巻号一覧
111 巻, 10 号
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広井 邦雄1991 年 111 巻 10 号 p. 551-569
発行日: 1991/10/25
公開日: 2008/05/30
ジャーナル フリーRecent progress of our studies on asymmetric induction reactions by using chiral organo-sulfur groups as main chiral auxiliaries is reviewed focused on thermal or palladiumcatalyzed rearrangements of chiral allylic sulfinates to sulfones, asymmetric cyclizations by Lewis acid- or palladium-catalyzed ene reactions of chiral allyl esters or phosphine groups in the molecules, and asymmetric 1, 2-rearrangements of cyclopropane systems with chiral sulfinyl groups.抄録全体を表示PDF形式でダウンロード (1369K) -
青山 豊彦1991 年 111 巻 10 号 p. 570-584
発行日: 1991/10/25
公開日: 2008/05/30
ジャーナル フリーVarious aspects of trimethylsilyldiazomethane (Me3SiCHN2, TMSCHN2) and its lithium salts (Me3SiC (Li) N2, TMSC (Li) N2) in organic synthesis as a stable and safe substitute for hazardous diazomethane are reviewed on the following items : 1) properties, 2) preparation, 3) application as a C1-unit introducing reagent, 4) application of [C-N-N] synthon for the preparation of azoles. As a C1-unit introducing reagent, TMSCHN2 and its lithium salt mostly behave in the same way as diazomethane. As a [C-N-N] azole synthon, however, they generally behave in an analogous but not the same way as diazomethane.抄録全体を表示PDF形式でダウンロード (1055K) -
中村 洋, 熊沢 紀子, 太田 節子, 藤田 孝, 岩崎 泰介, 篠田 雅人1991 年 111 巻 10 号 p. 585-591
発行日: 1991/10/25
公開日: 2008/05/30
ジャーナル フリーThe decoctions extracted from the bark and leaf of Acer nikoense MAXIM. (AN) have been used as a folk medicine for eye-wash and hepatic disease. As previously reported, the methanol extract from the bark of AN and the fractions of the methanol extract have protective effects for liver injury induced by carbon tetrachloride (CCl4) in rats. In this study, protective effects of the fractions extracted from the callus of AN were investigated on CCl4-induced liver injury in rat. The active principles for the protection of CCl4-induced liver injury were recognized in a fraction (EF 3-3) obtained by using silica gel chromatography (solvent : CHCl3-MeOH-H2O). The components were further fractionated by silica gel chromatography followed by gel filtration (solvent : CHCl3-MeOH). In addition, the mechanism of the protective action against liver injury induced by CCl4 was also examined. The fractions with protective effects in vivo showed the inhibitory effects on CCl4-dependent lipid peroxidation in microsomal fraction in vitro.抄録全体を表示PDF形式でダウンロード (761K) -
O-Carboxymethyl-O-ethyl-β-cyclodextrinによる1-Hexylcarbamoyl-5-fluorouracil (HCFU) の安定性及びバイオアベイラビリティの向上堀内 保秀, 平山 文俊, 上釜 兼人1991 年 111 巻 10 号 p. 592-599
発行日: 1991/10/25
公開日: 2008/05/30
ジャーナル フリーThe possible utility of O-carboxymethyl-O-ethyl-β-cyclodextrin (CME-β-CyD) as a novel drug carrier was studied in vitro and in vivo, by using 1-hexylcarbamoyl-5-fluorouracil (HCFU) as a model drug. The chemical instability of HCFU in solution and solid state was improved by CME-β-CyD complexation. The in vitro release of HCFU from the CME-β-CyD complex was decelerated in acidic solution, while accelerated at neutral pH regions, showing a typical delayed-release pattern. This pattern was clearly reflected in the blood levels after the oral administration of the complex to dogs, increasing the bioavailability. The present results suggested that CME-β-CyD is useful as a delayed-release-type carrier for the oral administration of chemically labile HCFU.抄録全体を表示PDF形式でダウンロード (855K) -
松木 洋子, 赤澤 美保, 土屋 浩一郎, 桜井 弘, 際田 弘志, 五郎丸 毅1991 年 111 巻 10 号 p. 600-605
発行日: 1991/10/25
公開日: 2008/05/30
ジャーナル フリーBy the use of electron spin resonance (ESR) spectroscopy and of spin-trapping technique, the effects of ascorbic acid on the formation of the free radical intermediates due to isoniazid (INAH) and its metabolites were investigated with a microsomal system. When α-(4-pyridyl 1-oxide)-N-tert butylnitrone (4-POBN) was used as a spin trapping agent, the ESR signal due to hydrazine (Hy) was formed to be most intensive among others. Therefore, it was presumed that Hy is a potent intermediate to cause an INAH-induced hepatic injury. In the presence of ascorbic acid (AA), the free radical formation of Hy, INAH and acetyl hydrazine was significantly inhibited, suggesting that AA may affect the INAH-hepatitis. By the addition of inhibitors of cytochrome P-450 like metyrapone and CO, the generation of the radical from Hy decreased, confirming that the radical is formed by the cytochrome P-450 dependent microsome systems. The 4-POBN-trapped radical species generated from Hy was presumed to be the hydrazyl radical by the results of mass spectrometry.抄録全体を表示PDF形式でダウンロード (621K) -
