Immediate release tablets of telmisartan using superdisintegrant-formulation, evaluation and stability studies.

abstract：:Orally disintegrating tablets (ODTs) are useful for improving benefits for patients of various ages. Masking the unpleasant taste of a drug is an important factor in the compliance of patients who take ODTs. We evaluated the taste acceptability effects of various taste-masking methods on bitter famotidine ODTs as a cl...

journal_title：Chemical & pharmaceutical bulletin

authors： Sugiura T,Uchida S,Namiki N

更新日期：2012-01-01 00:00:00

abstract：:We have already reported unique compounds containing a N,O-spiro acetal structure as an orally active factor Xa (FXa) inhibitor. This time, we described a N,N-spiro acetal structure as an analogue of the N,O-spiro acetal structure for an orally active FXa inhibitor. The synthesis of these analogues could be achieved i...

journal_title：Chemical & pharmaceutical bulletin

authors： Saitoh F,Mukaihira T,Nishida H,Satoh T,Okano A,Yumiya Y,Ohkouchi M,Johka R,Matsusue T,Shiromizu I,Hosaka Y,Matsumoto M,Ohnishi S

更新日期：2006-11-01 00:00:00

abstract：:From the methanolic extract of Indonesian Orthosiphon stamineus, nine new highly-oxygenated isopimarane-type diterpenes [7-O-deacetylorthosiphol B (1), 6-hydroxyorthosiphol B (2), 3-O-deacetylorthosiphol I (3), 2-O-deacetylorthosiphol J (4), siphonols A-E (5-9)] have been isolated together with nine known diterpenes [...

journal_title：Chemical & pharmaceutical bulletin

authors： Awale S,Tezuka Y,Banskota AH,Adnyana IK,Kadota S

更新日期：2003-03-01 00:00:00

abstract：:Two new stilbene glucosides [(+)-alpha-viniferin 13b-O-beta-glucopyranoside and resveratrol 12-C-beta-glucopyranoside] and two new resveratrol oligomers, hemsleyanols A and B, were isolated from the bark of Shorea hemsleyana along with four known resveratrol oligomers. The structures of the isolates, including the rel...

journal_title：Chemical & pharmaceutical bulletin

authors： Ito T,Tanaka T,Ido Y,Nakaya KI,Iinuma M,Riswan S

更新日期：2000-07-01 00:00:00

abstract：:A full account is given of the first chemical synthesis of the antitumor antibiotic guanine 7-oxide (5) and its 9-substituted derivatives (24a--k and 26). Coupling of appropriate primary amines (17a--e, g--k) with phenacyl bromide (16) produced, after treatment with HCl, the corresponding N-substituted phenacylamine h...

journal_title：Chemical & pharmaceutical bulletin

authors： Ogawa K,Nishii M,Inagaki J,Nohara F,Saito T,Itaya T,Fujii T

更新日期：1992-02-01 00:00:00

abstract：:The structures of new neo-lignans, isoamericanol A (1) and americanol A (2) isolated from the seeds of Phytolacca americana have been elucidated on the basis of spectroscopic data and then confirmed by chemical correlation with the previously known isoamericanin A (3) and americanin A (4). Isoamericanol A, americanol ...

journal_title：Chemical & pharmaceutical bulletin

authors： Fukuyama Y,Hasegawa T,Toda M,Kodama M,Okazaki H

更新日期：1992-01-01 00:00:00

abstract：:The prediction of a protein three-dimensional (3D) structure is one of the most important challenges in computational structural biology. We have developed an automatic protein 3D structure prediction method called FAMSD. FAMSD is based on a comparative modeling method which consists of the following four steps: (1) g...

