著者
大島 健吉
出版者
公益社団法人日本薬学会
雑誌
藥學雜誌 (ISSN:00316903)
巻号頁・発行日
no.154, pp.1114-1118, 1895-12-26
著者
竹内 洋文
出版者
公益社団法人日本薬学会
雑誌
ファルマシア (ISSN:00148601)
巻号頁・発行日
vol.26, no.4, pp.362-363, 1990-04-01
著者
菅澤
出版者
公益社団法人日本薬学会
雑誌
藥學雜誌 (ISSN:00316903)
巻号頁・発行日
no.512, pp.869-870, 1924-10-26
著者
松南 千壽
出版者
公益社団法人日本薬学会
雑誌
藥學雜誌 (ISSN:00316903)
巻号頁・発行日
no.520, pp.540-552, 1925-06-26

Tropacocainhydrochlorid kann eine Stunde lang auf 130° erhitzt werden, ohne dass dabei eine Veranderung (sowohl in chemische als auch in physikalischer Hinsicht) zu befurchten. Erst bei zwei stundigem Erhitzen auf 135-140° wird eine geringe Veranderung wahrnehmbar, die jedoch die Erfordernisse von Ph. Jap. nicht beeintrachigt. Sterilisirt man eine 2% ige wasserige salzsaure Tropacocainlosung nach der ublichen Methode, so bemerkt man ein Zeichen von Verseifung, indem man aus 10 g Salz 0.0004-0.0005 g Benzoesaure und 0.0006-0.0007 g Pseudotropin erhalt. Gegen Hitze ist die wasserige Losung des Pseudotropins sehr bestandig. Erst beim Erhitzen im Einschliessrohr auf 170-180° wird eine Spur Tropidins gebildet.Der Alkaligehalt des weichen Glases wirkt beforded auf die Verseifung der salzsauren Tropacocainlosung. Dem Sonnenlicht bezw. Urtraviolettstrahlen ausgesetzt zeigte das Tropacocainhydrochlorid und seine Losung eine auffallende Bestandigkeit.
著者
FURUSE KAZUMARO ISHIZEKI CHUICHI IWAHARA SHIGEO
出版者
公益社団法人日本薬学会
雑誌
Journal of pharmacobio-dynamics (ISSN:0386846X)
巻号頁・発行日
vol.6, no.6, pp.359-372, 1983-06

The spermicidal activities of seven nonionic surfactants against human spermatozoa were objectively determind by a statistical method, and two types of ionic surfactants were also studied for purposes of comparison. The nonionic surfactants, p-menthanylphenyl poluoxyethylene adducts used in this work were synthesized from turpentine oil. These surfactants were used in the experiment after a careful confirmation of their chemical composition and molecular weight distribution. The spermicidal activities of the surfactants in terms of minimum concentrations to accomplish irreversible immobilization of all sperms in zero time was, in decreasing order, nonionic, cationic and anionic. When the most commonly used nonionics alone were considered, the sequence of decreasing spermicidal potency was isononylphenyl polyoxyethylene (9.0) ether (nonoxynol-9), p-menthanylphenyl polyoxyethylene (8.8) ether (menfegol), isooctylphenyl polyoxyethylene (9.0) ether(octoxynol-9).The surface tension and wetting time of these surfactants were determined with a view to finding physico-chemical measures of their spermicidal activity. In the statistical analysis regarding all the nine surfactants, there was a significant correlation (p<0.05) between spermicidal potency and critical micelle concentration (cmc) whereas there was no significant relationship between spermicidal potency and cmc regarding the seven nonionics. There was again no significant correlation between spermicidal potency and wetting time in all but nonionics with a common hydrophobic structure. As neither surface tension nor wetting time appeared to be a valid factor, general measure of spermicidal potency of nonionic surfactants, the partition ratios between n-octanol or n-hexane and water was determind. As a result, it was revealed that there was a significant correlation (p<0.05) between spermicidal potency and partition coefficient, when four types of nonionic surfactants with different hydrophobic group, which were chosen from among the seven nonionics, were tested with n-hexane.The close relationship between spermical activity and partition coefficient suggests that the spermicidal activities of these surfactants are associated with their structural affinity to the lipids of spermatozoal cell membrane.
著者
砂本 順三 岩本 清 上杉 辰顕 小島 一幸 古瀬 一磨
出版者
公益社団法人日本薬学会
雑誌
Chemical & pharmaceutical bulletin (ISSN:00092363)
巻号頁・発行日
vol.32, no.8, pp.2891-2897, 1984-08-25

