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±.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 minutes, i.. the active substance should not be released within minutes at pH . The exposure at the second stage was conducted with pH (.±.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 ,±,%; 41,±,%; 62,±,%; 79,±2,%; ,±2,%; ,6±2,%; 80,6±,%; for Generic1 - ; 49,±,%; , ±2,%; 90,±,%; , 2±2,2%; 87,±2,%; 85,±1,1%; for Generic2 - ; 30,6±6,%; 66,±,2%; 76,±,%; ,±,%; 86,±,%; 84,6±,%: for Generic - 80,±,6%; ,±1,%; , ±,2%; ,±2,%; ,±2,1%; ,1±2,%; ,±2,%; for Generic - ,±1,%; 84,±,%; 84,2±1,2%; , ±,%; ,±,%; ,±,%; ,±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 - ,±,6%; 40, ±,%; 62,±2,%; 80,±,1%; 85,±2,%; ,±,%; 80,±,%; for Generic1 - ; 67,±,%; 89,±2,%; 91, ±,%; 89,1±1,6%; ,±1,%; 87,±1,2%; for Generic2 - ; 42,2±,6%; 75,1±,%; ,±6,%; ,±,2%; , 6±1,%; 87,±1,%; for Generic - 85,±,%; 85,6±,%; 84,±,%; ,±,%; 84,±,%; 84,±,%; 84,±,%, 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.

抄録全体を表示

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=1 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 : (1) 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.

抄録全体を表示

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.

抄録全体を表示

（はじめに）血清クレアチニン（Ｃｒe）は性・年齢による影響をうけるため正確に 腎機能を反映しないとされる。このため日本腎臓病学会から腎機能の評価に―ＧＦＲを用いることが提唱されている。そこで、今回、本院のドック・健診受診者の腎機能を－ＧＦＲで評価し、その有用性について検討したので報告する。 （対象・方法）対象は平成２１年月～月までの受診者、男２１９名、女３５０名（計５６９名）である。改訂ＭＤＲＤ簡易式により血清Ｃｒｅから－ＧＦＲを算出し、性・年代別に集計し、有用性を評価した。 （結果）男性のＣｒｅ平均値は.±.11、女性は.58±.08（基準値：男.～1.・女.2～.）であった。男性の年代別の－ＧＦＲ平均値は、２０代97.1±15.、３０代94.±10.、４０代.±.1、５０代.1±12.、６０代76.±13.2、７０代↑75.±12.。女性の２０代104.±18.、３０代.±15.6、４０代87.1±13.、５０代.±11.、６０代80.±15.1、７０代↑74.±17.であった。日本腎臓病学会のＣＫＤステージ分類ではステージ_II_（－ＧＦＲ60～89）をＧＦＲ軽度低下としている。－ＧＦＲの結果からするとステージ_II_は、男性１３１名（59.％）、女性１６４名（46.％）。ステージ_III_は男性１６名（.％）、女性１４名（.％）であった。 （まとめ）腎機能の指標として－ＧＦＲは血清クレアチニンよりは鋭敏とみなされるが女性高齢者では体表面積で補正した－ＧＦＲで評価すべきと考えられた。　　

抄録全体を表示

A biosynthetic pathway for (

)-methyl cinnamate formation was evaluated in Tricholoma matsutake by tracer experiments using ¹³C- and ²H-labeled precursors. One hundred percent selective ¹³C incorporation was observed when L-[1,2,,,,6,,,-

13C₉

, ^15/N]phenylalanine was converted to (

E

)-[1,2,

3

,

4

,

5

,6,

7

,

8

,

9

-

13C₉

]cinnamate and (

E

)-[1,2,

3

,

4

,

5

,6,

7

,

8

,

9

-

13C₉

]methyl cinnamate. Similarly, 100% selective ¹³C incorporation was observed when (

E

)-[1,2,

3

,

4

,

5

,6,

7

,

8

,

9

-

13C₉

]cinnamate was converted to (

E

)-[1,2,

3

,

4

,

5

,6,

7

,

8

,

9

-

13C₉

]methyl cinnamate. In contrast, the ²H incorporation selectivities were

82

.1% and

81

.