journal_title：Chemical & pharmaceutical bulletin

authors： Kanou K,Iwadate M,Hirata T,Terashi G,Umeyama H,Takeda-Shitaka M

更新日期：2009-12-01 00:00:00

abstract：:Adriamycin linked to oxidized dextran (ADM-OXD) via Schiff's base formation was compared with free adriamycin with regard to antitumor activity, acute toxicity and plasma pharmacokinetics in rats following i.v. administration. ADM-OXD showed higher activity against Walker carcinosarcoma 256 than free adriamycin. On th...

journal_title：Chemical & pharmaceutical bulletin

authors： Ueda Y,Munechika K,Kikukawa A,Kanoh Y,Yamanouchi K,Yokoyama K

更新日期：1989-06-01 00:00:00

abstract：:In this study, we describe a highly selective etherification procedure of unprotected morroniside catalyzed by molecular iodine in acetone. The etherification reaction furnished 7-O-alkyl ether derivatives in reasonable yields within few hours under neutral conditions. Studies of the obtained products on cytotoxicity ...

journal_title：Chemical & pharmaceutical bulletin

authors： Sunghwa F,Sakurai H,Saiki I,Koketsu M

更新日期：2009-01-01 00:00:00

abstract：:Solifenacin (Sol), an antimuscarinic agent has been widely used for the treatment of overactive bladder. Transdermal formulations can be administered without water as well as absorbed slowly into the blood over a long period of time. The aim of this study was to develop cream and tape formulations of Sol, and evaluate...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshida M,Uchida S,Kashiwagura Y,Tanaka S,Matsui R,Namiki N

更新日期：2019-01-01 00:00:00

abstract：:First, Raddeanin A, a cytotoxic oleanane-type triterpenoid saponin isolated from Anemone raddeana REGEL, was synthesized. Stepwise glycosylation was adopted in the synthesis from oleanolic acid, employing arabinosyl, glucosyl and rhamnosyl trichloroacetimidate as donors. The chemical structure of Raddeanin A was confi...

journal_title：Chemical & pharmaceutical bulletin

authors： Qian S,Chen QL,Guan JL,Wu Y,Wang ZY

更新日期：2014-01-01 00:00:00

abstract：:Manufacturing the solid dosage form of an orally administered drug requires lubrication to enhance manufacturability, ensuring that critical quality attributes such as disintegration and dissolution of the drug product are maintained during manufacture. Here, to evaluate lubrication performance during manufacture, we ...

journal_title：Chemical & pharmaceutical bulletin

authors： Dohi M,Momose W,Yamashita K,Hakomori T,Sato S,Noguchi S,Terada K

更新日期：2017-02-01 00:00:00

abstract：:Mycobacterial cell walls have diverse adjuvant activities, and in particular, cell wall skeleton (CWS) of Mycobacterium bovis BCG has been expected as a drug for tumor immunotherapy. However, its molecular structure-biological activity relationship has not been fully elucidated despite more than 30 years of intensive ...

journal_title：Chemical & pharmaceutical bulletin

authors： Uenishi Y,Okada T,Okabe S,Sunagawa M

更新日期：2007-06-01 00:00:00

abstract：:A series of 43 stilbene derivatives that showed cytotoxicity against human lung carcinoma (A549) was analyzed using comparative molecular field analysis (CoMFA) for defining the hypothetic pharmacophore model. The polyoxylated stilbenes were found to be active inhibitors of tubulin polymerization. Several cis-stilbene...

journal_title：Chemical & pharmaceutical bulletin

authors： Kim S,Min SY,Lee SK,Cho WJ

更新日期：2003-05-01 00:00:00

abstract：:To find candidates with high antimicrobial and low hemolytic activities, many gramicidin S (GS) analogs of various ring sizes have been designed and synthesized. However, syntheses of antimicrobially active analogues of GS having a disordered symmetry structure from C(2) have almost never been reported, because the st...

