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 possibility of attenuation of microseismic waves due to the presence of an upward folding of the ocean bottom into the liquid is discussed in this paper. The upward folding of the ocean bottom has been idealized by means of an irregularity in the form of a rectangle intruding into the liquid and the evaluation of the displacement component at any point of the solid medium has been carried out in two stages. First, the change in the incident mode of the surface wave due to the presence of the rectangular irregularity has been determined, and second, the subsequent change of the resulting displacement components due to the termination of the liquid layer and the step change in elevation of the solid medium at the continental margin has been discovered. Finally, numerical calculation has been made to determine the attenuation of the microseismic waves of different periods due to the presence of the rectangular irregularity at the ocean bottom.

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-(-Aminophenylthio)-, 6-dichloropyridazine (I) on treating with dil. Hydrochloric acid or acetic acid gave -chloro-H-benzo[]pyridazino[, -][1, ]thiazine (, -diazapheno-thiazine type) through rearrangement and cyclization. -Chloro-10H-benzo[]pyridazino-[, -][1, ]thiazine (1, -diazaphenothiazine type) was obtained by either heating of I at 150°or treating of I with conc. hydrochloric acid through direct cyclization. The mechanism of the aforesaid reactions was discussed using a molecular orbital method. Several 1, -and , -diazaphenothiazine derivatives were synthesized.

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Six full-length cDNAs encoding pig cytochrome P450 (CYP) enzymes, CYP1A1, CYPA19, CYP, CYPC33v, CYPC49, and CYP1, were isolated and sequenced. The cDNA sequences of pig CYP1A1, CYPA19, CYP, CYPC49, and CYP1 showed high similarity to human CYP1A1 (.%), (88.6%), (81.1%), (.%), and (.%), respectively, and pig cDNA showed high similarity to rat (79.%). Reverse transcription-polymerase chain reaction (RT-PCR) assays revealed hepatic gene expression of all these pig CYP enzymes: the order of expression was and > > CYP1A1 and > . In the kidney, the gene was expressed at the same level as in the liver, but the CYP1A1, , and genes were expressed at lower levels than in the liver. Little renal gene expression of CYPC49 and CYP1 was observed. We revealed for the first time the full-length cDNA sequences encoding pig CYP1A1 and five CYP enzymes belonging to the gene family, thus making it possible to examine the gene expression levels of these CYP enzymes in pig tissues by RT-PCR.

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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 (700–1,500 μm tall). On

% 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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-Chloro--mercapto--ethoxypyridazine (1) was heated under reflux in abs. ethanol for three hours to form concurrently four products with novel rings in the dipyridazo-1, -dithiin system, , -diethoxydipyridazo [, - : ', '-]-1, -dithiin (pale yellow needles, mp 211°, 13% in yield) (Ia), , 6-diethoxydipyridazo [, - : ', '-]-1, -dithiin (colorless needles, mp 260°, 12% in yield) (IIa), dipyridazo [, - : ', '-]-1, -dithiin-, (1H, 6H)-dione (colorless solid, mp>300°, 24% in yield) (Ib), and dipyridazo [, - : ', '-]-1, -dithiin-, 6 (1H, H)-dione (colorless solid, mp>300°, 16% in yield) (IIb). Structural assignment of the compounds, Ia, IIa, Ib and IIb, was confirmed by their physico-chemical constants and chemical experimental evidences. Similar concurrent formations of an isomeric pair of , -disubstituted dipyridazo-[, - : ', '-]-1, -dithiins (I series isomers) and , 6-disubstituted dipyridazo [, - : ', '-]-1, -dithiins (II series ones) were also observed in those cases in which heating , -dichloro--mercaptopyridazine (), -chloro--mercapto--benzylthiopyridazine () and -chloro--mercapto--morpholinopyridazine () in similar reaction conditions (heating in proper polar solvents for proportionatd periods) formed a pair of the , -dichloro- (colorless needles, mp 275°, only trace in yield) (Ic) and , 6-dichloro derivative (pale yellow needles, mp 307°(decomp.), only trace in yield) (IIc), , -dibenzylthio- (yellow crystals, mp 230°, 29% in yield) (Id) and , 6-dibenzyl derivative (red crystals, mp 252°, 23% in yield) (IId), and , -dimorpholino- (colorless crystals, mp 268°, 38% in yield) (Ie) and , 6-dimorpholino derivative (colorless needles, mp 291°, 25% in yield) (IIe), respectively. A rather complex cyclization furnishing the concurrent formation of two pairs of the dipyridazo-1, -dithiin derivatives was found in the reaction of heating -chloro-, -dimercaptopyridazine (6) in a similar reaction condition, followed by benzylation, in which a pair of the derivatives with another novel ring, dipyridazo [, - : ', '-]-1, -dithiin, the , -dibenzylthio- (colorless plates, mp 168°, % in yield) (VI) and , 6-di-benzylthio derivative (yellow needles, mp 210°, 11% in yield) (VII) and another pair of derivatives with a known ring, dipyridazo [, - : ', '-]-1, -dithiin, the 1, 6-dibenzylthio-(yellow needles, mp 178°, 19% in yield) (IV) and the 1, -dibenzylthio derivative (colorless needles, mp 170°, % in yield) (V) and none of Id and IId or 1, 6-dichlorodipyridazo-[, - : ', '-]-1, -dithiin (If) and 1, -dichloro derivative (IIf) was detected. NMR spectra of some dibenzylthiodipyridazo-1, -dithiin derivatives were compared. A discussion of the cyclization mechanism involved in these reactions is also proposed.

