Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
54 巻, 2 号
選択された号の論文の31件中1~31を表示しています
Regular Articles
  • Pittaya Tuntiwachwuttikul, Photchana Phansa, Yupa Pootaeng-on, Walter ...
    2006 年 54 巻 2 号 p. 149-151
    発行日: 2006年
    公開日: 2006/02/01
    ジャーナル フリー
    Sixteen compounds were isolated from the fresh roots of Piper sarmentosum. Seven of these have been previously isolated from the fruits and leaves of this plant: the aromatic alkene (1), 1-allyl-2-methoxy-4,5-methylenedioxybenzene (4), β-sitosterol, pyrrole amide (6), sarmentine (10), sarmentosine (13) and pellitorine (14). (+)-Sesamin (2), horsfieldin (3), two pyrrolidine amides 11 and 12, guineensine (15) and brachystamide B (16) are new for P. sarmentosum. Sarmentamide A, B, and C (7—9) are new natural products. Compounds 1—4 and 6—16 were tested for antiplasmodial, antimycobacterial and antifungal activities.
  • Abou El-Hamd H. Mohamed, Ahmed A. Ahmed, Eckhard Wollenweber, Bruce Bo ...
    2006 年 54 巻 2 号 p. 152-155
    発行日: 2006年
    公開日: 2006/02/01
    ジャーナル フリー
    Investigation of lipophilic exudates from the aerial parts of Balsamorhiza sagittata and B. macrophylla afforded three new highly oxygenated guaianolides (1—3), in addition to known guaianolides, germacranolide and eudesmane acids. Their chemical structures were elucidated by spectroscopic methods and the data for the compounds are reported in Tables 1 and 2 and in Experimental.
  • Jia-You Fang, Jyh-Ping Chen, Yann-Lii Leu, Hsin-Yuan Wang
    2006 年 54 巻 2 号 p. 156-162
    発行日: 2006年
    公開日: 2006/02/01
    ジャーナル フリー
    The objective of this study was to characterize and evaluate the physicochemical properties and drug release profiles of hydrogels composed of silk protein (SP) polymers. SPs with a low MW (SPL, ca. 18 kDa) and a high MW (SPH, ca. 76 kDa) were used for preparing hydrogels. Both the random coil form and β-sheet conformation simultaneously existed in the hydrogels according to Fourier-transformed IR determination. Morphologically, the hydrogels showed a sponge-like cross-linked structure produced by physical entanglement as well as chemical hydrogen and covalent bindings. The in vitro buprenorphine delivery from SPH hydrogels showed a slow-release effect, and a zero-order rate was obtained for all preparations. Drug release could be controlled by varying the SPH concentrations or incorporation of SPL into the systems. SP hydrogels showed a stronger barrier property for hydrophilic solutes than for hydrophobic solutes. The incorporation of SPH into Pluronic F-127 (PF-127) hydrogels changed the gel structure from amorphous micelles to a regularly interconnected texture with pores. Furthermore, SPH as an adjuvant polymer in PF-127 and chitosan hydrogels lowered and controlled the amount of drug released from those systems.
  • Tetsuji Noguchi, Naoki Tanaka, Toyoki Nishimata, Riki Goto, Miho Hayak ...
    2006 年 54 巻 2 号 p. 163-174
    発行日: 2006年
    公開日: 2006/02/01
    ジャーナル フリー
    A series of bisamidine derivatives each having a ring structure in the center of the molecule was synthesized and their Factor Xa (FXa) inhibitory activities were evaluated. Among them, some indoline derivatives showed potent inhibitory activities in vitro. In particular, (R)-18a having an (R)-configuration at the 2-position of the indoline ring exhibited the most potent FXa inhibitory activity in vitro, more potent than DX-9065a. Furthermore, (R)-18a exhibited more potent anticoagulant activity than DX-9065a. We also succeeded in obtaining an X-ray crystal structure of FXa bound with (R)-18a.
