The bioavailability (

) of 3810, an unstable compound in acid, was studeid by controlling gastric pH in beagle dogs. The BAs, after the administration of 3810 solution orally to dogs with a low or a high gastric pH, were 3.16 ± 1.28% and 76. ± 13.%, respectively. These results suggested that 3810 decomposes rapidly in the presence of gastric acid, but its is high if the decomposition of 3810 is avoided in the gastrointestinal tract. To establish a dosage form of 3810 for toxicity testing in the dog, 3810 enteric-coated tablets (ϕ=. mm) and 3810 solution were administered. The t_max after the administration of 3810 enteric-coated tablets was prolonged (t_max=.42 hr), suggesting a slow gastric emptying, or a delay in the release of 3810. In contrast, when the tablets were asministered orally to fasted beagle dogs, t_max was obtained within 1 hr, suggesting rapid release once the tablet left the stomach. After administration of 3810 solution to beagle dogs with a high gastric pH, the was high, with the lowest variability. In the preliminary toxicity test, 3810 solution was administered to dogs with a high gastric pH once a day for seven days. The plasma concentrations of 3810 on day 1 and day increased dose-dependently, and there is no difference in pharmacokinetics between day 1 and day . These results indicate that the method to control gastric pH in dogs is useful for the dosing of a compound that is unstable in gastric acid.

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A high performance liquid chromatographic method for the simultaneous determination of the cyanogenic glycosides, i. ., amygdalin (AM) and prunasin (PR), and their degradation products, i. ., benzaldehyde (BAL) and benzoic acid (), in processed foods containing ume (Japanese apricot Prunus mume Sieb et Zucc.) was developed.
The sample was extracted with 0.05M citric acid solution and cleaned up by use of a Seppak C₁₈ cartridge. The extract was chromatographed on a Capcell Pak C₁₈ SG120 column with acetonitrile-water-0.2M phosphate buffer, pH .0 (16: 79: ). Detection was achieved with a UV monitor set at 210nm. The peaks corresponding to AM and PR were confirmed by examination of the effect of emulsin treatment.
The recoveries from ume extract, umeboshi (dried and salted ume), umeshu (Japanese apricot wine) and ume jam fortified with AM, PR, BAL and at levels of 40-100μg/g each were 86.-100.% (C. V. 3.-.%) for AM, 69.-105.3% (0.-.2%) for PR, 71.-85.0% (1.-2.%) for BAL and 82.-99.1% (0.-.%) for , except for AM in the ume extract and the umeboshi. AM in ume extract and umeboshi could not be determined owing to interference by contaminants.
The determination limits were 10μg/g for AM, 2μg/g for PR, and 1μg/g for BAL and , respectively.

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Isotopic analyses of Sr and

and quantitative analyses of Rb, Sr, Cs, , and rare earth elements from chemical separates of four chondrites, i.., Cold Bokkeveld (CM2.2), Murray (CM2./2.), Nogoya (CM2.2), and NWA 4428 (H), were performed to investigate the origin of Sr and isotopic variations. Most isotopic deviations of the chemical separates showed positive isotopic anomalies of

135Ba

that correlated with

137Ba

and

138Ba

, suggesting a heterogeneous distribution of s-process isotopes in the early solar system. The Sr and

Ba

isotopic data for the acid residues showed significant isotopic deficits of

84Sr

,

130Ba

,

132Ba

,

135Ba

,

137Ba

, and

138Ba

derived from the enrichments of s-process isotopes caused by the presence of presolar SiC grains. Furthermore, the correlation between the isotopic data for

135Ba

,

137Ba

, and

138Ba

with the isotopic data for the acid residues suggested the contribution of n-process nucleosynthetic components. Assuming that the

Ba

isotopic compositions of the acid residues were a mixture of s- and n-process nucleosynthetic components and radiogenic components of

135Ba

, the upper limits of the initial ¹³⁵Cs isotopic abundance expressed as the ¹³⁵Cs/¹³³Cs ratio in the early solar system could be estimated as (2.

4

± 0.

4

) × 10–

4

for Cold Bokkeveld, (1.

6

± 0.

9

) × 10–

4

for Murray, and (

4

.

6

± 0.

7

) × 10–

4

for Nogoya, respectively.