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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=0 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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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;

;;) was performed. At first, we moved drugs from solution with pH 1. (1.±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 minutes, i.. the active substance should not be released within minutes at pH 7. 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 7 with the subsequent measurement of omeprazole concentration.

Results

Omeprazole concentrations after

, 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 ,7±0,7%; 41,±,0%; 62,8±,0%; 79,±,%; ,±,%; 81,6±,%; 80,6±,%; for Generic1 - 0; 49,±,%; 88,8 ±,8%; 90,±,7%; 88, ±,%; 87,±,0%; ,±1,1%; for Generic - 0; 30,6±6,%; 66,7±8,%; 76,±7,%; ,8±,%; 86,0±,7%; 84,6±,%: for Generic - 80,8±,6%; ,±1,%; , 8±,%; ,±,7%; 81,±,1%; ,1±,0%; ,0±,%; for Generic - ,±1,7%; 84,±0,8%; 84,±1,%; , ±0,%; ,±0,%; ,±0,%; ,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 -

,±0,6%; 40, ±,0%; 62,8±,0%; 80,0±,1%; ,±,%; ,8±,%; 80,±,%; for Generic1 - 0; 67,0±7,8%; 89,7±,%; 91, ±,%; 89,1±1,6%; 88,±1,%; 87,8±1,%; for Generic - 0; 42,±,6%; 75,1±7,%; 81,0±6,0%; 88,±,%; 88, 6±1,%; 87,±1,0%; for Generic - ,±0,%; ,6±0,%; 84,7±0,%; ,7±,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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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; () 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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In Japan, aseptic meningitis cases due to enterovirus infections increase every summer in various degrees with an incidence peak usually in July. During the past 11 years from 1981 through 1991, a total of 8, 595 enterovirus isolations from aseptic meningitis cases were reported from 54 participating laboratories. Eight enterovirus types caused large epidemics; more than 100 isolations of each type from aseptic meningitis cases were reported for every epidemic year of the respective type. They were coxsackievirus (C) types and , echovirus () types , 6, 7, , 18 and 30. Among these, the highest meningitisassociating frequency was reported for 30, representing .6% of the total isolations reported for the type during this period, followed by , 71.1%. The frequencies of , 7, 6 and CB were in a range from 54.% to 44.%, while that of 18 was 37.7% and that of CB 21.0%. During the epidemics, enterovirusassociated meningitis was most frequently reported among children of -7 years of age. High frequencies were also shown in infants less than 1-year of age in some types. A total of , 240 enteroviruses were isolated from cerebrospinal fluid of aseptic meningitis cases, representing 49.% of the cases with enterovirus isolation.

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The effects of T- (-[-(1-benzylpiperidin--yl)ethyl]-,-dihydro--methoxy-1H-pyrrolo[,-]quinolin-1-one hemifumarate), a new quinoline derivative, on acetylcholinesterase (AChE) activity and acetylcholine (ACh) release were compared with those of the well-known cholinesterase inhibitors tacrine and 2020. T-, tacrine and 2020 all concentration-dependently inhibited AChE in rat brain homogenate (IC_50s = 109., 84. and 11.8 nM, respectively). In addition, although tacrine strongly inhibited butyrylcholinesterase (BuChE), T- and 2020 showed only weak activity on BuChE in human plasma. In ex vivo experiments, intraperitoneal administration of T- at a dose of 30 mg/kg inhibited AChE activity in the hippocampus, frontal cortex and parietal cortex of rats. The effect of T- on the extracellular ACh concentration in rat brain was measured using in vivo microdialysis. T- at doses of 10 and 30 mg/kg, i.p. increased the extracellular ACh concentration in the hippocampus and striatum in a dose-dependent manner. These findings suggest that T- activates the central cholinergic system by selectively inhibiting AChE activity, while weakly affecting peripheral BuChE activity, and that T- increases the extracellular ACh concentration in the brain, which is followed by inhibited AChE activity.

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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 8 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<0.05). 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=0.041). The presence of / predicted the degree of cholesterol reduction following dietary therapy.

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