ラットに

3H

-CU-

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(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.

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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 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- , 18: n- 167, 18:4 n- , 20:5 n- 167, and : 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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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), 8 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-7,-diene-,5α,-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,-triol (4), 7-dehydrocholesterol (5) and cholecalciferol () were tested. The enzyme activities of MCT-1 cells were increased .0-fold by 10 μM 1 and 2.4-fold by 10 μM 4. However, 2, , 5 and 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- of 1 and 4 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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Virus-like particles (VLPs) were collected from geothermal vent water samples in the drift-way at Toyoha Mine, Hokkaido, Japan (−500 m level, 63.5°C) whose VLP and bacterial abundance was (No/ml±SD, n: 500), VLP: 9.60±0.29×10⁸ and bacteria: .61±0.14×10⁶. VLPs ranged in diameter from 30 to 320 nm, and the major size distribution (ca 62%) was .33. nm (n: 843). Ultrafiltration followed by CsCl density equilibrium ultracentrifugation gave purified TY-VLPs: .64×10¹³. Regardless of UV treatment, TY-VLP reduced the efficiency of plating to 68.-.4% at a multiplicity of infection of ca 0. on Escherichia coli 1157. Generalised transduction was observed on

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. coli 1157 with a frequency between 10^-4 and 10^-5 cells/particle using TY-VLPs without UV-treatment. The growth of generated

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. coli transductants (TY--trans) was compared to that of an

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. coli transductant (ST--trans) generated by Aquificales originating VLP (Chiura, 2002). The extent of the maximum growth of both transductants was ca 40% of the parental

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. coli used as a recipient. TY--trans acquired "budding-like" particle productivity, which has been demonstrated for ST--trans. ST--trans produced five different size particles, whose DNA content ranged between 291. and 382.0 kb, and TY--trans produced ten different size particles between 68.5 and 190.2 kb, respectively.

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The numerical values of the intervals betrween optieal levels are competed for the configurations *⁹4s, 5s, s and 7s 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 d. Those of 4s, 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 method for analyzing the uncertainties involving the use of empirical relationships in design is developed. It is applied to evaluate the reliability of the relationship s_u(mobilized)=(measured), whereby the pertinent uncertainties are analyzed using extensive laboratory and field observed data. On the average, the relationship s_u(mobilized)= (measured) is unbiased and the error implicit in the relationship is about 15%. When cone values are used to infer s'_p, additional uncertainties on the mobilized undrained strength will incur resulting mainly from the calibration uncertainty between σ'_p and the cone values. Alternatively, vane tests may be performed to infer the mobilized strength using Bjerrum correction factor. Results show that uncertainty level associated with using the vane tests is smaller than that using the cone values, provided that similar scatter is observed between measured vane and cone values at a given site. However, prediction of the mobilized strength is even more accurate if direct measurements can be made on the preconsolidation pressure. The proposed probabilistic method also assesses the benefit of additional tests besides comparing the accuracy of using various soil parameters for predicting mobilized undrained strength. Such information is essential for planning cost-effective site characterization program.

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This paper presents reinforcing mechanisms and a method for analyzing reinforced earth structures. The reinforcing mechanism presented is divided into two stages, a fixed slip surface and an arbitrarily selected slip surface. The mechanism is studied through direct shear tests and plane strain compression tests including some geotextiles. The reinforcing materials considered in this paper only have tensile strength. The authors have already proposed a method called Generalized Limit Equilibrium Method (GLEM) for analyzing stability problems. The validity of the method has already been shown in previously published papers. In this paper, the method is extended to carry out a stability analysis for reinforced earth structures. Finally, large scale model tests for the bearing capacity of foundations on reinforced slopes were carried out to investigate the validity of the proposed reinforcing mechanism and the analytical method. Through comparisons of observations of experiments and results of the analytical method, the validity of the present work is demonstrated.

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The pseudo-static analysis has been used in engineering practice to simplify the computation of the upper limit of a slope under seismic load. In this paper, the upper bound technique of limit analysis of perfect plasticity is used to determine the bearing capacity of a foundation near a down-hill slope. In this analysis (Chen et al., 1969; Chen, 1975), a logarithmic spiral rapture (Abdul-Baki et al., 1970; Sawada et al., 1984) is assumed to start at an edge of the loaded area far from the slope. A landslide is assumed to be of rigid body type with the inertia force acted at its center of gravity. The collapse state is reached when the rate of kinematic energy of the landslide together with the load is equal to the rate of dissipation of internal energy along the sliding surface. This energy balance leads to the equation of ultimate load with several parameters. The optimized numerical rcsults with respect to these parameters are compared with those by Kotter's method (Yamaguchi, 1959) and those obtained by the slice method.

