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Volume 109, Issue 10
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Hiroyuki ISHIBASHI1989 Volume 109 Issue 10 Pages 685-706
Published: October 25, 1989
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThis review describes our studies on the use of sulfur-stabilized carbocations (α-thiocarbocations) to accomplish carbon-carbon bond forming reactions. The reactions are classified into the following four features : 1) electrophilic aromatic substitution, 2) enetype reaction, 3) cationic polar cycloaddition, and 4) olefin cyclization. Applications of these reactions to the synthesis of some medicines and natural products are also described.View full abstractDownload PDF (1304K) -
Mamoru NAKANISHI1989 Volume 109 Issue 10 Pages 707-717
Published: October 25, 1989
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSStopped-flow fluorometry gave a unique opportunity to observe a direct cellular interaction between functionally different subsets of lymphocytes in vitro. By this method the molecular mechanism of receptor-mediated recognition and signaling in T lymphocytes (T cells) has been well analyzed. The method is further in progress to observe calcium signals in a single T lymphocyte by using a digital imaging fluorescence microscope.View full abstractDownload PDF (1133K) -
Makio KITAZAWA, Masuo AKAHANE, Yasushi NAKANO, Kazuhide HAYAKAWA, Kazu ...1989 Volume 109 Issue 10 Pages 718-736
Published: October 25, 1989
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThe derivatives (2) of 3-(2, 3-dihydro-2, 2-dimethyl-3-oxo-5-benzofuranyl) acrylic acid (2b) were synthesized. The compounds (3a-g) in which bromo, methoxy, nitro, amino or acetamido group was introduced on the benzene ring of the derivatives (2) and the compounds (3h-k) in which acryloyl moiety was introduced on the 6- or 7-position of the benzofuranone skeleton also synthesized. Furthermore, propionic acid derivatives (4a-c), acetic acid derivatives (4d-g), formic acid derivatives (4h-k) and oxyacetic acid derivatives (5) were prepared by converting the acryloyl moiety of the derivatives (2) into propionyl, acetyl, formyl and oxyacetyl groups. These compounds were tested for antiulcer activities. Among these compounds, 1-[3-(2, 3-dihydro-2, 2-dimethyl-3-oxo-5-benzofuranyl) acryloyl] piperidine (2d) and 4-[3-(2, 3-dihydro-2, 2-dimethyl-3-oxo-5-benzofuranyl) acryloyl] morpholine (2g) were found to have stronger antiulcer activities.View full abstractDownload PDF (1472K) -
Makio KITAZAWA, Masuo AKAHANE, Yasushi NAKANO, Kazuhide HAYAKAWA, Kazu ...1989 Volume 109 Issue 10 Pages 737-748
Published: October 25, 1989
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSA number of 2-substituted 2, 3-dihydro-3-oxo-5-benzofuranylacryloyl derivatives were synthesized and tested for antiulcer activities in order to study structure-activity relationships. Significant antiulcer activities were found in only the compounds (2e-g, p, s) in which hydroxymethyl and methyl groups or acetoxymethyl and methyl groups were introduced on the 2-position of the benzofuranone skeleton. Among the compounds tested, 1-[3-(2, 3-dihydro-2-hydroxymethyl-2-methyl-3-oxo-5-benzofuranyl) acryloyl] piperidine (2e) was the most promising compound.View full abstractDownload PDF (1000K) -
Tsukasa HAMADA, Tsuneo KAWASHIMA, Norio AWATA1989 Volume 109 Issue 10 Pages 749-754
Published: October 25, 1989
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThe selective and sensitive method for the determination of a new antiallergic agent, 1-(2-ethoxyethyl)-2-(hexahydro-4-methyl-1H-1, 4-diazepin-1-yl)-1H-benzimidazole difumarate (emedastine difumarate, KG-2413), in the human plasma has been developed. Emedastine was determined by the receptor assay after the separation from its metabolites by the use of high-performance liquid chromatography (HPLC). This combined method (HPLC-radioreceptor assay (RRA) method) allowed us the quantification only of 0.3 ng/ml of emedastine in the human plasma. The intra-assay coefficients of variation for the determination were below 12%. Furthermore, the total pharmacologically active metabolites, including unchanged emedastine, was determined by the extraction of the unconjugated metabolites in the human plasma with chloroform followed by the receptor assay (RRA method). The human plasma concentrations measured by the HPLC-RRA method were in good agreement with those by the RRA method. These results suggested that in human pharmacological activities occured by unchanged emedastine itself.View full abstractDownload PDF (663K) -
Susumu KIMURA, Teruko IMAI, Yorishige IMAMURA, Masao UENO, Takeo IIJIM ...1989 Volume 109 Issue 10 Pages 755-759
Published: October 25, 1989
