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SEIJI KUZUNA, MIKIHIKO OBAYASHI, SHIGERU MORIMOTO, KIYOHISA KAWAI
1979 Volume 99 Issue 9 Pages
871-879
Published: September 25, 1979
Released on J-STAGE: May 30, 2008
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A new steroid, 11β, 17α-dihydroxy-21-methylpregna-1, 4-diene-3, 20, 21-trione 17-acetate (TSC-5) was tested for its inhibitory effect on acute, subacute and chronic inflammation by systemic administration (p.o. and s.c.) or local application, as well as its glucocorticoid effects in experimental animals. TSC-5 showed potent anti-inflammatory activities comparable to those of prednisolone in acute and subacute inflammation models, but its inhibitory effect on chronic inflammation was less than that of prednisolone in rats. Unlike prednisolone, TSC-5 was found to have local anti-inflammatory activity in rats, where TSC-5 was one half as active as prednisolone 21-tert-butylacetate. TSC-5 was 1/12 as active as prednisolone in glycogendeposition activity by s.c. administration. The inhibitory effect of TSC-5 on antibody formation in mice by s.c. and p.o. administrations was less potent than that of prednisolone. TSC-5 was less potent than prednisolone in thymus-involution effect, but the adrenalinvolution effects of both compounds were almost the same in rats. Thus, TSC-5 showed a significant gap between anti-inflammatory and glucocorticoid activities.
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KAZUO KUBO, NORIKI ITO, YASUO ISOMURA, ISAO SOZU, HIROSHIGE HOMMA, MAS ...
1979 Volume 99 Issue 9 Pages
880-888
Published: September 25, 1979
Released on J-STAGE: May 30, 2008
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Condensation of 4-cyano-3-butenoates (IV) with 1, 2-diamine or 1, 2-aminothiol was carried out. Imidazopyridones were obtained by the reaction of IV with aliphatic 1, 2-diamine. The reaction of IV with o-phenylenediamine resulted in the formation of imino-pyridobenzimidazole (VII), which was converted to the corresponding pyridone derivative (IX) on hydrolysis. The predominant tautomeric forms of VII and IX are discussed on the basis of nuclear magnetic resonance and ultraviolet spectra. In the reaction of IV with 2-aminoethanethiol or o-aminothiophenol, the thiazoline ring was formed by condensation between the cyano group of IV and the amino and thiol groups of the 1, 2-aminothiol, and the resulting thiazoline compound was further converted into thiazolopyridone or oxo-pyridobenzothiazole, respectively, by cyclization with an acid catalyst. Some of these pyridone derivatives showed strong anti-inflammatory activity.
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SHIGERU AONUMA, YASUHIRO KOHAMA, SHIGEKO FUJIMOTO, MASAKO YONEDA, MASA ...
1979 Volume 99 Issue 9 Pages
889-894
Published: September 25, 1979
Released on J-STAGE: May 30, 2008
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A protein inhibitive of both gastric juice secretion and carrageenin edema formation in rats was isolated from rabbit skin tissues with Arthus reaction. The tissues obtained at 24 hr of Arthus reaction were minced and dried with acetone. Dried powder was extracted with distilled water (pH 8.0), and the precipitate formed at pH 4.5 was removed from the extract. An inhibitory activity was concentrated by precipitation with 30% ammonium sulfate saturation, followed by fractionation with chromatography over Sephadex G-200 and DEAE cellulose columns. The yield of the purified active component, anti-ulcerogenic protein from rabbit skin with Arthus reaction, (APRA) was 31 mg from 100 g of tissues. APRA was a protein with a small amount of carbohydrate and free of nucleic acid, had a molecular weight of 140000 in the native condition of gel filtration with Sephadex G-200 and consisted of 50000 and 23500 subunits with polyacrylamide gel electrophoresis in the presence of 2-mercaptoethanol and sodium dodecyl sulfate, as well as rabbit serum IgG. Its amino acid composition was similar to that of IgG except for histidine and cystine. But APRA did not react with guinea pig antiserum to rabbit serum IgG in precipitin test in agar. This protein (10 mg/kg, i.p.) showed the % inhibition of 46.9, 60.4, 42.2 and 46.5 in gastric juice volume, total acid output, total peptic activity and fore-stomach ulceration, respectively, in pylorus-ligated rats. Also, APRA (20 mg/kg, s.c.) inhibited carrageenin edema formation at a degree of 40% 4, 5 and 6 hr after irritant injection in rats. APRA did not represent irritant activity by subplantar injection in rats, any protease activity or any anti-papain activity in the casein digestion method.
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EIKO YOSHIOKA, RUMIKO KONDO, HIROAKI KUBO, IKUO MORIGUCHI, NOBUO SUGUR ...
