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Volume 51, Issue 1
Displaying 1-23 of 23 articles from this issue
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Regular Articles
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Kotaro Iida, Youhei Hayakawa, Hirokazu Okamoto, Kazumi Danjo, Hans Leu ...Article type: Regular Article
Subject area: [not specified]
2003 Volume 51 Issue 1 Pages 1-5
Published: 2003
Released on J-STAGE: January 01, 2003
JOURNAL FREE ACCESSAn attempt was made to produce carrier particles for dry powder inhalations by the surface treatment of lactose particles with aqueous ethanol solution. Drug/carrier powder mixtures were prepared consisting of lactose carriers with different particle surface properties and micronized salbutamol sulfate. These powder mixtures were aerosolized by Spinhaler®, and in vitro deposition properties of salbutamol sulfate were evaluated by twin impinger. The degree of adhesion between drug particles and carrier particles was determined by the ultracentrifuge separation method. In addition, the air jet sieve method was used to evaluate characteristics of the separation of drug particles from carrier particles in airflow. The average adhesion force (F50) between the surface-treated lactose carrier and drug particles was significantly lower than that of powder mixed with the untreated lactose carrier, indicating that the degree of separation (T50) of drug particles from carrier particles was improved when surface-treated lactose carrier was used. This resulted in an improvement of in vitro inhalation properties.View full abstractDownload PDF (1838K) -
Mohamed A. El-Ries, Gehad Mohamed, Shaeban Khalil, Manal El-ShallArticle type: Regular Article
Subject area: [not specified]
2003 Volume 51 Issue 1 Pages 6-10
Published: 2003
Released on J-STAGE: January 01, 2003
JOURNAL FREE ACCESSTwo simple and accurate methods are described for the determination of piroxicam and tenoxicam in their pharmaceutical preparations. The spectrophotometric method involves the oxidation of these drugs with potassium iodate in acid medium with the liberation of iodine and subsequent extraction with cyclohexane followed by measuring the absorbance at λ=522 nm. Beer's law is obeyed in the concentrartion range of 0.05—1.1 and 0.05—0.6 mg ml−1 for piroxicam and tenoxicam, respectively. The apparent molar absorptivities of the resulting coloured products are found to be 2.7×103 and 2.5×103 l mol−1 cm−1, whereas Sandell sensitivities are 0.012 and 0.013 g cm−2 for piroxicam and tenoxicam, respectively. The potentiometric method involves the direct titration of both drugs with N-bromosuccinimide in acid medium and the end point is determined potentiometrically using platinum indicator electrode. Piroxicam and tenoxicam can be determined quantitatively in the concentration range of 0.33—3.37 and 0.33—4.08 mg ml−1 for tenoxicam and piroxicam, respectively. The standard deviation and relative standard deviation velues are found to be ranged from 0.05—0.07 and 0.37—0.98% and 0.025—0.078 and 0.25—1.2% for tenoxicam and piroxicam, respectively. The two methods are accurate within ±1.0%. Optimum conditions affecting both methods are studied. The proposed methods are applied for the determination of the drugs in pure form and in commercial pharmaceutical preparations.View full abstractDownload PDF (223K) -
Masako Kajihara, Toshihiko Sugie, Akihiko Sano, Keiji Fujioka, Yosuke ...Article type: Regular Article
Subject area: [not specified]
2003 Volume 51 Issue 1 Pages 11-14
Published: 2003
Released on J-STAGE: January 01, 2003
