YAKUGAKU ZASSHI
Online ISSN : 1347-5231
Print ISSN : 0031-6903
ISSN-L : 0031-6903
102 巻 , 1 号
選択された号の論文の16件中1~16を表示しています
  • 佐藤 公道
    1982 年 102 巻 1 号 p. 1-16
    発行日: 1982/01/25
    公開日: 2008/05/30
    ジャーナル フリー
    Sites and mechanisms of analgesic action of opioid peptides (mainly enkephalins), kyotorphin and morphine, were described. It was particularly shown that the nucleus reticularis paragigantocellularis of the medulla oblongata plays an important role in the production of analgesic effect of these substances through the activation by them of the descending inhibitory system from the nucleus to the spinal dorsal horn neurons.
  • 中垣 正幸, 半田 哲郎, 赤対 茂子, 中山 守雄
    1982 年 102 巻 1 号 p. 17-22
    発行日: 1982/01/25
    公開日: 2008/05/30
    ジャーナル フリー
    Optical densities of liposomes loading different surface charge were measured in aqueous solutions of various added salts to study colloidal stabilities of the systems. Without added salts, surface charge generally resulted in enhanced stability of liposome. The salt effects upon liposome systems were dependent on the type of surface charge. In the cases of liposomes of zero net charge, destabilizing effects on liposomes by anion were as Cl->Br->SCN->I- and substantially corresponded to McBain's lyotropic series which indicated strength of dehydration from hydrophilic colloid. While, for charged liposomes, destabilization effects were in the order of SCN->I->Br->Cl- for postively charged liposomes and of Li+>Na+>K+>Cs+ for negatively charged liposomes, and the binding of counterions to ammonium group or to phosphate group was found to be critical to determine stabilities of liposomes.
  • 萩庭 丈寿, 樋口 義洋, 森 いずみ
    1982 年 102 巻 1 号 p. 23-26
    発行日: 1982/01/25
    公開日: 2008/05/30
    ジャーナル フリー
    1-Benzylisoquinoline N-oxide reacts with [Fe (dipy)3] Cl2 complex catalyst in dil. H2SO4 (pH 1.5-4.0) under N2 atmosphere at 85-95°C to give a protoberberine type compound. Laudanosine N-oxide (I) gives xylopinine (IV), O-methylcorypalline (VI), and N-methylcorydaldine (VII) in the respective yields of 12.5, 3, and 15%. 3, 4-Dimethoxy-N, N-dimethylphenethylamine N-oxide (III) gives a very small amount of VI under the same conditions.
  • 室 富雄
    1982 年 102 巻 1 号 p. 27-35
    発行日: 1982/01/25
    公開日: 2008/05/30
    ジャーナル フリー
    Each diastereomer was isolated from a mixture (Ic) of (2R, 5R)-2-phenyl-3-oxotetrahydro-2H-1, 4-thiazine-5-carboxylic acid (Ic1) and (2S, 5R)-2-phenyl-3-oxotetrahydro-2H-1, 4-thiazine-5-carboxylic acid (Ic2), which was derived from L-cysteine, by using thionyl chloride and their stereostructure was clarified by nuclear magnetic resonance. When each diastereomer (Ic1, Ic2) was allowed to react with equivalent sulfuryl chloride, (1S, 4R)-1-phenyl-2-oxa-5-aza-7-thiabicyclo [2.2.2] octa-3, 6-dione (Vc) was respectively obtained. The reaction of methyl (5R)-2-alkyl-3-oxotetrahydro-2H-1, 4-thiazine-5-carbox-ylates (VIa, b) with sulfuryl chloride afforded methyl (5R)-2-alkylidene-3-oxotetrahydro-2H-1, 4-thiazine-5-carboxylate (IXa, b). The reaction of methyl (5R)-2-phenyl-3-oxotetrahydro-2H-1, 4-thiazine-5-carboxylate (VIc) with sulfuryl chloride afforded N, N'-bis (α-oxophenylacetyl) cystine dimethyl ester (XIIIc) and (2R, 5R, 2'S, 5'R)-bis (5-methoxy-carbonyl-2-phenyl-3-oxotetrahydro-2H-1, 4-thiazin-2-yl) ether (XIVc). The plausible mechanism of the reaction was also discussed.