1979 Volume 99 Issue 9 Pages
895-900
Published: September 25, 1979
Released on J-STAGE: May 30, 2008
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The bioavailability of aminophylline was investigated by comparing the areas under concentration-time curves for intravenous aminophylline with a plain uncoated aminophylline tablet and an aminophylline suppository. Six healthy adult volunteers received 250 mg aminophylline intravenously, 300 mg orally and 600 mg rectally, according to the three-way crossover method. Serum theophylline concentration was measured for at least 30 hours by high-performance liquid chromatography. The fraction of the dose absorbed averaged 0.91±0.10 for the tablet while the value for the suppository was 0.73±0.11. The maximum serum concentration converted in terms of 250 mg aminophylline was 7.76±0.92 μg/ml for the tablet and 4.79±0.49 μg/ml for the suppository. Peak serum concentration time averaged 2.0±0.4 hr for the tablet and 4.9±0.5 hr for the suppository. These results demonstrate that absorption from these dosage forms was reliable and that the aminophylline tablet and suppository may be efficacious clinically. Dosage regimens of the aminophylline tablet and suppository calculated from the above data are presented.
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MASAKO MAEDA, AKIO TSUJI
1979 Volume 99 Issue 9 Pages
901-906
Published: September 25, 1979
Released on J-STAGE: May 30, 2008
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The electronic absorption and circular dichroism (CD) spectra of Ni (II) complex derived from N-salicylidene-d (+)-α-methylbenzylamine (I) were measured in various solvents. The chloroform solution of Ni (II) complex show the electronic absorption and CD spectra which are different from those in methanol and pyridine solutions. The Ni (II) complex took an octahedral structure in methanol or pyridine, and square planar structure in chloroform. Proton magnetic resonance spectra of Al (III) complexes of (I) and various N-salicylideneimines were measured and the relationship between chemical shift of imine proton and the structure of amine was discussed.
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YOSHIHISA MATSUDA, KIMIKO KOUZUKI, MARIKO TANAKA, YUKO TANAKA, JUNKO T ...
1979 Volume 99 Issue 9 Pages
907-913
Published: September 25, 1979
Released on J-STAGE: May 30, 2008
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Gelatin films, as a model of practical dosage form, and gelatin capsules were exposed to ultraviolet ray, and their photostability was examined from the point of water vapor permeability and dissolution properties. The rate of water vapor transmission decreased within the range of film thickness studied, and its reciprocal increased linearly with increasing exposure time. In indomethacin capsules, the water vapor transmission through the capsular wall was not apparently affected by the ultraviolet irradiation. The dissolution time of gelatin films was also affected and delayed by increasing exposure time. It was saturated after 2 hr exposure but did not change by further exposure. These evidences were reflected on the dissolution rate of indomethacin capsules after 8 hr exposure. It was found that the capsules were stable to photoirradiation under the ordinary storage condition.
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HIDEHARU YOKOI, HIROSHI KASHIWAGI, SABURO ENOMOTO, HIROSHI TAKAHASHI
1979 Volume 99 Issue 9 Pages
914-918
Published: September 25, 1979
Released on J-STAGE: May 30, 2008
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Free radicals were found on the surface of potato starch particles when in contact with some kinds of silicates and silicas. Similarly, radical formation also occurs when the potato starch alone is heated. The reaction mechanism of this radical formation of the mixture may be caused by the heat arising from immersional wetting of additives in the surface water of potato starch particles, or some kinds of chemical reactions on the surface. The maximum amount of radicals formed was 1.1-3.0×10
15 spins/g at the proportion of 0.5-1.0% of additives. Finally, the relationship between radical formation and fluidity is discussed.
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MOTOKO TAKEDA, AKIO TSUJI
1979 Volume 99 Issue 9 Pages
919-923
Published: September 25, 1979
Released on J-STAGE: May 30, 2008
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Fluorophotometric assays for serum lactate dehydrogenase (LDH) and creatine phosphokinase (CPK) were developed. α-Oxo-acids react with pyridoxamine and zinc (II) ion to produce a characteristic fluorescence (Ex. 395 nm, Em. 475 nm). This fluorescence reaction was applied to the assay of LDH and CPK activity. The method for the assay of LDH activity is based on the determination of pyruvate produced in the incubation mixture containing lactate and nicotinamide adenine dinucleotide. The CPK activity is also determined by fluorimetric assay of pyruvate in the incubation mixture containing creatine, adenosine triphosphate, phosphoenolpyruvate and pyruvate kinase. These methods require only 5-10 μl of serum sample. The values obtained by these methods satisfactorily correlate with those obtained by the ordinary ultraviolet methods and showed good reproducibility. The correlation coefficients are 0.960 for LDH and 0.965 for CPK, respectively. The method for CPK could be applied to the assay of CPK isoenzymes.
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FUMIHISA MIYOSHI, KENJI TOKUNO, TOKUNOSKE WATANABE, MASANORI MATSUI, T ...
