巻号一覧
50 巻, 9 号
選択された号の論文の35件中1～35を表示しています
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Regular Articles
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Changqi Sun, Hiroshi Kashiwagi, Masaharu Ueno原稿種別: Regular Article
専門分野: [not specified]
2002 年 50 巻 9 号 p. 1145-1150
発行日: 2002年
公開日: 2002/09/01
ジャーナル フリーThe effects of sub-solubilizing concentrations of sodium cholate (Na-chol) on several physicochemical properties of phosphatidylcholine (PC) small unilamellar vesicles (SUV) were considered in connection with the initial stage of membrane solubilization. ESR spectra of 12-doxylstearic acid (12-DS) in phosphatidylcholine from egg yolk (EPC) or dimyristoylphosphatidylcholine (DMPC) SUV at low concentrations (insufficient to destroy the vesicles) of Na-chol were composed of two (a strongly immobilized and an additional weakly immobilized) immiscible components. The origin of the additional bands was phase separation which occurred in the hydrophobic parts of PC SUV in the presence of Na-chol. Differential scanning calorimetry measurements demonstrated that the mixed DMPC/Na-chol SUV possessed two (a sharp low-temperature and a broad high-temperature) endothermic peaks, which is consistent with the coexistence of two immiscible phases in the vesicular membranes. ζ Potentials of the EPC/Na-chol SUV revealed that high anionic densities appeared on the surfaces of the SUV at a Na-chol concentration slightly below the upper boundary of the vesicle region. Thus, the initial stage of the solubilization of PC SUV by Na-chol was caused by the aggregation of hydrophobic parts of PC membranes, followed by the occurrence of high anionic densities on the surfaces of the vesicles. The fact that removal of Na-chol from PC/Na-chol mixed systems preferentially resulted in the formation of small vesicles might originate from these anionic charges.抄録全体を表示PDF形式でダウンロード (80K) -
Carmela Saturnino, Anna Capasso, Jean-Chanles Lancelot, Sylvain Rault, ...原稿種別: Regular Article
専門分野: [not specified]
2002 年 50 巻 9 号 p. 1151-1154
発行日: 2002年
公開日: 2002/09/01
ジャーナル フリーSeven morpholin derivatives were synthesized (compounds 1—7) and their behavioural effects were evaluated; the elements considered were locomotor activity, motor coordination, catalepsy, stereotyped behaviour and antinociception. All the compounds, at doses of 10—20—40 mg/kg/i.p., induced a reduction of all behavioural elements without a significant antinociceptive effect. These results indicate that these morpholin derivatives affect the central nervous system.抄録全体を表示PDF形式でダウンロード (69K) -
Miloud Rahmouni, Vincent Lenaerts, Danielle Massuelle, Eric Doelker, a ...原稿種別: Regular Article
専門分野: [not specified]
2002 年 50 巻 9 号 p. 1155-1162
発行日: 2002年
公開日: 2002/09/01
ジャーナル フリーCross-linked high amylose starch (CLA) is a pharmaceutical excipient used in direct compression for the preparation of controlled release tablets and implants. In this work the compression properties of CLA in bulk and granulated forms (without binder) were evaluated for the first time. Tablets were prepared on an instrumented single punch machine. The flow properties and the compression characteristics (compressibility, densification behavior, work of compression) of the materials as well as the mechanical strength of the finished compacts (compactibility) were systematically examined. Wet granulation was found to improve the flowability and the compressibility of CLA but concomitantly reduced its compactibility. It was demonstrated that CLA was a plastically deforming material with a plasticity index and a yield pressure value comparable to those of pregelatinized starch. The compactibility of granulated CLA was independent of particle size in the range of 75 to 500 μm, but slightly decreased when the percentage of the fine particles (<75 μm) in the bulk powder was increased. Water and colloidal silicone dioxide facilitated the consolidation of CLA, while magnesium stearate had an opposite effect on the tablet crushing force.抄録全体を表示PDF形式でダウンロード (134K) -
Hirokazu Suzuki, Manabu Yamamoto, Susumu Shimura, Ken-ichi Miyamoto, K ...原稿種別: Regular Article
専門分野: [not specified]
2002 年 50 巻 9 号 p. 1163-1168
発行日: 2002年
公開日: 2002/09/01