  • 三由 文久
    1982 年 102 巻 1 号 p. 36-42
    発行日: 1982/01/25
    公開日: 2008/05/30
    ジャーナル フリー
    The thermal behavior of cis-1-thioniabicyclo [4.4.0] decane iodide (cis-TBD-I) and its trans isomer (trans-TBD-I) were investigated in comparison with those of cis- and trans-TBD-Br (Miyoshi, Yakugaku Zasshi, 101, 891 (1981) by means of differential thermal analysis, X-ray diffraction and infrared absorption spectrometry. cis-TBD-I, having a monoclinic C-lattice at room temperature, is transformed into an orthorhombic F-lattice at 47°C. The cis-TBD cations in this orthorhombic F-lattice gradually isomerizes into an equilibrium state in the range of 130 to 180°C. This state contains cis- and trans-TBD cations in an approximately 3 : 2 molar ratio in the case of TBD-Br. This equilibrated compound also forms α-TBD-I crystal in the same way as in α-TBD-Br, in which isomeric cis- and trans-TBD cations are statistically distributed and have statistical orientations. trans-TBD-I, having an orthorhombic C-lattice at room temperature, corresponds to a super lattice of the high temperature phase. It is transformed into an orthorhombic F-lattice at 49°C, and isomerizes into α-TBD-I in the range of 120 to 180°C. On the other hand, cis- and trans-TBD-I form the face-centered orthorhombic mixed crystals which contain 3 to 40 mol percent of cis-TBD-I. From these results, it is concluded that α-TBD-I is one of the mixed crystals in which the content of cis-TBD-I is enriched up to 60 mol percent by thermal isomerization in the crystalline state.
  • 浅川 直樹, 津野 昌紀, 佐伯 保治, 松田 宗泰, 服部 禎一, 上山 政晤, 篠田 愛信, 三宅 康夫
    1982 年 102 巻 1 号 p. 43-48
    発行日: 1982/01/25
    公開日: 2008/05/30
    ジャーナル フリー
    The HPLC method, which has been developed in our previous reports, was examined whether it can be applied to simultaneous, efficient separation and identification of insulin from different species (equine, porcine, bovine and ovine). All of them could be satisfactorily chromatographed under isocratic elution system by using Nucleosil CN as a stationary phase and buffer solution (H3PO4-KH2PO4) as mobile phase.
  • 牧野 由紀子, 松原 行雄, 渡辺 敬三, 広部 雅昭
    1982 年 102 巻 1 号 p. 49-55
    発行日: 1982/01/25
    公開日: 2008/05/30
    ジャーナル フリー
    A method for the determination of Ara-C and Ara-U, the major metabolites of N4-behenoyl-1-β-D-arabinofuranosylcytosine (BH-AC), was established by means of mass fragmentography. The acetylmethylated Ara-C and acetylated Ara-U were prepared and examined by gas chromatography-mass fragmentography (GC-MF). Each derivative was separated on 3% SE-30 column at 250°C. The contents of Ara-C and Ara-U were estimated from the calibration curve with papaverine as an internal standard. The urinary metabolites of BH-AC could be analyzed by this method without any extraction or separation procedure. This method is suitable for the selective analysis of Ara-C and Ara-U from the urinary metabolites of BH-AC.
  • 難波 恒雄, 御影 雅幸, 牛山 つや子
    1982 年 102 巻 1 号 p. 56-62
    発行日: 1982/01/25
    公開日: 2008/05/30
    ジャーナル フリー
    The present paper describes elementary analysis for biological materials by using a wave dispersive type X.M.A. (X-ray microanalyzer). The wave dispersive analysis has been considered to be unadequate for analyzing the elements of biological materials because analytical specimens generally lack any specialized elements incorporated in the materials, and also tend to be damaged and charged at higher accelerating voltage. To overcome these defficulties, the specimens were treated with a reagent which reacted with the materials to be analyzed and then coated with carbon by means of vacuum evaporation. Thus, berberine could be analyzed accurately with the wave dispersive X.M.A. after reacting with ammonium reineckate to give a berberine -Cr- complex, followed by coating with carbon. This method was further applied to determine berberine presented in Coptidis Rhizoma.