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This paper presents a review for the crystallization of nonlinear optical crystals such as , , fresnoite-type and several langasite-type crystals in glasses and for the second order optical nonlinearities of those crystals. In this study, transparent surface crystallized glasses consisting of , and crystals were successfully fabricated from the corresponding glasses. Second order nonlinear optical coefficients, d₃₃, were evaluated by Maker fringe technique for those surface crystallized glasses. As a result, it was demonstrated that the and the crystals indicated large d₃₃ values, i.., – 1.3 pm/V and – pm/V, respectively. In particular, d₃₃ of the crystal is comparable to that of LiNbO₃ single crystal. Moreover, we confirmed for the first time that the langasite-type crystals, which are promising materials for SAW device, are formed by crystallization in the corresponding glasses.

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教室で経験した成人の先天性気管支疾患例の診断と治療法を検討した。内訳は, 食道気管支(-)瘻例, 気管支胆道(-)瘻1例, 気管支閉鎖症()2例である。-瘻の例は女性で, 年齢は40, 41, 68, 72歳, 他の1例は58歳の男性である。-瘻は38歳の男性である。-瘻, -瘻の全員が2∿30年間の繰り返す呼吸器感染症状を有していた。の2例は, 25, 38歳の男性である。1例は幼少児期から繰り返す肺炎の既往を持つが, 1例は検診(無症状)で発見された。診断には詳細な病歴聴取が重要であり, 確定診断には-瘻では食道造影と食道ファイバースコピー, -瘻, では気管支造影, 気管支ファイバースコピーが有用であった。治療は-瘻では3例に瘻孔切除術を, 2例に瘻孔切除術に加え肺区域あるいは部分切除術を施行した。-瘻に対しては瘻孔切除術を施行した。の1例には, 肺葉切除術を, 他の1例には肺区域切除術を施行した。成人の先天性気管支疾患の治療にあたっては, 良性疾患であることから縮小手術を施行しており, 肺機能を温存した良好な結果を得ることができた。

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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 -3dB frequency bandwidth, group delay ripple, 3rd-order distortion, and 3rd-order input intercept point (IIP3) were 200MHz, 2.2%, ≤ -55dB with a 100MHz input, and +10.3dBm, respectively, all with a ±0.1Vp-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.

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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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3810を雌雄ラットおよび雄性犬に単回投与したときの薬物動態について検討し，以下の成績を得た．
1．雄ラットに3810(，20， mg/kg)を単回十二指腸内投与すると，3810は速やかに吸収され，投与後分で最高値に達し，以後血漿中3810は消失半減期～分で速やかに消失した．投与量とAUCの関係は投与量が増加するに従い投与量比率以上にAUCが増加した．20mg/kgの十二指腸内投与時の雄性ラットにおけるバイオアベイラビリティ()は36。%であり，他方雌性では90．%であった．
2．絶食下雌雄ラットに3810(2，，20mg/kg)を単回経口投与したときのは，雌雄ともに.1%～21.1%であり，十二指腸内投与の場合よりもが減少した．これは胃酸による影響でが減少したものと推察された．
3．薬物投与前後に1%炭酸水素ナトリウム水溶液を胃内注入し胃内容pHを高くコントロールしたイヌ(1%炭酸水素ナトリウム水溶液処理群)に，3810(0.，1.，mg/kg)を単回経口投与すると3810は速やかに吸収され，血漿中濃度は投与後～12分で最高値に達し，以後24分の消失半減期で減少した．1.mg/kgの投与量におけるは，81.%であった．
．胃酸分泌刺激剤ペンタガストリンを筋肉内投与し，胃酸分泌を充進させたときのイヌ(ペンタガストリン処理群)における3810の経口投与時の血漿中3810のAUCは，1%炭酸水素ナトリウム溶液処理群のそれより16%の値を示したのみであった．これは胃酸による影響を受けたものと推察された．

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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 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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Streptomyces graminofaciens 14348, isolated from a soil sample, was found to produce new specific inhibitors of estrogen binding to its receptor. Five related substances, BE-14348A-, were isolated, and their structures were determined by analyses of spectral properties. Of these substances, A was identical with the known flavanone, naringenin. On the other hand, , C, D and were all new compounds; the structure of was determined to be 2(S):3(S)-3-methyl-', , -trihydroxyflavanone, C was a racemic mixture of 2(S):3(R) and 2(R):3(S)-3-methyl-', , -trihydroxyflavanone; D and were -chloro derivatives of and C, respectively.