伊東 明彦, 杉原 正泰1991 年 111 巻 10 号 p. 606-611
発行日: 1991/10/25
公開日: 2008/05/30
ジャーナル フリーThe relationship between dividing properties of the scored tablet and dynamic characteristics of the powder was investigated for proving the effects of physical characteristics of the powder on dividing properties of the scored tablet. Lactose, microcrystalline cellulose, corn starch, synthetic aluminum silicate and Perfiller[○!R] were used as excipients. The dynamic characteristics of the powder, such as tensile strength (T), cohesive force (C), angle of friction (δ), flow factor (FF), shear index (n), C/T (K) and constants of Kawakita's equation of tapping compaction (a, 1/b) were measured. No correlations between coefficient of variation of divided tablet weight and each dynamic characteristics of the powder were found. However, from the result of the multiple regression analysis, multiple regression equation containing C and a as variables was obtained. Then a significant correlation was obtained between coefficient of variation of divided tablet weight and C/a, and also between logaritbms of dividing strength of scored tablets and C/a. As a result, coefficient of variation of divided tablet weight decreased and dividing strength of scored tablets increased with decreasing C/a value.抄録全体を表示PDF形式でダウンロード (609K) -
五郎丸 毅, 池尻 久恵, 橋本 謙二, 松本 洋子1991 年 111 巻 10 号 p. 612-616
発行日: 1991/10/25
公開日: 2008/05/30
ジャーナル フリーQuantitative analyses of iproniazid (IPN) and deuterated analogue (IPN-d6) and of isopropylhydrazine (IP-Hy) and deuterated analogue (IP-Hy-d6) after conversion to pyrazole derivatives (IDP) were carried out by gas chromatography. The complete separation of protio- from deutero-forms of IPN and IDP was achieved by using a fused-silica CBP1 capillary column (50 m). The resolution coefficients between two isotopic molecules were 1.10 for IPN and 1.62 for IDP, respectively. The present isotopic fractionation procedure was applied to the isotope dilution analyses of IPN and IP-Hy. By the measurement of the samples prepared by the addition of known amounts of IPN and IPN-d6 to the control plasma and urine of rat, a linear relationship between peak height ratio and added amount ratio was observed. The correlation coefficients obtained by regression analysis were 0.9990 for the plasma and 0.9999 for the urine, respectively. In the case of IP-Hy, a linear relationship was also observed, and the correlation coeffcients were 0.9998 for the plasma and 0.9997 for the urine, respectively. The present method was compared with the gas chromatography-mass spectrometry method in urinary samples from rats treated with IPN. The results of these parallel determinations were comparable.抄録全体を表示PDF形式でダウンロード (598K) -
松崎 豊, 石橋 恵美子, 小口 幸子, 和久井 容子, 竹田 秀一, 油田 正樹, 尾山 力1991 年 111 巻 10 号 p. 617-620
発行日: 1991/10/25
公開日: 2008/05/30
ジャーナル フリーGomisin A (TJN-101) is one of the lignan components isolated from Schisandra Fruits. A high sensitive and precise method for the determination of TJN-101 and its major metabolite (Met. B) in the rat serum was developed by selected ion monitoring (SIM) with gas chromatography-mass spectrometry (GC/MS) using a fused silica capillary column (SPBTM-1, Supelco). A 100 μl serum sample was used for the solid phase extraction. The calibration curves of TJN-101 and Met. B both showed a good linearity between 2.0 and 2000.0 ng/ml. The analytical precision (intra-assay, C.V. <4.7%), recoveries (98.4±10.1%), and detection limit (2 ng/ml) of TJN-101 indicated that this system was suited for the determination of TJN-101 in biological fluid. In case of Met. B, the same results as TJN-101, were obtained. After oral administration of TJN-101 at a dose of 10 mg/kg to male rats, the average values of the maximal serum concentration of TJN-101 and Met. B were 1446.1±131.8 and 317.4±18.5 ng/ml, respectively. The serum concentrations of these substances could be monitored sufficiently for 8 h after dosing.抄録全体を表示PDF形式でダウンロード (485K) -
竹内 烈, 河部 多佳江, 濱田 喜樹1991 年 111 巻 10 号 p. 621-626
発行日: 1991/10/25
公開日: 2008/05/30
ジャーナル フリーThe title compounds (4b, d-f, h-j) were prepared from 1-[4-(p-substituted phenyl)-2-chloro-n-butyl]-1H-imidazoles and the corresponding thiophenols or mercaptopyridines. Acyloxy compounds (5a-e) were prepared from alcohol (2b) and the corresponding acyl chlorides. In the antifungal activity test, p-tolyl compounds (4e, f) showed as good activity as butoconazole (4c).抄録全体を表示PDF形式でダウンロード (548K)
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