ジャーナル フリーTo reverse the adverse reactions of alkylxanthines and to develop novel inhibitors of cyclic AMP phosphodiesterase 4 (PDE4), a series of heterocycle [a]-, [b]-, [c,d]-, and [i]-condensed purines were designed and synthesized. Although all compounds did not display PDE1 and PDE3 inhibitory activities, several heterocycle [i]-condensed purines strongly inhibited PDE4. Especially, dl-3,4-dipropyl-8-methyl-4,5,7,8-tetrahydro-1H-imidazo[2,1-i]purin-5-one (dl-7c) exhibited comparable PDE4 inhibitory activity (IC50=1.9 μM) to rolipram and denbufylline (DBF).抄録全体を表示PDF形式でダウンロード (82K) -
Norihito Shimono, Masumi Ueda, Yasuhiko Nakamura原稿種別: Regular Article
専門分野: [not specified]
2002 年 50 巻 9 号 p. 1169-1175
発行日: 2002年
公開日: 2002/09/01
ジャーナル フリーPellets containing active ingredients were coated with water-insoluble powders, i.e. hydrogenated caster oil (Lubliwax (WAX)) and magnesium stearate (Mg-St). The influences of the structural difference of the sustained release layer and curing conditions on the drug release rate were investigated. Sodium valproate (VP-Na) was used as a highly water-soluble model drug. Drug release profiles were influenced by the combination of the WAX layer and the Mg-St layer. Even if the formula of sustained release layers were the same, drug release rate could be affected by the structural difference of the controlled release layer. The Mg-St layer was more effective in prolonging drug release than the WAX layer. Compared with single and double layer types, the triple layer (sandwich) type was most effective in obtaining a long sustained drug release. Heat-treatment retarded drug release mainly by increasing the density of the sustained release layer of the WAX. The Mg-St was effective in protecting the agglomeration between particles during heat-treatment. Optimal heat-treatment conditions were found to exist. Scanning electron microscopy (SEM) analysis indicated that heat-treatment caused the WAX to melt, formed a film-like structure and made the release layer dense. Furthermore, heat-treatment changed the release pattern of VP-Na from sustained release pellets with a multi-layer of powder, leading to zero-order release.抄録全体を表示PDF形式でダウンロード (159K) -
Noriko Katori, Nobuo Aoyagi, Shigeo Kojima原稿種別: Regular Article
専門分野: [not specified]
2002 年 50 巻 9 号 p. 1176-1180
発行日: 2002年
公開日: 2002/09/01
ジャーナル フリーThe mass variation test is a simplified alternative test version of the content uniformity test. In the case of coating tablets and capsules, the mass variation test is principally applied to test the inner cores or fillings containing the active ingredient. However, some exceptions exist in pharmacopoeias. The effects of tablet coating and capsule shell on the results of the mass variation test were studied. The mass variation of outer crusts (coatings, capsule shells) and inner cores (core tablets, fillings) was measured separately in several products. The effects of coating on weight variability were very large for sugar-coated tablets. Relative standard deviation (RSD) of the formulation weight (RSDW) of sugar-coated tablets (2.73%) was larger than that of plain tablets (0.77%). The cause of the large RSDW is the large variation the weight of sugar-coating accounting for 44% of formulation weight. In the case of film-coated tablets, the effect of coating weight on the mass variation test was very small because the rate of coating in comparison to the whole weight was small. In the case of hard capsules, the usage of whole formulation weight resulted in underestimation of variations of filling weight. The differences between dosage forms in the applicability of the mass variation test are caused by differing weight proportions and variability of the outer coatings or shells. To avoid the underestimation of mass variation for hard capsules, a corrected acceptance value is useful. For all the dosage units, the mass variation test can principally be applied to determine which mass is expected to be proportional to the content of the active ingredient. However, some modification of acceptance values enables application of the mass variation tests to inapplicable cases, such as when the RSD of drug concentration (RSDC) is larger than 2%.抄録全体を表示PDF形式でダウンロード (66K) -
Yutaka Morita, Yuki Tsushima, Masanobu Yasui, Ryoji Termoz, Junko Ajio ...原稿種別: Regular Article
専門分野: [not specified]
2002 年 50 巻 9 号 p. 1181-1186
発行日: 2002年
公開日: 2002/09/01