JOURNAL FREE ACCESSSilicone has been utilized as a carrier material for sustained release system of lipophilic drugs. Extensive studies revealed that drug release rate is influenced by factors such as physicochemical properties of the drug and additives.1—5) When a lipophilic drug is highly potent at low concentrations, the drug release rate should be strictly controlled so as to avoid side effects. In this study, using vitamin D3 (VD3) as an example of such drugs, we investigated novel method to suppress initial burst and to modify drug release rate from silicone matrix. As a result, it was found that (a) addition of human serum albumin (HSA) suppressed initial burst and enhanced release rate in the later stage, resulting constant release of VD3, (b) covering a matrix formulation with a membrane of low diffusivity (core-rod formulation) suppressed initial burst and released drug in a constant rate, and (3) using materials for which the drug has high affinity as dissolution solvent (reservoir formulation), the drug release rate was reduced.View full abstractDownload PDF (3338K) -
Masako Kajihara, Toshihiko Sugie, Hiroo Maeda, Akihiko Sano, Keiji Fuj ...Article type: Regular Article
Subject area: [not specified]
2003 Volume 51 Issue 1 Pages 15-19
Published: 2003
Released on J-STAGE: January 01, 2003
JOURNAL FREE ACCESSDrug release mechanism from silicone carrier differs depending on physicochemical properties of the drug. So far, there have been few reports on controlled release of insoluble drug and on simultaneous release of two kinds of water-soluble drugs. The purposes of this study are to establish methods for (1) continuous release of insoluble drug, and (2) release of two kinds of water-soluble drugs from silicone carrier. Polystyrene beads (PSTB) and proteins such as interferon (IFN) and human serum albumin (HSA) were used as model drugs. PSTB was released from silicone only when citric acid (CA) and sodium bicarbonate (SB) existed as additives. The release patterns of IFN and HSA were almost same in the case of matrix and covered-rod formulations, but double-layered formulation released them in different patterns. As far as we are aware, this is the first report on the release of insoluble drug from silicone and the controlled release of two kinds of water-soluble drugs.View full abstractDownload PDF (1800K) -
Takeshi Kuwada, Miyako Fukui, Toshiyuki Hata, Tominari Choshi, Junko N ...Article type: Regular Article
Subject area: [not specified]
2003 Volume 51 Issue 1 Pages 20-23
Published: 2003
Released on J-STAGE: January 01, 2003
JOURNAL FREE ACCESSThe specific optical rotations of (R)-oxopropaline D calculated by two ab initio MO methods were +52±31° and +61±29°, respectively, and (+)-oxopropaline D (3) was presumed to have an R-configuration. On the basis of this theoretical result, the reaction of 1-litio-β-carboline with (R)-glyceraldehyde acetonide followed by oxidation with MnO2 gave (R)-oxopropaline D acetonide (4a), which was consistent with the previously synthesized (+)-oxopropaline D acetonide (4) in all respects. From the results of theoretical calculations and the experimental synthesis, we determined that natural (+)-oxopropaline D (3) has an R-configuration.View full abstractDownload PDF (185K) -
Luelak Lomlim, Noppong Jirayupong, Anuchit PlubrukarnArticle type: Regular Article
Subject area: [not specified]
2003 Volume 51 Issue 1 Pages 24-26
Published: 2003
Released on J-STAGE: January 01, 2003