1979 Volume 99 Issue 9 Pages
924-928
Published: September 25, 1979
Released on J-STAGE: May 30, 2008
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The existence of two polymorphic modifications (α and β) of 1-methylthiolanium iodide was found by means of thermal analysis, X-ray diffraction and infrared absorption spectrometry. The transition point and the enthalpy of transition (ΔH
tr) are 78° and 5.4 kJ mol
-1, respectively, by differential scanning calorimetry. The transition is enantiotropic. The crystal structure of the α-phase (room temperature) is determined by single-crystal X-ray analysis. The crystal is orthorhombic, space group pnma, with a=10.82, b=6.37, c=11.90 Å, Z=4. The structure was solved by heavy-atom methods and was refined by full-matrix least-squares calculations to R=0.056 for 637 observed reflections. The structure is ionic, composed of I
- ions and 1-methylthiolanium ions. The 1-methylthiolanium ion has mirror symmetry and adopts the envelope conformation with the methyl group in axial position. The β-phase was examined by X-ray powder diffraction methods at 100°. The lattice type is face-centered orthorhombic with a=10.97, b=6.72, c=11.63 Å, Z=4. Consequently, the space group is restricted to F222, Fmm2 or Fmmm. The zinc-blende type structure based on F222 is the most plausible one on the basis of the packing of the ions. These results suggest that in the β-phase the 1-methylthiolanium ions have statistical orientations.
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ISAMU SAIKAWA, SHUNTARO TAKANO, KAISHU MOMONOI, ISAMU TAKAKURA, CHIAKI ...
1979 Volume 99 Issue 9 Pages
929-935
Published: September 25, 1979
Released on J-STAGE: May 30, 2008
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7-[D(-)-α-(4-Alkyl-2, 3-dioxo-1-piperazinecarboxamido) phenylacetamido]-3-substituted methyl-3-cephem-4-carboxylic acids (I) were prepared. In vitro antibacterial activity against S. aureus, E. coli, Ps. aeruginosa, P. vulgaris and K. pneumoniae was tested and it was found to have a strong antibacterial activity against gram-negative bacilli, especially to Ps. aeruginosa and P. vulgaris.
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HIROSHI NAKAGAWA, EIHEI FUKUOKA, YOSHINOBU NAKAI
1979 Volume 99 Issue 9 Pages
936-943
Published: September 25, 1979
Released on J-STAGE: May 30, 2008
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The degree of preferred orientation of aspirin crystals in a tablet as a function of compression force was measured using the X-ray diffraction method. Preferred orientation took place during compression and the degree was affected by the size and morphology of the crystals. Thin, plate-like crystals had the strong tendency to orient preferentially at an early stage of compression, while pulverized crystals oriented gradually at over 100 kg/cm
2 of the compression force. In addition, volume, specfic surface area, pore size distribution and breaking strength of the tablets were measured and the relationship among these factors was investigated.
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MASAO TOHNO, KAZUHIKO KIMURA, MICHIKO NAGAHARA, YASUO SAKAI, TATSUYA O ...
1979 Volume 99 Issue 9 Pages
944-957
Published: September 25, 1979
Released on J-STAGE: May 30, 2008
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Urinary metabolites of dogs and humans receiving befunolol (BF) were isolated by column chromatography on Amberlite XAD-2 resin and thin layer chromatography on silica gel. Unchanged BF and the following ten metabolites containing five glucuronides were identified in the dog by mass spectrometry (including GC/MS) : I, II, III, IV, V, O-glucuronide of 7-side-chain of BF (BF-7-OG), O-glucuronide of 7-side-chain of I (I-7-OG), O-glucuronide of 2-side-chain of I (I-2-OG), O-glucuronide of phenolic OH of III (III-4-OG) and O-glucuronide of phenolic OH of IV (IV-4-OG). The following five substances were detected in humans : BF, I, BF-7-OG, I-7-OG and I-2-OG. Neither III-4-OG, a major metabolite in the dog, nor its aglycone (III) was detected in humans, suggesting a species difference in the metabolic pathway of BF.
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KOICHI SATOH, MASAO YAMAGUCHI, ISAO OGURA
1979 Volume 99 Issue 9 Pages
958-960
Published: September 25, 1979
Released on J-STAGE: May 30, 2008
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Guaiazulene (7-isopropyl-1, 4-dimethylazulene) was heated at 350-600° for about 20 min in a quartz tube under nitrogen atmosphere. Above 450°, it was converted to 7-isopropyl-4, 5-dimethylazulene, 7-isopropyl-4, 8-dimethylazulene and unkown products. The yields of the former two products were the maxima at 550°.
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YASUSHI TAKAGISHI, KOJI SATO, KEIZO TOMITA, TERUO SAKAMOTO
1979 Volume 99 Issue 9 Pages
961-963
Published: September 25, 1979
Released on J-STAGE: May 30, 2008
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A simple HPLC assay was developed for acetohexamide and hydroxyhexamide, its active metabolite in plasma. Plasma sample was extracted with benzene-ethyl acetate at pH 5 and the organic phase was evaporated. The 50% acetonitril solution of the residue was chromatographed using Lichrosorb RP-8 reverse phase column and the mobile phase composed 0.2% AcOH-acetonitrile (1 : 1). This method can be used for bioavailability and clinical pharmacokinetic studies of acetohexamide.
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