ジャーナル フリーMany kinds of rapidly disintegrating or oral disintegrating tablets (RDT) have been developed to improve the ease of tablet administration, especially for elderly and pediatric patients. In these cases, knowledge regarding disintegration behavior appears important with respect to the development of such a novel tablet. Ordinary disintegration testing, such as the Japanese Pharmacopoeia (JP) method, faces limitations with respect to the evaluation of rapid disintegration due to strong agitation. Therefore, we have developed a novel apparatus and method to determine the dissolution of the RDT. The novel device consists of a disintegrating bath and CCD camera interfaced with a personal computer equipped with motion capture and image analysis software. A newly developed RDT containing various types of binder was evaluated with this protocol. In this method, disintegration occurs in a mildly agitated medium, which allows differentiation of minor distinctions among RDTs of different formulations. Simultaneously, we were also able to detect qualitative information, i.e., morphological changes in the tablet during disintegration. This method is useful for the evaluation of the disintegration of RDT during pharmaceutical development, and also for quality control during production.抄録全体を表示PDF形式でダウンロード (118K) -
Hidemitsu Nishida, Yutaka Miyazaki, Takafumi Mukaihira, Fumihiko Saito ...原稿種別: Regular Article
専門分野: [not specified]
2002 年 50 巻 9 号 p. 1187-1194
発行日: 2002年
公開日: 2002/09/01
ジャーナル フリーIntravascular clot formation is an important event in a number of cardiovascular diseases. The prevention of blood coagulation has become a major target for new therapeutic agents. Factor Xa (FXa) is a trypsin-like serine protease that plays a key role in the blood coagulation cascade and represents an attractive target for anticoagulant drug development. We have investigated substituents in the central part of a lead compound (3: M55113), and discovered that compound M55551 (34: (R)-4-[(6-Chloro-2-naphthalenyl)sulfonyl]-6-oxo-1-[[1-(4-pyridinyl)-4-piperidinyl]methyl]-2-piperazinecarboxylic acid) is a potent inhibitor of FXa (IC50=0.006 μM), with high selectivity for FXa over trypsin and thrombin. The activity of this compound is ten times more powerful than the lead compound.抄録全体を表示PDF形式でダウンロード (101K) -
Chao-feng Zhang, Norio Nakamura, Supinya Tewtrakul, Masao Hattori, Qi- ...原稿種別: Regular Article
専門分野: [not specified]
2002 年 50 巻 9 号 p. 1195-1200
発行日: 2002年
公開日: 2002/09/01
ジャーナル フリーThree new eudesmane type sesquiterpenoid lindenanolides E (1), F (2) and G (3), and two new aporphine alkaloid lindechunines A (18) and B (20) were isolated from roots of Lindera chunii MERR., together with seven known sesquiterpenes including a new naturally-occurring lindenanolide H (4) and eight known aporphine alkaloids. The structures of these compounds were determined by spectroscopic means. Of the isolated compounds, hernandonine (14), laurolistine (16), 7-oxohernangerine (17) and lindechunine A (18) showed significant anti-human immunodeficiency virus type 1 (HIV-1) integrase activity with IC50 values of 16.3, 7.7, 18.2 and 21.1 μM, respectively. The major alkaloids presented in the roots of L. chunii were quantitatively analyzed by an HPLC method.抄録全体を表示PDF形式でダウンロード (91K) -
Eva Díez-Peña, Gloria Frutos, Paloma Frutos, José ...原稿種別: Regular Article
専門分野: [not specified]
2002 年 50 巻 9 号 p. 1201-1208
発行日: 2002年
公開日: 2002/09/01
ジャーナル フリーThe purpose of the present work was the study of the gentamicin sulphate (GS) release from a commercial acrylic bone cement CMW-1® with the aims of establishing the influence of the slabs preparation as well as the release mechanism and kinetics. The effect of the amount of GS on the release kinetic parameters has been also investigated. In vitro release studies were performed in a buffered saline solution at pH 7.4 and 37 °C. The GS concentration was determined using an indirect spectrophotometric method with an o-phthaldialdehyde as a derivatizing reagent. A commercial and three modified samples were tested. The free and fractured surfaces of the GS cement slabs before and after the release studies were observed by means of scanning electron microscopy (SEM). For low GS concentration loading the release was very incomplete because most of the GS beads were encapsulated by the hydrophobic PMMA matrix. A higher amount of antibiotic was released from cement that has a higher amount incorporated. A model and therefore a mechanism of release based on this model have been proposed. It has allowed us to explain the changes in dissolution kinetics of an acrylic matrix type controlled release system up to 12% GS loading. The cumulative amount of GS released Mt/Mi, was fitted as a function of time. For lower amounts of GS, the regression analysis (R2>0.99) revealed that the release is most adequately represented by Mt/Mi=b+ktn, where b represents a burst effect. The goodness of fit decreases as the amount of GS increases. The influence of some other type of release mechanism for higher amounts of GS must be taken into account and a second model for the release, Mt/Mi=b+k·[1−exp(−kt)], is proposed.抄録全体を表示PDF形式でダウンロード (584K) -
