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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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,±4,0%; 79,±2,%; ,±2,%; 81,±2,%; 80,±4,4%; for Generic1 - 0; 49,±,%; , ±2,%; ,4±,7%; , 2±2,2%; 87,±2,0%; 85,±1,1%; for Generic2 - 0; 30,±,%; 66,7±,2%; 76,4±7,4%; ,±,%; 86,0±,7%; 84,±,%: for Generic - 80,±,%; ,±1,%; , ±,2%; ,±2,7%; 81,±2,1%; ,1±2,0%; ,0±2,4%; for Generic4 - ,±1,7%; 84,4±0,%; 84,2±1,2%; , ±0,%; ,±0,%; ,±0,%; ,±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, ±,0%; 62,±2,0%; 80,0±,1%; 85,4±2,%; ,±,4%; 80,±,%; for Generic1 - 0; 67,0±7,%; 89,7±2,%; 91, ±4,%; 89,1±1,%; ,±1,4%; 87,±1,2%; for Generic2 - 0; 42,2±,%; 75,1±7,%; 81,0±,0%; ,4±,2%; , ±1,%; 87,±1,0%; for Generic4 - 85,±0,%; 85,±0,%; 84,7±0,%; ,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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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- 35, 18:2 n- , 18: n- 167, 18:4 n- , 20: 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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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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1. The chromosome numbers of 64 species have been studied on which 56 are investigated for the first time.
2. Morphological, anatomical and cytological findings on the Musaceae in the broad sense are considered from a phylogenetical standpoint and three distinct groups:
a) Musa-Ensete, ) Ravenala-Strelitzia-Phenakospermum and ) Holiconia are recognised as suggested by some authors. For these groups sub-familial status is proposed.
. Lowiaceae have been studied for the first time cytologically and their chromosome morphology, distinct from that of any other group of Zingiberales, confirms their claim to familial status.
4. Consideration of the conflicting theories proposed to account for the higher chromosome number in genera like Globba, Alpinia, and Phaemeria, etc. leads to rejection of Chakravorti's hypothesis of wholesale fragmentation of chromosomes and the acceptance of the opposed view of Raghavan and Venkatasubban and others.
. Holttum's transference of the genus Zingiber to the tribe Hedychieae has been given cytological support on the following points:
a) the basic number in the genus Zingiber correlates with that of Kaempferia.
) the new tribe Alpinieae (which is infact Zingibereae without Zingiber) have consistently 48 chromosomes in their somatic complements.
. It is suggested that the African representatives of Kaempferia should be given the status of genus; Cienkowskya on the following points:
a) the difference in floral morphology
) geographical separateness and
) the difference in the number and morphology of the chromosomes. By comparing the present and past findings, various lines of evolution of the chromosome complements within each group are discussed.
7. The basic number 11 is considered to be probably the original one for the Zingiberales as a whole, being present in Ravenala which is the most primitive member in the order. From this secondary basic numbers have arisen through evolution.

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Nアルキル,4:,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[4a～]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,4-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,4:,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-,4:,10-ペリレンビス(ジカルボキシミド)(〔a～〕,〔a～〕,〔7a～〕,〔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-,4:,10-ペリレンビス(ジカルボキシミド)(たとえば〔〕や〔〕)がとくにすぐれた耐光性を示した.

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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=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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Nine isoquinoline alkaloids belonging to the protoberberine, proaporphine and bisbenzyl-isoquinoline series were isolated from Caryomene olivascens (Menispermaceae). Four compounds are new : (-)-2-norlimacine (4), (-)-caryolivine (), (+)-1, 2-dehydro-2-norlimacusine () and N-formylstepharine (). The last one is the first N-formyl derivative to be reported in the proaporphine group. Its biogenetic origin is discussed. Structures were established on the basis of 360 MHz (FT) nuclear magnetic resonance measurements and also by chemical correlation in the case of .

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Clinical results of rotator cuff repairs using the same therapeutic exercises from an early stage after surgery were investigated and compared with the preoperative X-ray findings. 70 shoulders with rotator cuff tears treated operatively and followed by active-assistive exercises in a supine position from 1 week and active exercises standing from weeks after surgery were evaluated. The average age was 63 years old and follow-up periods were 11. months. The operative procedures were McLaughlin's method in 41 shoulders, side to side sutures in , acromioplasty in 17 and a tendon transfer in . The preoperative X-ray findings were classified into groups: group A, superiorly migrated humeral head and narrowed joint space in 4 shoulders; group , only superior migration in 7; group , only narrowed joint space in ; group D, no changes in 36; group , subacromial spurs more than mm without superior migration in 20. The postoperative results were assessed according to the JOA score and the failure rate of each group was investigated. No significant differences in the preoperative JOA score were found in the groups. The postoperative JOA scores were 62.±. in group A, 75.1±12. in , 78.0±12.2 in , .4±7. in D, and .±11.1 in . Especially groups D and treated by McLaughlin's methods showed a significant higher score at follow-up. Rotator cuff repairs with the same therapeutic exercises from an early stage after surgery for groups A, and showed poor results. Groups A and with a superior migration of the humeral head showed a high failure rate of 40 % compared with 4.7% in group , D and with no superior migration. For these cases more careful postoperative exercises were recommended.

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The correction factor (η_ie) for the ultimate bearing capacity of a footing placed adjacent to a slope, taking into account the combined effect of horizontal and vertical seismic loads, represented by horizontal and vertical seismic coefficients, k_h and k_v, respectively, was derived using a modified Janbu's slice method. The influence of slope angles ‘α’ on the values of ‘η_ie’ are studied here. It was found that the values of η_ie can be expressed as an exponential function of ‘k_h/(1-k_v)’ and ‘α’, with a measurable interdependency between ‘α’ and ‘η_ie’. The influence of ‘α’ on the value of ‘η_ie’ increases as the input value of ‘k_h/(1-k_v)’ increases. Equations derived based on the analytical results are proposed to account for this effect. Based on the analyses of 11 near-fault seismographers obtained in the 1999 Chi-Chi earthquake in Taiwan, a ratio between the vertical and the horizontal seismic coefficients, λ, of between ±0.25 is suggested for including the combined effect of vertical and horizontal seismic forces in evaluating the seismic bearing capacity of footings located in near-fault areas.

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At present, analytical or empirical formula for seismic bearing capacity of footings adjacent to slopes is not available. This study uses a pseudo-static-based approach in conjunction with rigorous Janbu's slice method to derive analytical values of seismic bearing capacity factors (N_γ) and correction factors for the effects of inertia of soil mass and load inclinations for a rigid footing adjacent to cohesionless slopes. It is shown that both the bearing capacity factors (N_γ) and the correction factors for the seismic bearing capacity of footings placed on level ground derived herein are comparable with those reported in the literature. Empirical equations regarding the effects of slope angles and load inclinations, expressed using generalized forms of those proposed in the literature, are also derived. It is also found that the empirical equations derived in the present study provide values of correction factors in good agreements with the analytical ones, indicating the validity of using these empirical equations for assessing the bearing capacity of rigid footings situated on the slope subjected to pseudo-static seismic loading.

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