JOURNAL FREE ACCESSThe stability of andrographolide, the major active diterpene lactone from Andrographis paniculata (BURM. f.) WALL. ex NEES., was determined to show that, while crystalline andrographolide was highly stable even at 70 °C (75% relative humidity) over a period of 3 months, its amorphous phase degraded promptly. Heat-accelerated conditions revealed second-order kinetics of the decomposition with the rate constant at 25 °C (k25 °C) predicted from the Arrhenius plot of 3.8×10−6 d−1. The major decomposed product under elevated temperature (70 °C, 75% relative humidity) is 14-deoxy-11,12-didehydroandrographolide.View full abstractDownload PDF (93K) -
Nobuko Mibu, Miho Yukawa, Nobuhiro Kashige, Yukiko Iwase, Yoshinobu Go ...Article type: Regular Article
Subject area: [not specified]
2003 Volume 51 Issue 1 Pages 27-31
Published: 2003
Released on J-STAGE: January 01, 2003
JOURNAL FREE ACCESSReactions of 1,3-propanediamine with α-dicarbonyl compounds (1a—e) were examined and various condensed heterocyclic compounds such as 1,4-diazepines (2) and 3-pyrimidine derivatives (3) were obtained. Some of 1,4-diazepines (2) showed DNA strand breakage activity.View full abstractDownload PDF (116K) -
Toru Ishikawa, Kyoko Kondo, Junichi KitajimaArticle type: Regular Article
Subject area: [not specified]
2003 Volume 51 Issue 1 Pages 32-39
Published: 2003
Released on J-STAGE: January 01, 2003
JOURNAL FREE ACCESSFrom the water-soluble portion of the methanol extract of coriander (fruit of Coriandrum sativum L.), which has been used as a spice and medicine since antiquity, 33 compounds, including two new monoterpenoids, four new monoterpenoid glycosides, two new monoterpenoid glucoside sulfates and two new aromatic compound glycosides were obtained. Their structures, were clarified by spectral investigation.View full abstractDownload PDF (178K) -
Koichi Itoh, Yuichi Tozuka, Toshio Oguchi, Keiji YamamotoArticle type: Regular Article
Subject area: [not specified]
2003 Volume 51 Issue 1 Pages 40-45
Published: 2003
Released on J-STAGE: January 01, 2003
JOURNAL FREE ACCESSTo improve the aqueous solubility of a poorly water-soluble drug, N-[2-(3,5-di-tert-butyl-4-hydroxyphenethyl)-4,6-difluorophenyl]-N′-[4-(N-benzylpiperidyl)]urea (N-4472), organic acid/N-4472 evaporates were prepared by using succinic acid, L-tartaric acid, citric acid and L-ascorbic acid (VC). Among these evaporates, only the VC/N-4472 evaporate at a molar ratio of more than 2 (VC/N-4472) formed stable colloidal particles (with a mean particle size ≤100 nm) in aqueous solution. In particular, the evaporate prepared at the molar ratio of 5 (VC/N-4472) formed a clear solution comprising fine particles with a narrow particle size distribution of 8—15 nm. On the basis of surface tension measurement, zeta potential determination and static light scattering measurement, it was conceivable that both N-4472 and VC contributed to the formation of a surface-active complex in aqueous solution, while the colloidal particles could be interpreted as the self-association product of these complexes. According to the findings on 1H-NMR and attenuated total reflectance Fourier transform infrared spectra, it was postulated that upon combining both components at a molar ratio of 2 (VC/N-4472), a 1 : 1 association complex of N-4472 and VC was formed, whereas the higher order complexes were assumedly formed with use of a molar ratio of more than 2 (VC/N-4472). Furthermore, it was evidenced that all of these complexes were composed of amphiphilic structures comprising both hydrophobic N-4472 moiety and hydrophilic VC moiety, thereby properly accounting for surface-active property of these complexes.View full abstractDownload PDF (270K) -
Koji Yamada, Akiko Hamada, Fumiaki Kisa, Tomofumi Miyamoto, Ryuichi Hi ...Article type: Regular Article
Subject area: [not specified]
2003 Volume 51 Issue 1 Pages 46-52
Published: 2003
Released on J-STAGE: January 01, 2003
