition, in which autonomous mobile robots run on a route set on a public road under a real environment. Their task includes not only simple running but also finding multiple specific persons at the same time. This study proposes a method that would realize person searching. While many person-searching algorithms use a laser sensor and a camera in combination, our method only uses an omnidirectional camera. The search target is detected using a convolutional neural network (CNN) that performs a classification of the search target. Training a CNN requires a great amount of data for which pseudo images created by composition are used. Our method is implemented in an autonomous mobile robot, and its performance has been verified in the Tsukuba Challenge 2017.

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The performance of single pitch and multi pitch screw anchors during the application of installation torque is presented. An experimental testing program was conducted using five models of screw anchors with different geometry. The effect of the shape of the screw element, sand properties, and installation depth on the required installation torque value was examined. A theoretical model was developed from which the required installation torque value can be calculated in terms of the influencing factors. The required installation torque can be determined in terms of the ultimate uplift resistance calculated from any of the available theories. Based on the actual installation torque value measured in the field, the anticipated pullout capacity can be back calculated from the present theory. A comparison between theoretical and experimental results showed good agreement. Also, good agreement was observed when the present theoretical results were compared with the available field results reported in the literature.

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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: n-9 35, 18:2 n-6 , 18: n- 167, 18:4 n- , 20: 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 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 ability of Climacodon septentrionalis to immobilize and kill a mycophagous nematode (Aphelenchoides sp.) in vitro is described for the first time. Two isolates produced droplets (20–45 μm in diameter) that formed at the apices of tall, stalked, and branching secretory cells (700–

,500 μm tall). On 2% modified malt extract agar, nematodes became enveloped in the droplets, which restricted their ability to move and resulted in complete immobilization and death within several hours of contact. The rate of decomposition of the nematodes varied considerably, with most individuals persisting for weeks whereas others were degraded within several days and appeared to be colonized by dense hyphal growth. This study provides the first documentation of a non-agaricoid fungus producing secretory cells that are able to immobilize nematodes.

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Plate anchors are the popular type of anchors used in civil engineering construction both on land and offshore. In this paper, the uplift capacity of plate anchor in a sloped clayey ground has been brought out with the help of an experimental programme, carried out on a 50mm diameter model plate anchor. The tests have been conducted at slopes of O°, 15°, 30°and 45°. From the test results, it is found that in the case of shallow anchor, as the slope is increasing from O°to 45°, there seems to be a reduction in uplift capacity. Simple expressions are suggested to arrive at the uplift capacities in sloped ground. The mechanisms involved in the reduction of capacity with slope are explained based on the observed behaviour.

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Laboratory model test results for the holding capacity of inclined shallow square plate anchors in clay (φ= concept) have been presented. The inclination of the anchor with respect to the horizontal was varied from zero to 90°. Based on the model study, an empirical relationship for estimating the ultimate holding capacity of the anchors has been presented.

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The numerical values of the intervals betrween optieal levels are competed for the configurations *⁹4s, s, 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 fors, 2s, 2p, s, p and d. Those of 4s, s, .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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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-C 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 ±.Vp-p input signal at each input terminal in the pseudodifferential configuration. The LPF including an output buffer dissipated 60mW in the case of a .2V supply. Wide spurious-free dynamic range (SFDR) characteristics were confirmed up to high frequencies.

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The applicability of a method for predicting 'bearing capacity increase'in reinforced sandy ground was examined using tests performed under various test conditions. It was found that the present method predicted, with reasonable accuracy, the bearing capacity increase in sandy ground, reinforced with stiff reinforcement. This method may not be applicable for sandy ground reinforced with extensible reinforcement due to the unsuccessful formation of a semirigid zone under the footing. An investigation into the settlement of a footing on reinforced sandy ground, at ultimate footing load condition, suggested that the settlement of footing for reaching peak footing load may be correlated to the 'deep-footing'and the 'wide-slab'mechanisms. That is, the ultimate settlement ratio between reinforced and unreinforced model sandy ground, SR_f, may be linearly correlated to 'BCR_D'and 'BCR_s', which represent 'deep-footing' and 'wide-slab'effects, respectively, on the ultimate bearing capacity increase in reinforced sandy ground.

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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 (G

;2;;4) was performed. At first, we moved drugs from solution with pH .2 (.2±.05) to pH . (.±.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 4 minutes, i.. the active substance should not be released within 4 minutes at pH . The exposure at the second stage was conducted with pH 4 (4.±.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 4, 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 4,±,%; 41,4±,%; 62,±4,%; 79,±2,9%; ,±2,9%; 81,6±2,9%; 80,6±4,4%; for Generic - ; 49,±9,9%; 88, ±2,%; 90,4±,%; 88, 2±2,2%; 87,±2,%; 85,9±,%; for Generic2 - ; 30,6±6,%; 66,±,2%; 76,4±,4%; ,±,%; 86,±,%; 84,6±,%: for Generic - 80,±,6%; ,±,9%; , ±,2%; ,±2,%; 81,9±2,%; ,±2,%; ,±2,4%; for Generic4 - ,±,%; 84,4±,%; 84,2±,2%; , 9±,9%; ,9±,9%; ,9±,9%; ,±,%, respectively.

An analysis of the omeprazole concentration in pH

solution at the second stage revealed the following parameters after the same time: for OO - 4,4±,6%; 40, ±,%; 62,±2,%; 80,±,%; 85,4±2,9%; ,±,4%; 80,9±,%; for Generic - ; 67,±,%; ,±2,%; , 9±4,%; ,±,6%; 88,±,4%; 87,±,2%; for Generic2 - ; 42,2±,6%; 75,±,%; 81,±6,%; 88,4±,2%; 88, 6±,%; 87,9±,%; for Generic4 - 85,±,%; 85,6±,%; 84,±,9%; ,±,%; 84,4±,%; 84,4±,%; 84,±,4%, respectively. Generic release and degradation were completely realized at pH 4.

Conclusion

Decreased gastric stability of Generic

and Generic4 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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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.nm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•±•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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