To evaluate the spermicidal effect of several nonionic surfactants against human spermatozoa, the physicochemical lysis of liposomal membranes by the surfactants has been investigated. Surfactants employed in this work were menfegol (TS-88), nonoxynol-9 (INP-90), octoxynol-9 (NOP-90), hexadecyltrimethylammonium bromide (CTAB), and sodium dodecylsulfate (SDS). Lysis of liposomes by these spermicidal surfactants was quantitatively followed by monitoring the induced release of carboxyfluorescein (CF) encapsulated in the interior of liposomes. When the liposomes reconstituted with boar spermatozoal lipids and about 31% (by wt.) cholesterol were employed, the sequence in efficiency of the surfactant-induced CF release from the liposomes was significantly correlated with that of efficiency of the surfactants in immobilizing human sperm (p<0.05). On the other hand, when egg lecithin liposomes or the liposomes reconstituted with boar spermatozoal lipids and cholesterol less than 21% (by wt.) were utilized, the sequence in efficiency of CF release from these liposomes coincided with that in the inhibiting effect of the surfactants on the fertilizing ability of sea urchin sperm. These effects were closely correlated with the membrane fluidity as controlled by the cholesterol content or lipid composition. Among menfegol analogues from TS-40 through TS-200,the efficiency in induced CF release from the liposomes showed a maximum at around ten ethylene oxide units length of the hydrophilic moiety in the surfactant. This was also the case for spermicidal effect of the TS-series surfactants. The data obtained are discussed at the molecular level from the viewpoint of the structural characteristics of the surfactants.
著者
神津 公
出版者
公益社団法人日本薬学会
雑誌
衛生化学 (ISSN:0013273X)
巻号頁・発行日
vol.28, no.2, pp.111-113, 1982-02-28

Caffeine and sodium benzoate were determined by high performance liquid chromatography with a UV detector by use of stainless column (4.0 mm×0.15 m) packed with Nucleosil _5C_<18>. Mobile phase was M/30 KH_2PO_4+M/30 Na_2HPO_4・2H_2O-methanol (70 : 30). The sample was dissolved in 20% aqueous methanol. Determination was carried out successfully by using antipyrine as an internal standard and by maintaining the temperature at 40℃. The recovery of sodium benzoate and caffeine from synthetic mixtures were 97.2±1.0% and 99.8±1.1%. This method was applied to three kinds of pharmaceutical preparations. The contents of sodium benzoate and caffeine were 48.4-50.1% and 49.0-49.6%.
著者
Liu Weiping Qing Chen Chen Xizhu YE Qingsong YU Yao HOU Shuqian
出版者
公益社団法人日本薬学会
雑誌
Chemical & pharmaceutical bulletin (ISSN:00092363)
巻号頁・発行日
vol.56, no.5, pp.659-662, 2008-05-01
被引用文献数
1 6

New JM118 (active form of satraplatin) analogues with N-cyclohexyl-1,3-propanediamine (N-chpda) as the carrier, cis-[Pt(N-chpda)X_2] (X_2=2Cl^- (1), oxalate (2), malonate (3), 1,1-cyclobutanedicarboxylate (CBDCA) (3), and 3-hydroxy-1,1-cyclobutanedicarboxylate(HO-CBDCA) (4)), have been synthesized and characterized by elemental analysis and spectroscopic data along with X-ray crystal structure for a representative compound cis-[Pt(N-chpda)Cl_2]. The complexes have also been evaluated for their in vitro anticancer activity. All these analytical data are in good agreement with the structures of the desired compounds. The Pt(II) is in a square planar environment and is coordinated by a chelating N-chpda ligand and 2Cl^- in cis position, and there are two crystallo-graphically independent cis-[Pt(N-chpda)Cl_2] molecules linked together by intermolecular N-H…Cl hydrogen bonds. Compounds 1 and 2 are very active against human lung cancer cell line (AGZY) and human lymphocytic leukemia cell line (Raji), and are much more active than carboplatin. Platinum(II) complexes with N-cyclohexyl-1,3-propanediamine is an alternative choice for mixed ammine/aminoplatinum anticancer drugs.
著者
衣笠
出版者
公益社団法人日本薬学会
雑誌
藥學雜誌 (ISSN:00316903)
巻号頁・発行日
no.319, pp.946-948, 1908-09-26
著者
平古 場朗 森木 弘樹 石橋 龍吾 森本 昌宏
出版者
公益社団法人日本薬学会
雑誌
衛生化学 (ISSN:0013273X)
巻号頁・発行日
vol.18, no.5, pp.342-346, 1972
被引用文献数
1