  • 合屋 周次郎, 高舘 明, 藤野 博之
    1982 年 102 巻 1 号 p. 63-68
    発行日: 1982/01/25
    公開日: 2008/05/30
    ジャーナル フリー
    A fluorescent labeling method has been developed for the determination of α-ketocarboxylic acids (pyruvic acid, α-ketobutyric acid and phenylpyruvic acid). Their reactions with N, N'-dicyclohexyl- and N, N'-diisopropyl-O-(7-methoxycoumarin-4-yl)-methylisourea (DCCI and DICI) in the presence of N, N-dimethylhydrazine in acetonitrile at 80°C for 1 h yielded (7-methoxycoumarin-4-yl) methyl esters of α-substituted α-(N, N-dimethylhydrazono) acetic acid (IIIa-c). Thin-layer chromatographic separation and fluorescence measurement of the esters allow the determination of α-keto acids at concentrations as low as 1-150 n mol/ml. Levulinic acid (γ-keto acid) reacted with DCCI and DICI as well as monocarboxylic acids to give the corresponding ester in a good yield.
  • 松丸 秀夫, 土屋 晴嗣, 紺野 恭史, 吉本 秋雄
    1982 年 102 巻 1 号 p. 69-75
    発行日: 1982/01/25
    公開日: 2008/05/30
    ジャーナル フリー
    To study the dissolution behaviour of aminophylline (AP) and the mechanism of the crystallization phenomenon of theophylline (TH) in aqueous solution, the property of interaction of TH with aliphatic amines was investigated. It was observed that the solubility of AP was dependent on its amount fed to water and the maximum solubility appeared at the initial stage of dissolution of AP. The solubility of TH decreases with the crystallization of TH. It was found that the interaction of TH with aliphatic amines was affected by pH of the solution and the stability constants of complexes apparently varied with pH. In the case of ethylenediamine (ED), the molar ratio 2 : 1 (TH : ED) complex was formed at relatively high pH. It was suggested that AP was unstable in water (pH 6-7), dissociated to TH and ED rapidly, and TH crystallized in the solution.
  • 松田 芳久, 川口 祥代, 臼杵 佳代子, 江口 直美
    1982 年 102 巻 1 号 p. 76-82
    発行日: 1982/01/25
    公開日: 2008/05/30
    ジャーナル フリー
    In order to improve the dissolution characteristics of hydrophobic drug from capsule dosage forms, a hydrophilic and non-ionic surfactant was allowed to adsorb onto crystal surfaces ; the solid-state polyoxyethylene cetyl ether and phenylbutazone, dissolved into methylene chloride, were cospray-dried in a mini-spray drier. The concentrations of surfactant added varied in the range of 0-1%. From the results of scanning electron photomicrographic observations of spray-dried samples, it was estimated that a thin film of the surfactant was developed over the crystal surfaces. The surface characteristics of the samples were evaluated by a contact angle measured by the droplet method. The contact angle decreased significantly in the range of more than 0.2% addition of surfactant, and, thus, the effective hydrophilization could be achieved. As for hydrophobic or hydrophilic formulation systems containing a small amount of surfactant-treated phenylbutazone, the hydrophilization effect was plainly reflected in the contact angle and a dissolution rate from an encapsulated formulation in the former system, whereas it was not apparently reflected in the latter.
  • 池田 陽一, 松元 孝次, 国弘 和雄, 不破 亨, 上釜 兼人
    1982 年 102 巻 1 号 p. 83-88
    発行日: 1982/01/25
    公開日: 2008/05/30
    ジャーナル フリー
    The interactions of 12 essential oils with α- and β-cyclodextrins (α-CyD, β-CyD) were investigated in aqueous solution and in solid phase by solubility method, powder X-ray diffractometry, and thermal analyses (DTA, TG). Referring to the Bs type phase solubility diagrams, the solid complexes of essential oils with α- and β-CyDs were prepared, and their molar ratios were found to be 1 : 2 (guest molecule/α-CyD) and 1 : 1 (guest molecule/β-CyD), respectively. X-Ray diffraction patterns of the complexes showed a typical channel type of crystal packing for both α- and β-CyD systems. Apparent stability constants (Kc') of β-CyD complexes were greater than those of α-CyD complexes, where the steric and hydrophobic factors of the essential oils appeared to be responsible for the magnitude of Kc'values. The volatility and photooxidation of essential oils were significantly retarded by the binding to CyDs. The improved thermal and photochemical stabilities of the essential oils through inclusion complex formation suggest the ease of handling with prolonged storage time.