JOURNAL FREE ACCESSThree ganglioside molecular species, SCG-1, SCG-2, and SCG-3, were obtained from the lipid fraction of the chloroform–methanol extract of the sea cucumber Stichopus chloronotus. On the basis of chemical and spectroscopic evidence, the structures of these gangliosides have been determined to be 1-O-[(N-glycolyl-α-D-neuraminosyl)-(2→6)-β-D-glucopyranosyl]-ceramide (SCG-1), 1-O-[8-O-sulfo(major)-(N-acetyl-α-D-neuraminosyl)-(2→6)-β-D-glucopyranosyl]-ceramide (SCG-2), and 1-O-[α-L-fucopyranosyl-(1→11)-(N-glycolyl-α-D-neuraminosyl)-(2→6)-β-D-glucopyranosyl]-ceramide (SCG-3). The ceramide moieties were composed of heterogeneous long-chain base and fatty acid units. SCG-3 is the first type of ganglioside containing a fucopyranose in the sialosyl trisaccharide moiety. Moreover, these three gangliosides exhibited neuritogenic activity toward the rat pheochromocytoma PC12 cells in the presence of nerve growth factor.View full abstractDownload PDF (230K) -
Tatsuya Kitade, Hisashi Konda, Shigehiko Takegami, Kumiyo Ishii, Chika ...Article type: Regular Article
Subject area: [not specified]
2003 Volume 51 Issue 1 Pages 53-57
Published: 2003
Released on J-STAGE: January 01, 2003
JOURNAL FREE ACCESSAn easy and sensitive method for the quantitative determination of ofloxacin (OFLX), a new fluoroquinolone antimicrobial agent, in a pharmaceutical formulation, tablet, was developed by using solid-substrate room-temperature phosphorimetry (RTP) on a poly(vinyl alcohol) substrate. The method did not require a dry gas flush during the measurement of phosphorescence. The influence of different conditions such as solution pH and concentrations of heavy atoms, used as the enhancer, were studied. The phosphorescence intensity of OFLX was enhanced using NaOH and KI as enhancers. A linear relationship between concentration and RTP intensity for each standard solution was obtained in the concentration range of 4—18000 ng/ml, and the determination limit was 4 ng/ml. The proposed method was applied to a determination of OFLX in a commercial tablet, and the results were compared with those of fluorescence and UV methods. It was proven that OFLX in a commercial tablet can be accurately measured by this method with a very small amount of sample solution.View full abstractDownload PDF (811K) -
Hideyuki Shigemori, Toshinori Kagata, Haruaki Ishiyama, Frank Morah, A ...Article type: Regular Article
Subject area: [not specified]
2003 Volume 51 Issue 1 Pages 58-61
Published: 2003
Released on J-STAGE: January 01, 2003
JOURNAL FREE ACCESSFive new monoterpene indole alkaloids, naucleamides A—E (1—5), were isolated from the bark and wood of Nauclea latifolia, and the structures and relative stereochemistry were elucidated from the spectroscopic data. Naucleamide E (5) is a unique monoterpene indole alkaloid possessing a pentacyclic ring system with an amino acetal bridge.View full abstractDownload PDF (122K) -
Toshio Morikawa, Jing Tao, Kazuho Ueda, Hisashi Matsuda, Masayuki Yosh ...Article type: Regular Article
Subject area: [not specified]
2003 Volume 51 Issue 1 Pages 62-67
Published: 2003
Released on J-STAGE: January 01, 2003
JOURNAL FREE ACCESSFour new aromatic constituents, rhododendroketoside, (−)-sakuraresinoside, acernikol, and nikoenoside, were isolated from a Japanese folk medicine, the stem bark of Acer nikoense MAXIM. The structures of the new constituents were determined on the basis of chemical and physicochemical evidence. The principle cyclic diarylheptanoids were found to show inhibitory effects on the release of β-hexosaminidase in RBL-2H3 cells.View full abstractDownload PDF (252K) -
Nian-He Wang, Masahiko Taniguchi, Daisuke Tsuji, Mitsunobu Doi, Hirohu ...Article type: Regular Article