4

% when L-[2,

3

,

4

,

5

,6,

7

,

7

,

8

-

2H₈

]phenylalanine was converted to (

E

)-[2,

3

,

4

,

5

,6,

7

,

8

-

2H₇

]cinnamate and (

E

)-[2,

3

,

4

,

5

,6,

7

,

8

-

2H₇

]methyl cinnamate, respectively. Thus, T. matsutake synthesizes (

E

)-methyl cinnamate from L-phenylalanine via (

E

)-cinnamate. (

E

)-cinnamate was likely formed through two pathways: one was major and the other was a minor.

抄録全体を表示

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.

抄録全体を表示

The association between apolipoprotein (Apo-) polymorphism and the response of plasma cholesterol to dietary therapy (cholesterol intake of less than 300mg/day) was investigated for about weeks in 208 nonfamilial hypercholesterolemia patients (/ 161, / 47). The baseline lipoprotein concentration and the intake of energy and lipids were not significantly different between subjects with / and those with / phenotypes. After the dietary therapy plasma total cholesterol and low density lipoprotein cholesterol were significantly decreased in both phenotype groups (p<.05). The patients with / had significantly smaller reductions of LDL-C than the patients with /. The changes of LDL-C showed a significant difference between the patients with / and / by the Kruskal Wallis test (p=.041). The presence of / predicted the degree of cholesterol reduction following dietary therapy.

抄録全体を表示

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-,,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-,,6β-triol (), -dehydrocholesterol () and cholecalciferol (6) were tested. The enzyme activities of MCT-1 cells were increased .-fold by 10 μM 1 and 2.-fold by 10 μM . However, 2, , and 6 did not induce MCT-1 cell ALP activity at .1—10 μM. These results suggested that the OH groups at C- 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.

抄録全体を表示

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.

抄録全体を表示

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.

抄録全体を表示

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.

抄録全体を表示

Activity-directed isolation of the ethyl acetate, methylene chloride and n-hexane fractions of Gloiopeltis furcata resulted in the isolation of 18 compounds. Their structures were elucidated as 2-(-hydroxy--oxotetrahydrofuran--yl)acetic acid (1), glutaric acid (2), succinic acid (), nicotinic acid (), ()--hydroxyhex-2-enoic acid (), cholesterol (6), -hydroxycholesterol (), uridine (), glycerol (), -(hydroxymethyl)-2-methoxybenzene-1,-diol (10), (,)--oxodeca-,-dienoic acid (11), (Z)--ethylidene--methylpyrrolidine-2,-dione (12), dehydrovomifoliol (13), loliolide (14), cholesteryl stearate (15), palmitic acid (16), cis-,,11,14,17-eicosapentaenoic acid (17) and α-linolenic acid (18) on the basis of spectroscopic and chemical evidences. Their anticholinesterase and antioxidant activities were evaluated via inhibitory activities on acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) as well as scavenging activities on 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical and peroxynitrite (ONOO⁻). All isolated compounds (1—18) exhibited moderate AChE inhibitory activities with IC₅₀ values ranging from 1.14—12.50 μg/ml, whereas 1, , , 17, and 18 showed mild BChE inhibitory activities with IC₅₀ values ranging from .57—15.89 μg/ml. Although most of the compounds isolated were lacking the scavenging activity on DPPH radical and ONOO⁻, and 10 showed good DPPH radical scavenging activity, and , 10, and 16 showed potent ONOO⁻ scavenging activity.

抄録全体を表示

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～〕,〔6a～〕,〔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〔6〕)がとくにすぐれた耐光性を示した.

抄録全体を表示

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 ±.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.

抄録全体を表示

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。

抄録全体を表示