  • 府川 和永, 伊藤 義彦, 大林 繁夫, 岩舘 克治, 入野 理, 沢辺 隆司
    1982 年 102 巻 1 号 p. 89-98
    発行日: 1982/01/25
    公開日: 2008/05/30
    ジャーナル フリー
    Several test conditions for evaluating acute and chronic irritancy of powder drugs to be used in the treatment of erosive and ulcerative skin lesions were studied on the skin of rats and rabbits. It was found histologically that the stratum corneum could be removed satisfactorily from the skin of rabbits by repetition of the stripping technique with a cellophane adhesive tape. Applications of a powder containing a high concentration of aluminum chlorohydroxy allantoinate, which possesses a low irritancy level as active substance, to this stratum corneum-removed skin and to ulcerated skin produced surgically confirmed simillar sensitivities in both prepared surfaces in eliciting acute irritation reactions. Chronic irritation reaction, fibrosis and granuloma formation were observed histologically after a single application of unabsorbable powder bases, talc and zinc oxide on the wounded skin of rats, while absorbable powder base, corn starch produced little or no reaction. By grading the extent of granuloma in the tissue, it was possible to evaluate the chronic irritancy of powder bases. It was found that the addition of magnesium carbonate to the corn starch as a dispersal agent was essential for rapid absorption and minimum reaction in tissue. The above results indicate that co-evaluation by using the stratum corneum-removed rabbit skin test to observe the acute irritative effects of active substances and the wounded rat skin test to observe the chronic irritative effects of bases provide a sensitive and reliable indicator of the irritancy of powder drugs on erosive and ulcerative skin lesions.
  • 三ヶ島 浩, 後藤 一洋
    1982 年 102 巻 1 号 p. 99-103
    発行日: 1982/01/25
    公開日: 2008/05/30
    ジャーナル フリー
    Addition of adenosine diphosphate (2 μM) and adrenaline (5 μM) to human plateletrich plasma (PRP) resulted in biphasic aggregation in vitro. The preincubation of 2-{4-(2-imidazo [1, 2-α] pyridyl) phenyl} propionic acid (miroprofen) with PRP showed a dose-dependent inhibition of the second phase but not of the first phase. Rabbit platelet aggregation (PA) with a concomitant malondialdehyde (MDA) formation induced by arachidonic acid (AA, 0.5 mM) was inhibited by miroprofen and acetylsalicylic acid (ASA). The concentration of miroprofen causing a 50% inhibition of PA and MDA formation was 0.154 and 0.121 μg/ml, and about 30 and 50 times as potent as that of ASA respectively. Oral treatment of rabbit with miroprofen and ASA resulted in inhibition of AA-induced PA and generation of prostaglandin I2-like material (PGI2) from vessel walls. The duration of miroprofen-induced inhibition of PA was longer than that of PGI2 generation at doses of 1 and 3 mg/kg. At a dose of 3 mg/kg of miroprofen, inhibition of PA lasted up to 24 h. When ASA was treated with 100 mg/kg inhibition of PA was shorter than that of PGI2 generation, whereas inhibition of PA lasted slightly longer than that of PGI2 generation at a dose of 10 mg/kg. These results suggest that miroprofen inhibits the prostaglandin synthetic pathway of platelets more selectively than that of the vessel wall, and that it may have an antithrombotic activity.
  • 鹿島 長次, 加藤 明良, 表 美守
    1982 年 102 巻 1 号 p. 104-106
    発行日: 1982/01/25
    公開日: 2008/05/30
    ジャーナル フリー
    The antiinflammatory activity of eighteen 1-aryl substituted 2 (1H)-pyrimidinones (I and II) and five their salts of D-camphor-10-sulfonic acid was examined. Six 2 (1H)-pyrimidinones (Ia, b, e, h, IIb, and d) exhibited potent antiinflammatory activity, but the safety area of these compounds was found to be narrow from the result of LD50 value.
  • 原 昭二, 岡 希太郎, 土橋 保夫, 大熊 俊一
    1982 年 102 巻 1 号 p. 107-109
    発行日: 1982/01/25
    公開日: 2008/05/30
    ジャーナル フリー
    A system for programmed flow preparation was developed by carrying the usual batch process into flow manipulations. All processes in preparative chemistry, including reactions, extraction, and chromatography, can be performed by passing the solution along a programmed course controlled by simple valve operations. As an application of the system to chemical synthesis, usual acylation reaction such as protection of α-amino acid was carried out successfully.
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