  • Masaaki Sugimoto, Shinji Narisawa, Koji Matsubara, Hiroyuki Yoshino, M ...
    2006 年 54 巻 2 号 p. 175-180
    発行日: 2006年
    公開日: 2006/02/01
    ジャーナル フリー
    The aim of this article was to determine the optimal ingredients for the rapidly disintegrating oral tablets prepared by the crystalline transition method (CT method). The effect of ingredients (diluent, active drug substance and amorphous sugar) on the characteristics of the tablets was investigated. The ingredients were compressed and the resultant tablets were stored under various conditions. The oral disintegration time of the tablet significantly depended on diluents, due to differences in the penetration of a small amount of water in the mouth and the viscous area formed inside the tablet. The oral disintegration time was 10—30 s for tablets with a tensile strength of approximately 1 MPa, when erythritol, mannitol or xylitol was used as the diluent. The increase in the tensile strength of tablets containing highly water-soluble active drug substances during storage was as large as that of tablets without active drug substances, while the increase in the tensile strength of tablets containing low water-soluble active drug substances was small. It was therefore found that highly water-soluble active drug substances were more suitable for the formulation prepared by the CT method than low water-soluble active drug substances. Irrespective of the type of amorphous sugar (amorphous sucrose, lactose or maltose) used, the porosity of tablets with 1 MPa of tensile strength was 30—40%, and their oral disintegration time was 10—20 s. The optimal ingredients for rapidly disintegrating oral tablets with reasonable tensile strength and disintegration time were therefore determined from these results.
  • Seitaro Kamiya, Yasuo Nozawa, Astuo Miyagishima, Takurou Kurita, Yasuy ...
    2006 年 54 巻 2 号 p. 181-184
    発行日: 2006年
    公開日: 2006/02/01
    ジャーナル フリー
    We have attempted to prepare micronized drug particles and to maintain the micronized state long-term in order to improve the solubility of a practically insoluble drug, griseofulvin (GF). GF nanoparticles (GFNPs) prepared by high-pressure homogenization were micronized to about 45 nm (mean particle size). GFNPs were subjected to transmission electron microscopy (TEM) observation. The mean particle size remained at about 50 nm for 3 months at 25 °C. However, increased to about 300 nm in 6 months. After 5% (w/v) sugar was added, GFNP was freeze-dried and rehydrated. The mean particle size of the rehydrated GFNPs was about 160 nm when the sugar was a monosaccharide. In contrast, it was about 55—65 nm when the sugar was a disaccharide. The powder X-ray diffraction pattern of the monosaccharide-containing freeze-dried GFNPs revealed a crystal state of sugar. On the other hand, that of the disaccharide-containing freeze-dried GFNPs indicated an amorphous state of sugar. From this result, it is considered that the high viscosity of an amorphous sugar prevents GFNPs from aggregating through retardation of molecular movement. Freeze-dried GFNPs stored for six months at 25 °C showed a good re-dispersibility. After the rehydration the mean particle size of GFNPs was 55—65 nm. It was found that freeze-dried GFNPs containing sucrose, maltose or trehalose were stable for longer periods than GFNP suspensions.
  • Tomoo Hosoe, Takeshi Itabashi, Nao Kobayashi, Shun-ichi Udagawa, Ken-i ...
    2006 年 54 巻 2 号 p. 185-187
    発行日: 2006年
    公開日: 2006/02/01
    ジャーナル フリー
    Three new type indoloditerpenes, emindoles PA (1), PB (2), and PC (3), were isolated from the mycelium of Emericella purpurea along with the sesterterpenes variecolol and variecolactone, and the dicyanide derivatives epurpurins A to C. The structures of 1—3 were confirmed by the spectroscopic investigation. The structure of emindoles PA (1) was revised from our preliminary report. Emindoles PA (1), PB (2), and PC (3) are the indoloditerpenes having a new type of carbon skeleton.