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Hydroxyapatite ceremic has an excellent biocompatibility. However, there is required some improvement in respect to the mechanical characteristics of hydroxyapatite ceramic. In order to improve the mechanical characteristics of hydroxyapatite ceramic, this study is on the method of forming a composite structure of hydroxyapatite ceramic adhered to the metals by glass.
Experimental proceaures were as follows:
a) Bonding strength of the metals with types of glasses adhered to them.
) Bonding strength of the metals by the addition to the glass of % (wt%) of Sn or .
c) Bonding strength of hydroxyapatite ceramics by the addition to the glass of % (wt%) of Sn or .
d) Bonding strength of hydroxyapatite ceramic and metals by the addition to the glass of wt% . % (wt%)
) Study of adherence mechanism by S. . M. and . P. M. A.
The results obtained showed that the bonding strength between the glass, which was produced in this study, and the Ti, Co-Cr-Ti alloy was good.
Especially, the bonding strength between the Co-Cr-Ti alloy and the hydroxy-apatite by the addition to the glass of % (wt%) of was shown to be from 308. kg/cm² to 420 kg/cm² in the pull out test.

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Two new partially saturated tricyclic ring systems, , a, , , , 10, 10a, 11-octahydro-11-oxodibenz [, ] oxepins (3a and 3), and -thiepins (a and ) were synthesized. Compounds a and were desulfurized to give a pair of isomeric 2-methylbenzoylcyclohexanes (10a and 10). Deuterated a and (11a and 11) were prepared starting from butadiene- (12). The stereochemical features of 3a (trans), 3 (cis), a (trans) and (cis) are compared with those of 10a, 10, 11a and 11 on the basis of proton nuclear magnetic resonance data.

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Many attentions have long been paid to the question about the reason why benz [a]-anthracene (), a very weak carcinogen, increases its carcinogenic activity to the level of the most potent carcinogenic hydrocarbons, such as benzo [a] pyrene (BP) and 3-methylcholanthrene (3-MC), by the substitution of methyl group(s) for the "L-region" (-and 12-positions) hydrogens, .g. , 12-dimethyl- (DMBA) has a higher carcinogenic activity than BP, and -methyl- (-MBA) is as carcinogenic as 3-MC (Cavalieri, 1979; Selkirk, 1980). In addition, 3-MC is also an alkyl-substituted . The marked increase in carcinogenicity of aromatic hydrocarbons by a methyl substituent is observed not only with but also with other aromatic hydrocarbons, such as chrysene and anthrabene (Cavalieri, 1979; Selkirk, 1980). -Methylchrysene, for instance, has as highly carcinogenic activity as 3-MC whereas carcinogenicity of chrysese is very weak. Similarly, , 10-dimethylanthracene is carcinogenic whereas the mother compound; anthracene, is not carcinogenic (Fig. 1). Several attempts have been made to know active metabolites of DMBA in relation to epoxide formation. DMBA , -oxide has been isolated and identified as an active metabolite from a hepatic mitrosomal reaction mixture (Keysell et al., 1973). DMBA 3, -diol-1, 2-epokide was also strongly assumed to be an active metabolite, but has not been detected yet from the in vitro system (Jerina et al., 1978 ; Malaveille et al., 1978 ; Wislocki bt al:, 1980). These studies, however, were carried out by using liver microsomes from rats pretreated with the P-448 inducer, 3-MC or polychlorinated biphenyls. , - and 10, 11-epoxides of DMBA might also be candidates for the active metabolites since their hydrolysis products, , - and 10, 11-dihydrodiols, have been isolated from a rat liver microsomal system (DiGiovanni and Juchau, 1980).

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A methanol extract of the flowers of Mammea siamensis (Calophyllaceae) was found to inhibit enzymatic activity against aromatase (IC₅₀=16. µg/mL). From the extract, two new geranylated coumarins, mammeasins C (1) and D (2), were isolated together with seven coumarins: -hydroxy--methyl--(3,-dimethyl-octa-2,-dienyl)--(2-methyl-1-oxobutyl)-,-dihydropyrano[,3,2-de]chromen-2-one (), -hydroxy--methyl--(3,-dimethyl-octa-2,-dienyl)--(3-methyl-1-oxobutyl)-,-dihydropyrano[,3,2-de]chromen-2-one (10), mammeas A/AA (14), A/AB (15), A/AA cyclo D (18), / (23), and /BC cyclo D (25). The structures of 1 and 2 were elucidated on the basis of spectroscopic evidence. Among the isolates including 17 previously reported coumarins, 1 (IC₅₀=2. µM), 2 (3. µM), and mammea /AB cyclo D (21, 3.1 µM) showed relatively strong inhibitory activities comparable to the activity of the synthetic nonsteroidal aromatase inhibitor aminoglutethimide (2.0 µM).

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