Subject area: [not specified]
2003 Volume 51 Issue 1 Pages 68-70
Published: 2003
Released on J-STAGE: January 01, 2003
JOURNAL FREE ACCESSFour new guaianolides, sinodielides A—D (1—4), were isolated from Sinodielsia yunnanensis WOLFF together with a known polyacetylene, falcarindiol, and two known coumarins, bergapten and scopoletin. Their structures were established by spectral and X-ray analyses.View full abstractDownload PDF (179K) -
Hirotaka Shibuya, Chinami Kitamura, Shoji Maehara, Marie Nagahata, Hen ...Article type: Regular Article
Subject area: [not specified]
2003 Volume 51 Issue 1 Pages 71-74
Published: 2003
Released on J-STAGE: January 01, 2003
JOURNAL FREE ACCESSThe microbial transformation of four Cinchona alkaloids (quinine, quinidine, cinchonidine, and cinchonine) by endophytic fungi isolated from Cinchona pubescens was investigated. The endophytic filamentous fungus Xylaria sp. was found to transform the Cinchona alkaloids into their 1-N-oxide derivatives.View full abstractDownload PDF (115K) -
Akikazu Kakehi, Suketaka Ito, Hiroyuki Suga, Takeyuki Miwa, Takashi Mo ...Article type: Regular Article
Subject area: [not specified]
2003 Volume 51 Issue 1 Pages 75-84
Published: 2003
Released on J-STAGE: January 01, 2003
JOURNAL FREE ACCESSVarious ethyl 1-arylcarbonyl-3-[(un)substituted methylthio]thieno[3,4-b]indolizine-9-carboxylates were synthesized in good yields by a novel methodology in which the S-alkylation of 5-arylcarbonyl-4-ethoxycarbonylmethyl-3-(1-pyridinio)thiophene-2-thiolates with alkyl or benzyl halides, the 1,5-dipolar cyclization of the resulting pyridinium salts in the presence of a base, and the aromatization were performed. In the X-ray analyses of some 3-(benzylthio)thieno[3,4-b]indolizine-9-carboxylates, a gauche and two anti conformers in relation to the exocyclic sulfide linkage were found. Interestingly, all of the 3-(benzylthio)thieno[3,4-b]indolizine derivatives showed significant high-field shifts (δ up to 0.3 ppm) for the 5- and 6-proton signals compared with those of the 3-methylthio derivatives in the 1H-NMR spectra and exhibited a definite absorption band near 425 nm in their UV spectra, indicating an intramolecular arene–arene interaction between the thieno[3,4-b]indolizine and the phenyl ring.View full abstractDownload PDF (404K) -
Ibrahim Iliya, Zulfiqar Ali, Toshiyuki Tanaka, Munekazu Iinuma, Miyuki ...Article type: Regular Article
Subject area: [not specified]
2003 Volume 51 Issue 1 Pages 85-88
Published: 2003
Released on J-STAGE: January 01, 2003
JOURNAL FREE ACCESSThree stilbene trimers (gnemonols D, E, F) were isolated from the root of Gnetum gnemon. The structures were determined by spectroscopic analysis. In addition, the antioxidant activity of the compounds on lipid peroxide inhibition and super oxide scavenging activity were also investigated.View full abstractDownload PDF (193K)
Notes
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Yoshitaka Toriumi, Rie Kakuda, Masafumi Kikuchi, Yasunori Yaoita, Masa ...Article type: Note
Subject area: [not specified]
2003 Volume 51 Issue 1 Pages 89-91
Published: 2003
Released on J-STAGE: January 01, 2003
JOURNAL FREE ACCESSThree new triterpenoids, 2,3-seco-3-oxours-12-en-2-oic acid, 2,3-seco-3-oxoolean-12-en-2-oic acid, and betulin 3-O-palmitate, have been isolated from the rhizomes and roots of Gentiana lutea, together with five known ones. The structures of the new compounds were determined by spectral and chemical methods.View full abstractDownload PDF (79K) -
Kazutomo Ori, Minpei Kuroda, Yoshihiro Mimaki, Hiroshi Sakagami, Yutak ...Article type: Note
Subject area: [not specified]
2003 Volume 51 Issue 1 Pages 92-95
Published: 2003