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSTwo kinds of soft gelatin capsules containing meclizine dihydrochloride (MZ) were prepared by using a medium-chain length triglyceride as a base. One is a self-emulsifying type, and the other is an oil dispersing type. The release of MZ from soft capsules and its in vivo absorption behavior were examined and compared with those of a commercial tablet. The release of MZ from the self-emulsifying soft capsule which was only slightly affected by pH was greater than those from the oil dispersing soft capsule and commercial tablet. The serum levels of MZ after the administration of preparations orally to beagle dogs increased in the order of self-emulsifying soft capsule, commercial tablet, oil dispering soft capsule. This result suggests that the self-emulsifying soft capsule is useful for the increase of the bioavailability of the drug.View full abstractDownload PDF (563K) -
Hiroaki MIZUTA, Yasushi KAWAZOE, Keiichiro HAGA, Kenji OGAWA, Tetsuo Y ...1989 Volume 109 Issue 10 Pages 760-765
Published: October 25, 1989
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThe method for the assessment of small intestinal transit time (SITT) in beagle dogs was investigated by using the time for the first appearance of sulfapyridine in the plasma (TFA) after oral administration of salicylazosulfapyridine (SASP). After administration of SASP into the small intestine or the cecum of anesthetized dogs, sulfapyridine (SP) was detected in the plasma only in the latter case. These results indicate that TFA could be an index of arrival time in the cecum, an index of SITT in dogs. A remarkable inter-individual variation of TFA was observed after oral administration of SASP to fasting dogs, and the mean value of TFA was about 3 h. As for intra-individual variation of TFA, both variable and less variable dogs were observed. TFA was prolonged significantly by atropine (0.1 mg/kg, i.v.) and shortened significantly by metoclopramide (0.5 mg/kg, i.v.). As the pharmacological modification of gastrointestinal motility was thus mirrored by TFA, SASP method is considered to be useful for the assessment of SITT in beagle dogs.View full abstractDownload PDF (608K) -
Kazuyoshi SUDEJI, Masao KAWASAKI, Hirohiko INADA, Kazunori KATAYAMA, M ...1989 Volume 109 Issue 10 Pages 766-770
Published: October 25, 1989
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThe effect of iontophoresis on percutaneous absorption of formoterol fumarate (FF) was investigated in vitro with abdominal skin excised from guinea pig. By passive diffusion, the flux at steady state for stripped skin was about 230 times greater than that for intact skin. Therefore, it is suggested that stratum corneum is a barrier for the percutaneous absorption of FF. Penetrated amount of FF increased significantly with an increase in donor concentration from 0.035% to 0.07%. Under the constant current iontophoresis the large flux accompanied with the high applied voltage was shown at the beginning of iontophoresis. Thereafter the flux decreased with a decrease in applied voltage. Under the constant voltage iontophoresis a linear relationship between penetrated amount of FF and time was observed.View full abstractDownload PDF (517K) -
Kazuyoshi SUDEJI, Kazuyoshi FURUSAWA, Hirohiko INADA, Kazunori KATAYAM ...1989 Volume 109 Issue 10 Pages 771-777
Published: October 25, 1989
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSTo clarify the effect of polarity, pulse frequency and duty on the iontophoretic transport of formoterol fumarate (FF), in vitro and in vivo studies were performed with guinea pigs. In the in vitro studies, the flux at steady state was enhanced by the factor 7.61 with anodal iontophoresis in comparison with control, whereas, with cathodal iontophoresis it was restrained by the factor 0.79. When pulse frequency was varied from 0 to 40 kHz, the flux at steady state was enhanced with an increase in pulse frequency. In the in vivo studies with varying the duty of pulse potential from 10 to 100%, the maximum plasma concentration of FF was obtained at a 30% duty. In contrast, the plasma concentration of FF achieved at 100% duty was not high. With stripped skin, no significant difference in the plasma concentration of FF was shown between iontophoresis and control. Consequently, it is suggested that iontophoresis contributes to FF penetration across stratum corneum.View full abstractDownload PDF (619K) -
Hakaru SEO, Kaneto UEKAMA1989 Volume 109 Issue 10 Pages 778-782
Published: October 25, 1989
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThe inclusion complex of digoxin with γ-cyclodextrin was prepared in a molar ratio of 1 : 4, and evaluated for sublingual and oral administrations in humans. In the dissolution tests of digoxin tablets, the increase in dissolution rate and decrease in acid hydrolysis were attained by γ-cyclodextrin complexation. The serum levels of digoxin after sublingual and oral administrations to human healthy volunteers in the form of complex tablets were higher than the digoxin alone, particularly in the case of the sublingual form of γ-cyclodextrin complex. The present data suggested that the sublingual administration of the rapid dissolving form of γ-cyclodextrin complex may be useful for improving the bioavailability of digoxin due to the prevention of acid hydrolysis in stomach and the enhancement of drug absorption rate.View full abstractDownload PDF (589K)
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