journal_title：Chemical & pharmaceutical bulletin

authors： Tamaki M,Takanashi K,Harada T,Fujinuma K,Shindo M,Kimura M,Uchida Y

更新日期：2011-01-01 00:00:00

abstract：:The crystal of bovine trypsin complexed with a potent inhibitor, 4-[4-(N,N- dimethylcarbamoylmethoxycarbonylmethyl)phenoxycarbonylphenyl ]guanidinium (FOY-305) in the novel orthorhombic from with a low molecular packing density was studied by the X-ray diffraction method. Using synchrotron radiation, the intensity dat...

journal_title：Chemical & pharmaceutical bulletin

authors： Matsumoto O,Taga T,Matsushima M,Higashi T,Machida K

更新日期：1990-08-01 00:00:00

abstract：:Two alkaloids, megistoquinone I (1) and megistoquinone II (2), were isolated from the bark of Sarcomelicope megistophylla. Their structures have been elucidated on the basis of MS and NMR data. Both belong to quinoline alkaloid series and should be considered as oxidation products of a furo[2,3-b]quinoline precursor. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Fokialakis N,Magiatis P,Chinou I,Mitaku S,Tillequin F

更新日期：2002-03-01 00:00:00

abstract：:High-performance liquid chromatography coupled with solid phase extraction method was developed for determination of isofraxidin in rat plasma after oral administration of Acanthopanax senticosus extract (ASE), and pharmacokinetic parameters of isofraxidin either in ASE or pure compound were measured. The HPLC analysi...

journal_title：Chemical & pharmaceutical bulletin

authors： Sun H,Lv H,Zhang Y,Wang X,Bi K,Cao H

更新日期：2007-09-01 00:00:00

abstract：:Gadolinium-diethylenetriaminepentaacetic acid (Gd-DTPA), a paramagnetic contrast agent for use in magnetic resonance imaging (MRI) was bound to stearylamine and incorporated into the liposomal membranes (Gd-DTPA liposomes). In addition, the Gd-DTPA liposomes were coated with mannan (cholesterol-aminoethylcarbamylmethy...

journal_title：Chemical & pharmaceutical bulletin

authors： Kunimasa J,Inui K,Hori R,Kawamura Y,Endo K

更新日期：1992-09-01 00:00:00

abstract：:To understand more fully the effect of polyunsaturated fatty acids (PUFAs) on lipid bilayers, we investigated the effects of treatment with fatty acids on the properties of a model membrane. Three kinds of liposomes comprising dipalmitoylphosphatidylcholine (DPPC), dioleylphosphatidylcholine (DOPC), and cholesterol (C...

journal_title：Chemical & pharmaceutical bulletin

authors： Onuki Y,Hagiwara C,Sugibayashi K,Takayama K

更新日期：2008-08-01 00:00:00

abstract：:A powder solid dispersion system (SD) of indomethacin (IM) with crospovidone (CrosPVP) possesses good fluidity and can be used for tablet formulation. Tablets of SD can be prepared by direct compression and have adequate hardness and a small variation in weight. Forces during the tableting process were measured with a...

journal_title：Chemical & pharmaceutical bulletin

authors： Shibata Y,Fujii M,Okada H,Noda S,Kondoh M,Watanabe Y

更新日期：2005-07-01 00:00:00

abstract：:The structures of the adducts derived from the reactions of substituted ketenes with dihydropyridine derivatives have been clarified by single crystal X-ray analyses and the formation mechanism is discussed on the basis of the reaction-path calculations by semiempirical and density functional theory (DFT) molecular or...

journal_title：Chemical & pharmaceutical bulletin

authors： Oiso S,Eto M,Yoshitake Y,Harano K

更新日期：2003-09-01 00:00:00

abstract：:In the course of our research on spiro-compounds as neurokinin receptor antagonists, N-[2-aryl-4-(spiro-substituted piperidin-1'-yl)butyl]carboxamides were designed, based on YM-35375 (3) as a lead compound, and evaluated for NK2 receptor-antagonistic activities. Some derivatives inhibited the binding of radio-labeled...

journal_title：Chemical & pharmaceutical bulletin

authors： Kubota H,Kakefuda A,Nagaoka H,Yamamoto O,Ikeda K,Takeuchi M,Shibanuma T,Isomura Y