Hiroyuki Nojima, Mayuko Takeda-Shitaka, Youji Kurihara, Masaaki Adachi ...原稿種別: Regular Article
専門分野: [not specified]
2002 年 50 巻 9 号 p. 1209-1214
発行日: 2002年
公開日: 2002/09/01
ジャーナル フリーClass I major histocompatibility complex (MHC) binds antigen peptides with various sequences. We performed a normal mode analysis of HLA-A2 MHC that binds three peptides with different affinity. HLA-A2 MHC has a peptide-binding groove composed of two α-helices (residue 49—84, residue 140—179). Some residues in the center of the groove showed an increase in fluctuations and some residue pairs between two helix groups showed a negative change in correlations by removing the antigen peptide. The extent of the fluctuation and correlation changes correlated well with the experimental ranking of the three peptides in binding affinity. Some definite anti-correlative motions were found between two helix groups in low frequency modes (<50 cm−1) by removing the antigen peptide. We propose that the above anti-correlative motions play an important role to bind the antigen peptide, especially in obtaining a “dynamic fit.”抄録全体を表示PDF形式でダウンロード (245K) -
Jaime A. Valderrama, Claudio Astudillo, Ricardo A. Tapia, Eric Prina, ...原稿種別: Regular Article
専門分野: [not specified]
2002 年 50 巻 9 号 p. 1215-1218
発行日: 2002年
公開日: 2002/09/01
ジャーナル フリーThe synthesis of 3-amino-2-methoxycarbonyl-4,7-dimethoxybenzo[b]thiophene (5) and benzothieno[3,2-d][1,3]oxazin 15 from 3,6-dimethoxy-2-nitrobenzaldehyde (1) is reported. Benzo[b]thiophene-4,7-quinones 9 and 10 were prepared in good yields by oxidative deprotection of the corresponding dimethoxybenzothiophenes 8 and 7. Cycloaddition reaction of quinone 8 with 1-(E)-trimethylsilyloxy-1,3-butadiene followed by acid-induced aromatization provides access to naphtho[2,3-b]thiophene-4,9-quinone 13 and 14. The in vitro activity of the new quinones against Leishmania amazonensis and human-T-cell leukemia virus type 1 (HTLV-1) is reported.抄録全体を表示PDF形式でダウンロード (60K) -
Yorinobu Yonezawa, Sumio Ishida, Shinobu Suzuki, Hisakazu Sunada原稿種別: Regular Article
専門分野: [not specified]
2002 年 50 巻 9 号 p. 1219-1222
発行日: 2002年
公開日: 2002/09/01
ジャーナル フリーGeneralization of the release process through the wax matrix layer was examined by use of a reservoir device tablet. The wax matrix layer of the reservoir device tablet was prepared from a physical mixture of lactose and hydrogenated castor oil to simplify the release properties. Release through the wax matrix layer showed zero-order kinetics in a steady state after a given lag time, and could be divided into two stages. The first stage was the formation process of water channel by dissolving the soluble component in the wax matrix layer. The lag time obtained by applying the square root law equation was well connected with the amount of the matrix layer and mixed weight ratio of components in this layer. The second stage was the zero-order release process of drug in the reservoir through the wax matrix layer, because the effective surface area was fixed. The release rate constants were connected with thickness of the matrix layer and permeability coefficient, and the permeability coefficients were connected with the diffusion coefficient of drug and porosity. Hence the release rate constant could be connected with the amount of matrix layer and the mixed weight ratio of components in the matrix layer. It was therefore suggested that the release process could be generalized using the amount of matrix layer and the mixed weight ratio of components in the matrix layer.抄録全体を表示PDF形式でダウンロード (55K) -
Jaskiran Kaur, Narendra Nath Ghosh, Anita Talwar, Ramesh Chandra原稿種別: Regular Article
専門分野: [not specified]
2002 年 50 巻 9 号 p. 1223-1228
発行日: 2002年
公開日: 2002/09/01