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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=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.

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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;

;4) was performed. At first, we moved drugs from solution with pH 1.2 (1.2±0.05) to pH 7.0 (7.0±0.05) and measure concentration of omeprazole in solution by high-performance liquid chromatography. According to our self-developed formula, pH 7 exposure time of resistance to PDGR for omeprazole is 4 minutes, i.. the active substance should not be released within 4 minutes at pH 7. The exposure at the second stage was conducted with pH 4 (4.0±0.05), that imitated gastric pH after PPI administration. And then we also moved drugs to pH 7 with the subsequent measurement of omeprazole concentration.

Results

Omeprazole concentrations after 4, 10, 15, 20, 30, 45, 60 minutes in pH 7 solution at the first stage were different for OO and generics. For OO, these values were 4,7±0,7%; 41,4±

,0%; 62,8±4,0%; 79,5±2,9%; ,5±2,9%; 81,±2,9%; 80,±4,4%; for Generic1 - 0; 49,±9,9%; ,8 ±2,8%; 90,4±,7%; , 2±2,2%; 87,±2,0%; 85,9±1,1%; for Generic2 - 0; 30,±,%; 66,7±8,2%; 76,4±7,4%; ,8±5,%; 86,0±,7%; 84,±,%: for Generic - 80,8±,%; ,5±1,9%; , 8±,2%; ,±2,7%; 81,9±2,1%; ,1±2,0%; ,0±2,4%; for Generic4 - ,5±1,7%; 84,4±0,8%; 84,2±1,2%; , 9±0,9%; ,9±0,9%; ,9±0,9%; ,8±1,1%, respectively.

An analysis of the omeprazole concentration in pH 7 solution at the second stage revealed the following parameters after the same time: for OO - 4,4±0,

%; 40, 5±,0%; 62,8±2,0%; 80,0±,1%; 85,4±2,9%; ,8±,4%; 80,9±,5%; for Generic1 - 0; 67,0±7,8%; 89,7±2,%; 91, 9±4,%; 89,1±1,%; ,±1,4%; 87,8±1,2%; for Generic2 - 0; 42,2±5,%; 75,1±7,%; 81,0±,0%; ,4±,2%; , ±1,%; 87,9±1,0%; for Generic4 - 85,5±0,5%; 85,±0,5%; 84,7±0,9%; ,7±,0%; 84,4±0,%; 84,4±0,%; 84,±0,4%, 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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This paper focuses on an extension of the log-spiral analysis of bearing capacity that has been presented in the authors' previous work for strip foundations placed on the level ground, to those on the top of slopes. Comparisons are made with other analytical and experimental results to examine applicability of the method to practical problems. It is revealed that the log-spiral analysis somewhat overestimates bearing capacity values as compared to other solutions, the errors involved being around 20 percent at maximum and varying sensitively to the angle of internal friction and slope inclination. Also noticed is a relatively good correspondence with experimental results, especially with model tests on clay (φ=0), on both the ultimate bearing capacity and the shape of sliding surfaces.

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A total of 176

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

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. coli isolates was to tetracycline (.%), followed by streptomycin (80.7%) and ampicillin (64.8%). Resistance to cefazolin, cefoperazone, cefepime and amikacin was very low. Of the 176

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. coli strains, forty (.7%) 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

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. 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

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

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. 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

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. coli within a farm or between farms is plausible.

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The bearing capacity and compressibility of a calcareous sand were examined by drained triaxial compression tests and laboratory model tests on strip footings 51mm by 305mm. The tests were carried out on two sands-a calcareous sand having a carbonate content of 18% and a clean sand obtained by washing the calcareous sand with Hydrochloric Acid (HCI) and water. All tests were performed at a relative density of 66%. The results indicate increased compressibility and no change in the peak strength parameters due to the presence of carbonates. The bearing capacity of the calcareous sand was smaller than that of the clean silica sand. Various methods of analysis were discussed to account for the effect of compressibility on bearing capacity.

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