更新日期：1998-02-01 00:00:00

abstract：:Structural optimization of 2-aminonicotinamide derivatives as ghrelin receptor inverse agonists is reported. So as to avoid mechanism-based inactivation (MBI) of CYP3A4, 1,3-benzodioxol ring of the lead compound was modified. Improvement of the main activity and lipophilicity was achieved simultaneously, leading to co...

journal_title：Chemical & pharmaceutical bulletin

authors： Takahashi B,Funami H,Shibata M,Maruoka H,Koyama M,Kanki S,Muto T

更新日期：2015-01-01 00:00:00

abstract：:The sugar-inositol portion of the novel glycosylinositol-phosphoceramides, ZGL1 and ZGL2, from the filamentus fungi, Acremonium sp., were elucidated by a combination of NMR techniques including (1)H-(1)H (COSY and HOHAHA) and (1)H-(13)C (HMQC and HMBC) spectroscopy. Further, examination of the (1)H-(31)P HMQC spectrum...

journal_title：Chemical & pharmaceutical bulletin

authors： Yamada-Hada J,Hada N,Aoki K,Yamamoto K,Takeda T

更新日期：2004-04-01 00:00:00

abstract：:Silver loaded zeolite (Ag-Z) was previously found to have effective bactericidal activity against Escherichia coli. To understand the mechanisms of bactericidal activity of Ag-Z, role of light irradiation was focused and investigated in this study. In this study, we focused on light irradiation. Antibacterial assay an...

journal_title：Chemical & pharmaceutical bulletin

authors： Inoue Y,Kogure M,Matsumoto K,Hamashima H,Tsukada M,Endo K,Tanaka T

更新日期：2008-05-01 00:00:00

abstract：:Even though experimental designs are becoming popular especially for conventional dosage forms, limited studies have been performed to optimize formulations of orally disintegrating films (ODFs). This study aimed to evaluate sildenafil citrate-loaded ODFs for a controlled release with hydroxypropyl methylcellulose as ...

journal_title：Chemical & pharmaceutical bulletin

authors： Lee Y,Thapa P,Jeong SH,Woo MH,Choi DH

更新日期：2017-02-01 00:00:00

abstract：:In line with the recent globalization of the drug supply chain and promotion of the use of generic drugs worldwide, quality assurance is required for drugs globally. In particular, controlling impurities is one of the biggest areas of interest regarding pharmaceutical quality, and it is desirable that the latest scien...

journal_title：Chemical & pharmaceutical bulletin

authors： Matsuhama M,Saito R,Miyazaki S

更新日期：2020-01-01 00:00:00

abstract：:Two new friedelane-type triterpenes named 12alpha-hydroxyfriedelane-3,15-dione and 3beta-hydroxyfriedelan-25-al, together with six known compounds were isolated from the stems of Drypetes paxii Hutch. (Euphorbiaceae). Their structures were established on the basis of conventional 1 dimensional (1D) NMR methods, 2D shi...

journal_title：Chemical & pharmaceutical bulletin

authors： Chiozem DD,Trinh-Van-Dufat H,Wansi JD,Mbazoa Djama C,Fannang VS,Seguin E,Tillequin F,Wandji J

更新日期：2009-10-01 00:00:00

abstract：:The percutaneous penetration of R-(+)- and S-(-)-propranolol (PL) through rat excised skin was investigated in vitro. The flux of S-(-)-PL after application to normal skin was high compared with that of R-(+)-PL. On the other hand, in damaged rat skin, the flux of R-(+)-PL was almost equivalent to that of S-(-)-PL. It...

journal_title：Chemical & pharmaceutical bulletin

authors： Miyazaki K,Kaiho F,Inagaki A,Dohi M,Hazemoto N,Haga M,Hara H,Kato Y

更新日期：1992-04-01 00:00:00