ジャーナル フリーThe synthesis and structure–activity-relationship (SAR) for a series of N-substituted piperazinyl carbamoyl 7—15 and piperazinyl acetyl 18—26 derivatives of tetrahydropapaverine have been carried out. The general synthetic methods of carbamoyl tetrahydropapaverine analogues involve N-substituted piperazines and carbamoyl imidazole tetrahydropapaverine as starting materials. Another route for synthesizing these compounds, involving the formation of carbamoyl imidazole piperazine has also been explored. Acylation of tetrahydropapaverine followed by substitution with various piperazinyl moities afforded the acetyl tetrahydropapaverine derivatives. Variously substituted piperazines have been used to monitor the effect of electron releasing and electron withdrawing substituents upon the antispasmodic activity of the molecules. Effect of varying electron densities on the antispasmodic activity, by altering the position of these groups on the benzene ring has also been monitored. Pharmacological methods involve the in vitro antispasmodic activity studies on a freshly removed guinea pig ileum using a force displacement transducer amplifier connected to a physiograph. Among the analogues synthesized in the present study, a promising compound 7, a potent muscle relaxant as compared to papaverine has been obtained.抄録全体を表示PDF形式でダウンロード (73K) -
Yuichi Susuki, Keiko Hojo, Ikuko Okazaki, Haruhiko Kamata, Masahiko Sa ...原稿種別: Regular Article
専門分野: [not specified]
2002 年 50 巻 9 号 p. 1229-1232
発行日: 2002年
公開日: 2002/09/01
ジャーナル フリーA bivalent poly(ethylene glycol) or PEG hybrid of fibronectin-related peptides was prepared. An active site peptide (RGD) and its synergistic site peptide (PHSRN) of fibronectin were conjugated with an amino acid-type PEG (aaPEG) to form PHSRN–aaPEG–RGD. A moderate spatial array between RGD and PHSRN in fibronectin may be required for synergic activity. The bivalent hybrid exhibited potent cell spreading activity and exhibited potent anti-metastatic activity in a model of experimental metastasis with B16–BL6 cells in mice. PEG may serve as a spacer for maintaining the desired spatial array.抄録全体を表示PDF形式でダウンロード (63K) -
Ju-Xiu He, Teruaki Akao, Tadato Tani原稿種別: Regular Article
専門分野: [not specified]
2002 年 50 巻 9 号 p. 1233-1237
発行日: 2002年
公開日: 2002/09/01
ジャーナル フリーA simple and reproducible HPLC method for the determination of paeoniflorin (PF)-metabolizing activity of intestinal bacteria in rat feces was developed and validated. Orally administered PF, a major active constituent of Paeoniae Radix, is metabolized into a bioactive compound, paeonimetabolin I (PM-I) by intestinal bacteria. Direct determination of the PF-metabolizing rate into PM-I is hard to achieve by HPLC due to the lack of intense chromophore in PM-I. However, when PF was incubated with Lactobacillus brevis, an intestinal bacterium, in the presence of phenylmercaptan, the metabolizing rate of PF into 8-phenylthio-paeonimetabolin I (PT-PM-I) was found to be equivalent to that of PF into PM-I. Thus, the PF-metabolizing activity of intestinal bacteria in rat feces was determined by measuring the rate of biotransformation of PF into PT-PM-I, which was detected by HPLC at 255 nm. This method can be utilized in the biopharmaceutical study of traditional Chinese formulations containing Paeoniae Radix.抄録全体を表示PDF形式でダウンロード (79K) -
Supaporn Sriwongsitanont, Masaharu Ueno原稿種別: Regular Article
専門分野: [not specified]
2002 年 50 巻 9 号 p. 1238-1244
発行日: 2002年
公開日: 2002/09/01
ジャーナル フリーEgg phosphatidylcholine (EggPC) or dimyristoylphosphatidylcholine (DMPC) liposomes containing polyethylene glycol (PEG)-lipids covering a range of 0—30 mol% have been prepared by Extrusion method. The physicochemical properties including size evolution and calcein permeation were evaluated to investigate the effect of PEG-lipids on bilayer structure. The results from quasielasetic light scattering (QELS), freeze-fracture microscopy, and gel exclusion chromatography revealed that presence of low concentration of PEG-lipid results in decreasing of vesicle size and further increase in the PEG-lipid concentrations lead to a transition from the lamellar membranes to micelles. The permeability for calcein increased with increase in concentration of distearoylphosphatidylethanolamine (DSPE)-PEG. On the other hand, the permeability decreased with low amount of cholesterol-PEG (blow 20% cholesterol-PEG) and increased with high amount of it. The maximum concentration of PEG-lipid that may be incorporated without alteration of the liposome structure depends on the composition of the bilayer. The concentration of DSPE-PEG2000 incorporated into vesicles without damaging vesicle structures were <20 mol% for EggPC and <10% for DMPC.抄録全体を表示PDF形式でダウンロード (855K) -