  • Zhijun Yang, Chi Sun Wong, Chun Yang, Zhi-Hong Jiang, Zhongzhen Zhao, ...
    2006 年 54 巻 2 号 p. 188-195
    発行日: 2006年
    公開日: 2006/02/01
    ジャーナル フリー
    This research investigated the effects of control release of binders that are used in the pills of Chinese herbal medicine, namely, as processed honey, starch paste, beeswax, or mixtures thereof. Aspirin and baicalin were used as the active pharmaceutical ingredients (API). The processed honey was heated to 110 °C, 120 °C, or 130 °C. In these pills, the binders were the only excipients. The pills were prepared by the stir method using a mixer at 80 °C without pressure. The differential thermal analysis (DTA) showed that the melting points of aspirin and baicalin were changed by the binders. The Fourier Transform infrared spectra (FT-IR) of aspirin and baicalin suggest that there are different non-covalent molecular interactions between the API and the binders, such as C–H–π and hydrogen bond interaction. The dissolution profiles indicate that changing the ratio of the binders altered the patterns of dissolution of the API; thus, this ration may be used to control the release of API from the pills.
  • Shigeki Sano, Hisashi Shimizu, Kweon Kim, Woo Song Lee, Motoo Shiro, Y ...
    2006 年 54 巻 2 号 p. 196-203
    発行日: 2006年
    公開日: 2006/02/01
    ジャーナル フリー
    Diethyl α-alkynyl-α-methoxymalonates (2a—e) were smoothly hydrolyzed and then decarboxylated under alkaline conditions employing 1 N KOH in EtOH to give conjugated allenyl esters (6a—e) in high yields, and similar alkaline treatment of diethyl α-alkynyl-α-acetylaminomalonates (5a, b, d, e) furnished unexpectedly the oxazoles (7a, b, d, e) having three substituent groups in excellent yields.
  • Reiko Fujita, Toshiteru Yoshisuji, Sota Wakayanagi, Hideaki Wakamatsu, ...
    2006 年 54 巻 2 号 p. 204-208
    発行日: 2006年
    公開日: 2006/02/01
    ジャーナル フリー
    Diels–Alder reactions of 3-nitro-2(1H)-quinolones with 1,3-butadiene derivatives were carried out to give the phenanthridone derivatives under both atmospheric and high pressure conditions. Furthermore, the reactivity of 3-substituted 2(1H)-quinolones acting as a dienophile with 2,3-dimethyl-1,3-butadiene was examined using molecular orbital (MO) calculation.
  • Reiko Fujita, Sota Wakayanagi, Hideaki Wakamatsu, Hisao Matsuzaki
    2006 年 54 巻 2 号 p. 209-212
    発行日: 2006年
    公開日: 2006/02/01
    ジャーナル フリー
    A novel Diels–Alder (DA) reaction with 4-nitro-1(2H)-isoquinolones acting as the dienophile afforded 5(6H)-phenanthridone derivatives. The DA reaction of 4-nitro-1(2H)-isoquinolone with 1-methoxy-1,3-butadiene gave biologically active 5(6H)-phenanthridone possessing in a high yield. Regioselectivity of 4-nitro-1(2H)-isoquinolones with 1-methoxy-3-silyloxy-1,3-butadiene was calculated using molecular orbital (MO) calculations.
  • Suresh Awale, Thein Zaw Linn, Yasuhiro Tezuka, Surya Kant Kalauni, Arj ...
    2006 年 54 巻 2 号 p. 213-218
    発行日: 2006年
    公開日: 2006/02/01
    ジャーナル フリー
    Ten new furanocassane-type diterpenes named, caesalpinins H—P (1—9) and norcaesalpinin F (10), were isolated from the CH2Cl2 extract of the seed kernels of Caesalpinia crista, together with 13 known diterpenes. Their structures were determined based on the spectroscopic analysis. Among the isolated compounds, caesalpinin N (7) represents the first example of furanocassane-type diterpene possessing an aldehyde group at C-14.
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