Released on J-STAGE: January 01, 2003
JOURNAL FREE ACCESSTen lanostane glycosides (1—10), including two new norlanostane glycosides (2 and 7) and a new lanostane glycoside with a spirolactone ring system (9), were isolated from the fresh bulbs of Chionodoxa luciliae (Liliaceae). The structures of the new compounds were determined on the basis of extensive spectroscopic analysis and the results of hydrolytic cleavage to be (23S)-3β-[(O-β-D-apiofuranosyl-(1→2)-O-[β-D-glucopyranosyl-(1→3)]-O-β-D-glucopyranosyl-(1→2)-α-L-arabinopyranosyl-(1→6)-β-D-glucopyranosyl)oxy]-17α,23-epoxy-28,29-dihydroxy-27-norlanost-8-en-24-one (2), (23S)-17α,23-epoxy-29-hydroxy-3β-[(O-α-L-rhamnopyranosyl-(1→2)-O-[O-β-D-glucopyranosyl-(1→2)-β-D-glucopyranosyl-(1→3)]-O-β-D-glucopyranosyl-(1→2)-α-L-arabinopyranosyl-(1→6)-β-D-glucopyranosyl)oxy]-27-norlanost-8-ene-15,24-dione (7), and (23S,25R)-17α,23-epoxy-29-hydroxy-3β-[(O-α-L-rhamnopyranosyl-(1→2)-O-[β-D-glucopyranosyl-(1→3)]-O-β-D-glucopyranosyl-(1→2)-α-L-arabinopyranosyl-(1→6)-β-D-glucopyranosyl)oxy]lanost-8-en-23,26-olide (9), respectively. The cytotoxic activity of the isolated compounds against HSC-2 human oral squamous cell carcinoma cells are also reported.View full abstractDownload PDF (107K) -
Yasushi Arakawa, Tomoaki Murakami, Yukimi Arakawa, Shigeyuki YoshifujiArticle type: Note
Subject area: [not specified]
2003 Volume 51 Issue 1 Pages 96-97
Published: 2003
Released on J-STAGE: January 01, 2003
JOURNAL FREE ACCESSElectrocyclic reaction product of 1-(methoxycarbonyl)-1,2-dihydropyridine was stereospecifically converted by RuO4 oxidation into azetidine-cis-2,3-dicarboxylic acid.View full abstractDownload PDF (68K) -
Vassilis John Demopoulos, Ioannis Nicolaou, Chariklia ZikaArticle type: Note
Subject area: [not specified]
2003 Volume 51 Issue 1 Pages 98-99
Published: 2003
Released on J-STAGE: January 01, 2003
JOURNAL FREE ACCESSAn effective synthesis of 1-(6-hydroxyindol-1-yl)-2,2-dimethylpropan-1-one (4) was developed starting from 1H-indole (2). The key step involved suitable utilization of 4-(1-pyrrolidino)pyridine for the removal of the chloroacetyl moiety from chloroacetic acid 1-(2,2-dimethylpropionyl)-1H-indol-6-yl ester (3); a possible mechanism is, also, presented. Compound 4 might lead to selectively substituted derivatives, either on the phenolic-OH or the indolyl-NH, with putative biological interest. In this respect, we found that the core structure of 1H-indol-6-ol (1) possesses a degree of aldose reductase inhibitory potential, at a concentration of 100 μM.View full abstractDownload PDF (67K) -
Hideto Miyabe, Akiyoshi Nishiki, Takeaki NaitoArticle type: Note
Subject area: [not specified]
2003 Volume 51 Issue 1 Pages 100-103
Published: 2003
Released on J-STAGE: January 01, 2003
JOURNAL FREE ACCESSThe stannyl radical mediated-cyclization of oxime ether, derived from D-glucose, gave the aminocyclohexitol derivative. Stereoselective C–C bond forming cyclization proceeded via favorable conformers minimizing A1,3-strain between the oxime ether group and α-substituents.View full abstractDownload PDF (215K)
Communicatins to the Editor
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Keisuke Hanada, Norio Miyazawa, Kunio OgasawaraArticle type: Communication to the Editor
Subject area: [not specified]
2003 Volume 51 Issue 1 Pages 104-106
Published: 2003
Released on J-STAGE: January 01, 2003
JOURNAL FREE ACCESSA new route to (+)-estrone has been developed starting from the chiral building block having a bicyclo[3.2.1]octane framework based on the inherent stereochemical chemical nature of the chiral building block.View full abstractDownload PDF (119K)
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