Sang-Myung Lee, Hyo-Kon Chun, Choong-Hwan Lee, Byung-Sun Min, Eun-Sook ...原稿種別: Regular Article
専門分野: [not specified]
2002 年 50 巻 9 号 p. 1245-1249
発行日: 2002年
公開日: 2002/09/01
ジャーナル フリーTwo new eucosterol oligoglycosides, 15-deoxo-30-hydroxyeucosterol 3-O-α-L-rhamnopyranosyl-(1→2)-[(β-D-glucopyranosyl-(1→3)]-β-D-glucopyranosyl-(1→2)-α-L-arabinopyranosyl-(1→6)-β-D-glucopyranoside (scillanoside L-1, 1) and 3β,31-dihydroxy-17α,23-epoxy-5α-lanost-8-en-23,26-olactone 3-O-α-L-rhamnopyranosyl-(1→2)-[β-D-glucopyranosyl-(1→3)]-β-D-glucopyranosyl-(1→2)-α-L-arabinopyranosyl-(1→6)-β-D-glucopyranoside (scillanoside L-2, 2), were isolated from the bulbs of Scilla scilloides, together with four that were known (3—6), have been isolated from the bulbs of Scilla scilloides. The structures of the new compounds were determined on the basis of spectroscopic and chromatographic methods, and some chemical transformations were discussed. Amongst the isolated compounds, 3 showed the most significant cytotoxicity against tumor cells tested several types with ED50 value of 1.53—3.06 nM. In vivo experiments, 3 apparently increased the life span of mice bearing Sarcoma 180 tumor cell with T/C value of 239% at dose of 3 mg/kg.抄録全体を表示PDF形式でダウンロード (64K) -
Motoo Tori, Yoshiko Takeichi, Hiroe Kuga, Katsuyuki Nakashima, Masakaz ...原稿種別: Regular Article
専門分野: [not specified]
2002 年 50 巻 9 号 p. 1250-1254
発行日: 2002年
公開日: 2002/09/01
ジャーナル フリーFour new germacrane-type sesquiterpenoids with unsaturated acids as esters at the 8-position, two chlorine atom-containing lactones, 2α-acetoxyepitulipinolide, and 12 previously known compounds have been isolated from the MeOH extract of Eupatorium glehni (Compositae) and their structures have been determined on the basis of spectral data analyses.抄録全体を表示PDF形式でダウンロード (68K) -
Masashige Yamauchi, Kazuhiro Itai, Yuko Honda原稿種別: Regular Article
専門分野: [not specified]
2002 年 50 巻 9 号 p. 1255-1257
発行日: 2002年
公開日: 2002/09/01
ジャーナル フリーThe enantioselective Lewis acid-catalyzed Diels–Alder reaction of 3-(2-propenoyl)-1,3-oxazolidin-2-one 8 with cyclopentadiene was examined using a series of chiral mox ligands 2—6, deferring in the side chain at 2-position of the chiral oxazoline and in the nature of the substituent at the chiral center (4-position) of the oxazoline ring, and a combination of N-[(1R)-2-chloro-1-phenylethyl]-2-[(4R)-4-phenyl-4,5-dihydrooxazol-2-yl]butyramide 2–MgI2–I2 was the most efficient catalyst.抄録全体を表示PDF形式でダウンロード (56K) -
Satoru Watano, Tomohiro Hamashita, Teruo Suzuki原稿種別: Regular Article
専門分野: [not specified]
2002 年 50 巻 9 号 p. 1258-1261
発行日: 2002年
公開日: 2002/09/01
ジャーナル フリーA novel fine particle removal system composed of a corona-discharge neutralizer, a pulse-jet air unit and an image processing system has been developed. First of all, adhesion force between particle and film was directly measured and effect of electrostatic force on the adhesion force was calculated experimentally and theoretically. The electrostatic force was found to be significant, leading to the suggestion that the countermeasure for the electrostatic force was required to effectively remove fine particles. This system was then applied to the removal of fine particles from surface of a gelatin film used for conventional capsule material. The number of particles removed by the system was calculated by an image processing system and number base removal efficiency was computed with and without the elimination of electrostatic charge by the neutralizer. It was found that the difference between the removal efficiency of particles with elimination of electrostatic charge and that of without the elimination showed linear relationship with the electrostatic adhesion force. The data confirmed the necessity of electrostatic charge elimination for the effective removal of fine particles.抄録全体を表示PDF形式でダウンロード (62K) -
Satoru Watano, Takumi Okamoto, Teruo Suzuki原稿種別: Regular Article
専門分野: [not specified]
2002 年 50 巻 9 号 p. 1262-1264
発行日: 2002年
公開日: 2002/09/01