An examination was made on the sensitive spectrophotometric determination of ammonia-nitrogen in water. Ammonia was determined indirectly by measuring the blue complex produced by reaction with potassium iodide-starch reagent and chloramine compound, which was formed by the reaction of ammonia and hypochlorite at pH 5.4. Unreacted hypochlorite was destroyed with ferrous sulfate before addition of potassium iodide-starch reagent. The absorbance of developed color of the blue complex was measured at 570 mμ. The method was applicable for the determination of ammonia-nitrogen in the range of 0.01 to 0.4 ppm, at between 21 and 26°. The standard deviation was 2.2% on an average absorbance 0.496 of a sample containing 0.2 ppm of ammonia-nitrogen.
著者
沢田 英夫 矢野 博子 木戸 啓
出版者
公益社団法人日本薬学会
雑誌
藥學雜誌 (ISSN:00316903)
巻号頁・発行日
vol.92, no.10, pp.1237-1241, 1972-10-25

Besides the unchanged drug, two major metabolites were found from the urine of animals that received orally high doses of bromazepam, 7-bromo-1,3-dihydro-5-(2-pyridyl)-2H-1,4-benzodiazepin-2-one. The metabolites were purified by column chromatography on silica gel and recrystallization. From the spectral and elemental analysis data, the structure of these metabolites were identified as 2-amino-5-bromobenzoylpyridine and assumed to be 2-amino-5-bromo-3-hydroxybenzoylpyridine, the latter being excreted as its glucuronide in the urine. It may be concluded that bromazepam after opening of the diazepine ring undergoes a process of hydroxylation.
著者
沢田 英夫 原 明
出版者
公益社団法人日本薬学会
雑誌
藥學雜誌 (ISSN:00316903)
巻号頁・発行日
vol.95, no.4, pp.430-438, 1975-04-25

Five metabolites appearing in the urine of the rabbit fed bromazepam were isolated; these are 2-(2-amino-5-bromobenzoyl)pyridine (ABBP), 2-(2-amino-5-bromo-3-hydroxybenzoyl)pyridine (3-OH ABBP), 3-hydroxybromazepam, and two new matabolites, 9-hydroxybromazepam and 5'-hydroxybromazepam. The new metabolites were characterized by thin-layer chromatography (TLC) ; elemental analysis, and infrared, nuclear magnetic resonance, and mass spectrometries. Metabolites, which were excreted mainly as conjugates of glucuronic acid and/or sulfuric acid, were measured by preparative TLC and characteristic colorimetric method after enzymic hydrolysis of the conjugates. Urinary excretion of bromazepam and its metabolites have been studied in dogs, rabbits, mice, rats and guinea pigs after massive doses of bromazepam. The conjugated 3-OH ABBP was the major metabolite in rabbits (17.1% of the dose) and dogs (6.2% of the dose) during 24 hr. The major metabolites found in rats, however, were the conjugated form of 3-OH ABBP (5.3% of the dose), 5'-hydroxybromazepam (4.2% of the dose), and ABBP (3.8% of the dose), and 9-hydroxybromazepam was not excreted. In mice the major metabolite was the unconjugated form of 3-hydroxybromazepam (7.5% of the dose). In guinea pigs, two unknown metabolites, besides the above five metabolites, were excreted, and it was confirmed that one of them was benzhydrol analog of ABBP. When intraperitoneal injection was compared with oral administration of the same dose in the rabbit, the urinary excretion of the ring-cleaved metabolites, ABBP and 3- OH ABBP, decreased, but that of the others, 3-hydroxybromazepam and 5'-hydroxybromazepam, increased. On the basis of these data, pathways of bromazepam were postulated (Chart 1). Quantitative differences in the urinary metabolites of bromazepam in each species was clearly observed during the first 24-hr period.
著者
松本 仁 磯部 明彦
出版者
公益社団法人日本薬学会
雑誌
Chemical & pharmaceutical bulletin (ISSN:00092363)
巻号頁・発行日
vol.29, no.3, pp.603-608, 1981-03-25

The emission spectra and the fluorescence quantum yields of psoralens were measured in various solvents. We found that these compounds show a large Stokes shift, which can be explained in terms of intermolecular charge transfer interaction between a solute molecule and a solvent molecule in an excited singlet state. Psoralens have a larger fluorescence quantum yield in hydroxylic solvents than in non-hydroxylic solvents. These were in the following order : TMP&ap;5-MOP>PS&ap;8-MOP&ap;8-iso-AOP. We postulate that the fluorescence quantum yield is increased by the hydrogen bonding between a solute molecule and a solvent molecule in an excited singlet state. In addition, the fluorescence efficiency was enhanced by the presence of an electron-donating substituent group. The peak wavelengths of the phosphorescence spectra were little affected by the different solvents.