ジャーナル フリーIn the previous paper, a novel fine particle removal system composed of a corona-discharge neutralizer, a pulse-jet air unit and an image processing system has been developed and applied to the removal of fine particles from film surface. We have calculated the van der Waals and electrostatic forces between particle and film and then reported that the electrostatic force influenced the adhesion characteristics significantly and thus the elimination of electrostatic charge should be necessary for the effective removal of fine particles. In this paper, we have modified the corona-discharge neutralizer for getting much better removal performance. The effect of operating parameters on the removal efficiency was investigated experimentally. The ratio of fine particle remained on the film surface after removal experiment as a function of particle size was measured. It was found that fine particles smaller than 15 μm, which were impossible to remove by other conventional techniques, could be almost completely removed. This method is anticipated to be used in the capsule filling, film packaging and tabletting processes for prevention of stain on lens of video automatic inspection machines, unpredictable movement of electronic devices, and deteriorates of product quality.抄録全体を表示PDF形式でダウンロード (69K)
Notes
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Xiang-Li Shen, Xian-Li Zhou, Qiao-Hong Chen, Dong-Lin Chen, Feng-Peng ...原稿種別: Note
専門分野: [not specified]
2002 年 50 巻 9 号 p. 1265-1267
発行日: 2002年
公開日: 2002/09/01
ジャーナル フリーFrom the roots of Delphinium potaninii var. jiufengshanense, two new lycoctonine-type C19-diterpenoid alkaloids called jiufengdine (1) and jiufengtine (4) have been isolated. The structures of the new alkaloids (1, 4) were established by 1D and 2D NMR spectra.抄録全体を表示PDF形式でダウンロード (47K) -
Hichem Ben Salah, Raoudha Jarraya, Marie-Thérèse Martin, ...原稿種別: Note
専門分野: [not specified]
2002 年 50 巻 9 号 p. 1268-1270
発行日: 2002年
公開日: 2002/09/01
ジャーナル フリーA new flavonol triglycoside, isorhamnetin 3-O-β-D-xylopyranosyl-(1″″→3)-α-L-rhamnopyranosyl-(1→6″)-β-D-galactopyranoside, has been isolated from the leaves of Hammada scoparia together with two known compounds, isorhamnetin 3-O-β-D-apiofuranosyl-(1→2″)[α-L-rhamnopyranosyl-(1″″→6″)]-β-D-galactopyranoside and isorhamnetin 3-O-α-L-rhamnopyranosyl-(1→2″)[α-L-rhamnopyranosyl-(1″″→6″)]-β-D-galactopyranoside. The structures were determined by spectroscopic methods.抄録全体を表示PDF形式でダウンロード (55K) -
Yerra Koteswara Rao, Mopur Vijaya Bhaskar Reddy, Chunduri Venkata Rao, ...原稿種別: Note
専門分野: [not specified]
2002 年 50 巻 9 号 p. 1271-1272
発行日: 2002年
公開日: 2002/09/01
ジャーナル フリーTwo new 5-deoxyflavones, 7,8-dimethoxy-3′,4′-methylenedioxyflavone (1) and 7,2′,4′-trimethoxyflavone (2) together with a known flavone, 7,4′-dimethoxy-3′-hydroxyflavone (3) were isolated from the rootbark of Albizia odoratissima. The structures of these new compounds were elucidated by electrospray ionization mass spectrometry (ESI-MS) and 1D and 2D-NMR spectral studies including 1H–1H correlation spectroscopy (COSY), heteronuclear single quantum coherence (HSQC), heteronuclear multiple bond connectivity (HMBC) and nuclear Overhauser enhancement spectroscopy (NOESY).抄録全体を表示PDF形式でダウンロード (49K) -
Takahisa Nakane, Yoshiko Maeda, Hideharu Ebihara, Yoko Arai, Kazuo Mas ...原稿種別: Note
専門分野: [not specified]
2002 年 50 巻 9 号 p. 1273-1275
発行日: 2002年
公開日: 2002/09/01
ジャーナル フリーTwo new migrated hopane triterpenoids, viz. 4α-hydroxyfilican-3-one and fern-9(11)-en-12β-ol, and olean-18-en-3-one and olean-12-en-3-one as the first example of oleanane compounds from Adiantum ferns were isolated along with many other known triterpenoids from Adiantum capillus-veneris of China and Egypt. Their structures were elucidated by spectroscopic analyses.抄録全体を表示PDF形式でダウンロード (53K) -
Hideo Kitagawa, Teruaki Mukaiyama原稿種別: Note
専門分野: [not specified]
2002 年 50 巻 9 号 p. 1276-1279
発行日: 2002年
公開日: 2002/09/01
ジャーナル フリーN-tert-Butylbenzenesulfenamide (1) catalyzed oxidation of various alcohols with stoichiometric amount of anhydrous chloramines-T (2) proceeded smoothly at room temperature to afford the corresponding carbonyl compounds in good yields.抄録全体を表示PDF形式でダウンロード (57K) -
Shinichi Uesato, Yuichiro Hashimoto, Masaru Nishino, Yasuo Nagaoka, Hi ...原稿種別: Note
専門分野: [not specified]
2002 年 50 巻 9 号 p. 1280-1282
発行日: 2002年
公開日: 2002/09/01
ジャーナル フリーIn order to seek a urease inhibitor more potent than hydroxyurea (1), its alkyl- or phenyl-substituted derivatives were synthesized and evaluated for their effect on the jack bean urease. Of 16 compounds tested, m-methyl- (10) and m-methoxy-phenyl substituted hydroxyurea (13) showed the most potent inhibitory activities against the enzyme.抄録全体を表示PDF形式でダウンロード (50K) -
Koichi Goto, Kentaro Nakashima, Osamu Tanoue, Satoshi Nukushina, Isao ...原稿種別: Note
専門分野: [not specified]
2002 年 50 巻 9 号 p. 1283-1285
発行日: 2002年
公開日: 2002/09/01
ジャーナル フリーWith respect to the hydrolysis (deacylation) of Z-D(L)-amino acid esters (N-(benzyloxycarbonyl)-D(L)-amino acid p-nitrophenyl esters) mediated by α-, β- and γ-cyclodextrins (CyDs), a remarkably high enantioselectivity (L/D=9.0) was observed for the deacylation of Ala substrate with γ-CyD. The kinetic results on the basis of the Michaelis–Menten principle indicate that the enantioselectivity should be mainly originated in the deacylation process of substrates following the formation of γ-CyD–substrate (1 : 1) complexes. The computer modeling (molecular mechanics) studies on the inclusion complexes are also described.抄録全体を表示PDF形式でダウンロード (57K) -
Makoto Iwashima, Ikuo Terada, Kazuo Iguchi, Takao Yamori原稿種別: Note
専門分野: [not specified]
2002 年 50 巻 9 号 p. 1286-1289
発行日: 2002年
公開日: 2002/09/01
ジャーナル フリーA new bisabolane-type sesquiterpenoid, (E)-3-isocyanobisabolane-7,10-diene (1), and a new epidioxyergostane-type steroid, 9(11)-dehydroaxinysterol (2), were isolated from the Okinawan sponge of the genus Axinyssa. Their structures were elucidated based on the results of spectroscopic analysis and chemical conversion. Epidioxysterol 2 was found to show significant growth inhibitory effects against human cancer cell lines.抄録全体を表示PDF形式でダウンロード (62K) -
Liva Harinantenaina, Ryoji Kasai, Kazuo Yamasaki原稿種別: Note
専門分野: [not specified]
2002 年 50 巻 9 号 p. 1290-1293
発行日: 2002年
公開日: 2002/09/01
ジャーナル フリーFive new triterpene saponins, cussosaponins A (2), B (3), C (4), D (5), and E (6), were isolated from the dried leaves of Cussonia racemosa BAKER. The structures of these new compounds were deduced on the basis of chemical and spectroscopic evidence.抄録全体を表示PDF形式でダウンロード (58K) -
Young Hae Choi, Ki-Pung Yoo, Jinwoong Kim原稿種別: Note
専門分野: [not specified]
2002 年 50 巻 9 号 p. 1294-1296
発行日: 2002年
公開日: 2002/09/01
ジャーナル フリーSupercritical fluid extraction using carbon dioxide modified with methanol, methanol–diethylamine, or methanol–triethylamine was used to extract vinblastine from the aerial portions of Catharanthus roseus. An HPLC-electrospray ionization (ESI)/MS analysis method was also developed to quantify the alkaloids in these extracts. Of the supercritical solvents evaluated, carbon dioxide–methanol–triethylamine (80 : 18 : 2) at 80 °C and 34.0 MPa greatly improved the supercritical fluid extraction (SFE) yield of vinblastine by as much as 76.4% over methanol extraction, while the other solvent conditions extracted the compound at yields less than 25% that of a methanol extraction. These results were confirmed by the robust HPLC-ESI/MS analytical method developed in this study.抄録全体を表示PDF形式でダウンロード (49K) -
Safdar Hayat, Atta-ur-Rahman, Muhammad Iqbal Choudhary, Khalid Mohamme ...原稿種別: Note
専門分野: [not specified]
2002 年 50 巻 9 号 p. 1297-1299
発行日: 2002年
公開日: 2002/09/01
ジャーナル フリーTwo new natural products, n-butyl and isopropyl 3,5-dimethoxy-4-hydroxycinnamate were isolated from Spatoglossum variabile. Three known compounds, methyl 3,4,5-trihydroxybenzoate, 2-deoxyinosine and 9-β-(D-ribofuranosyl)adenine were isolated for the first time from the methanolic extracts of this alga. The structure elucidations of the new compounds were carried out with the help of modern spectroscopic techniques.抄録全体を表示PDF形式でダウンロード (51K) -
Shigeki Sano, Tomoka Takehisa, Shiho Ogawa, Kenji Yokoyama, Yoshimitsu ...原稿種別: Note
専門分野: [not specified]
2002 年 50 巻 9 号 p. 1300-1302
発行日: 2002年
公開日: 2002/09/01
ジャーナル フリーTetrasubstituted (Z)-alkenes were readily prepared through the Horner–Wadsworth–Emmons reactions of methyl 2-[bis(2,2,2-trifluoroethyl)phosphono]propionate with aryl alkyl ketones by employing Sn(OSO2CF3)2 and N-ethylpiperidine.抄録全体を表示PDF形式でダウンロード (56K)
Communicatins to the Editor
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Hiromitsu Takayama, Tomotake Ichikawa, Mariko Kitajima, Maribel G. Non ...原稿種別: Communication to the Editor
専門分野: [not specified]
2002 年 50 巻 9 号 p. 1303-1304
発行日: 2002年
公開日: 2002/09/01
ジャーナル フリーTwo new pyrrolidine alkaloids, pandamarilactonine-C and -D, were isolated from Pandanus amaryllifolius. Based on the total synthesis of pandamarilactonine-C and its related alkaloid, pandamarilactonine-A, the relative stereochemistry of pandamarilactonine-A and -B, which was previously proposed by spectroscopic analysis, was revised.抄録全体を表示PDF形式でダウンロード (48K)
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