Analysis of the release process of phenylpropanolamine hydrochloride from ethylcellulose matrix granules II. effects of the binder solution on the release process.

abstract：:We previously reported 2-[2-(4-tert-butylphenyl)ethyl]-N-(4-fluorophenyl)-1,2,3,4-tetrahydroisoquinoline-6-sulfonamide 2 as on orally available monoacylglycerol acyltransferase 2 (MGAT2) inhibitor which exhibited an in vivo efficacy at an oral dose of 100 mg/kg in a mouse oral lipid tolerance test. Further optimizatio...

journal_title：Chemical & pharmaceutical bulletin

authors： Busujima T,Tanaka H,Iwakiri K,Shirasaki Y,Munetomo E,Saito M,Masuko A,Kitano K,Io F,Kato K,Kamigaso S,Nozoe A,Sato N

更新日期：2016-01-01 00:00:00

abstract：:Analogues with the scaffolds of 3-cyano-4-alkoxyphenyl-6-bromoaryl-2-pyridone and 2-amino-3-cyano-4-alkoxyphenyl-6-bromoarylpyridine were synthesized. Cyclization of the 2-amino derivatives with formic acid and formamide gave the corresponding pyrido[2,3-d]pyrimidin-4(3H)-one and the pyrido[2,3-d]-pyrimidin-4-amine de...

journal_title：Chemical & pharmaceutical bulletin

authors： Abadi AH,Hany MS,Elsharif SA,Eissa AA,Gary BD,Tinsley HN,Piazza GA

更新日期：2013-01-01 00:00:00

abstract：:Optically active structural isomers (1b-f and dst-1b-f) of 3',4'-di-(O)-(-)-camphanoyl-(+)-khellactone (DCK) were synthesized and their anti-human immunodeficiency virus (HIV) activity was investigated. The value of the sensitivity index (SI) of 1b was greater than that of DCK. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Nishioka H,Uesugi K,Ueda N,Kondo Y,Tsuji M,Abe H,Harayama T,Hamasaki T,Baba M,Takeuchi Y

更新日期：2011-01-01 00:00:00

abstract：:A novel crystalline Zn(II) complex of L-carnosine was prepared and evaluated for inhibitory activity against gastric ulceration in rats. The complex was found to be much more active than various other Zn(II) compounds. It was characterized by means of infrared (IR) spectroscopy, solid-state carbon-13 (13C) and nitroge...

journal_title：Chemical & pharmaceutical bulletin

authors： Matsukura T,Takahashi T,Nishimura Y,Ohtani T,Sawada M,Shibata K

更新日期：1990-11-01 00:00:00

abstract：:A nondestructive, efficient, and rapid method for quantitative analysis of two bioactive components (salidroside and p-tyrosol) in Rhodiola crenulata, a traditional Tibetan medicine, by Fourier transform near-infrared (FT-NIR) spectroscopy was developed. Near-infrared diffuse reflectance spectra in the range of 4000 t...

journal_title：Chemical & pharmaceutical bulletin

authors： Li T,He X

更新日期：2016-01-01 00:00:00

abstract：:A series of N-(trifluoromethyl-2-pyridinyl)alkane- and arenesulfonamides 2-5 have been synthesized by the substitution reaction of 2-chloro(trifluoromethyl)pyridines 6 with alkane- and arenesulfonamides 7. Their inhibitory activities against secretory phospholipase A₂ of porcine pancreas were examined and the analog N...

journal_title：Chemical & pharmaceutical bulletin

authors： Nakayama H,Morita Y,Kimura H,Ishihara K,Akiba S,Uenishi J

更新日期：2011-01-01 00:00:00

abstract：:Conferols A (1) and B (2), the new 4-hydroxyisoflavones, have been isolated from the dichloromethane sub-fraction of the methanolic extract of Caragana conferta along with 3',5'-dihydroxy, 7,4'-dimethoxyisoflavone (3), E-cinnamic acid (4), tetracosyl 3,4-dihydroxy-E-cinnamate (5), docosyl 3,4-dihydroxy-E-cinnamate (6)...

journal_title：Chemical & pharmaceutical bulletin

authors： Khan R,Malik A,Adhikari A,Qadir MI,Choudhary MI

更新日期：2009-04-01 00:00:00

abstract：:Enantioselective fluorinating agents, (R)- and (S)-,N-fluoro-3-tert-butyl-7-nitro-3,4-dihydro-2H-benzo[e][1,2]thiazine 1,1-dioxides (BNBT-F, 2) are readily prepared in 3 steps from racemic 3-tert-butyl-7-nitro-3,4-dihydro-2H-benzo[e][1,2]thiazine 1,1-dioxides (5) via optical resolution and fluorination. These agents m...

journal_title：Chemical & pharmaceutical bulletin

authors： Shibata N,Liu Z,Takeuchi Y

更新日期：2000-12-01 00:00:00

abstract：:We designed and synthesized a new class of peptidomimetic human immunodeficiency virus protease inhibitors containing a unique unnatural amino acid, allophenylnorstatine [Apns; (2S,3S)-3-amino-2-hydroxy-4-phenylbutyric acid], with a hydroxymethylcarbonyl isostere as the active moiety. From a structure-activity relatio...

journal_title：Chemical & pharmaceutical bulletin

authors： Mimoto T,Hattori N,Takaku H,Kisanuki S,Fukazawa T,Terashima K,Kato R,Nojima S,Misawa S,Ueno T,Imai J,Enomoto H,Tanaka S,Sakikawa H,Shintani M,Hayashi H,Kiso Y

更新日期：2000-09-01 00:00:00

abstract：:Italian canned tomatoes contain the tomato glycosides esculeosides B-1 (1, 0.0052%) and B-2 (2, 0.0068%) without esculeoside A. Herein, the structure of esculeoside B-1 (1) is characterized to be 3-O-β-lycotetraosyl (5S,22R,23S,25S)-22,26-epimino-16β,23-epoxy-3β,23,27-trihydroxycholestane 27-O-β-D-glucopyranoside. We ...

journal_title：Chemical & pharmaceutical bulletin

authors： Manabe H,Fujiwara Y,Ikeda T,Ono M,Murakami K,Zhou JR,Yokomizo K,Nohara T

更新日期：2013-01-01 00:00:00

abstract：:The effects of storage on the crystallization, dissolution and absorption of tolbutamide from amorphous tolbutamide-2-hydroxypropyl-beta-cyclodextrin (HP-beta-CyD) complex were investigated, in comparison with those of polyvinylpyrrolidone (PVP) solid dispersion. The amorphous solid complex of tolbutamide with HP-beta...

journal_title：Chemical & pharmaceutical bulletin

authors： Kimura K,Hirayama F,Arima H,Uekama K

更新日期：2000-05-01 00:00:00

abstract：:Improvement of solubility for fullerene (C60) was studied by cogrinding with cycloamyloses using a ball mill in the solid state. Cycloamylose is a novel cyclic alpha-1,4-glucan produced from synthetic amylose by enzymatic reaction. Although sample solutions showed a pale yellow for the initial period of cogrinding wit...

journal_title：Chemical & pharmaceutical bulletin

authors： Fukami T,Mugishima A,Suzuki T,Hidaka S,Endo T,Ueda H,Tomono K

更新日期：2004-08-01 00:00:00

abstract：:Among the muscarinic acetylcholine receptor (mAChR) subtypes, the M4 receptor has been investigated as a promising drug target for the treatment of schizophrenia. These investigations have been based on findings from M4-deficient mice studies as well as on the results of a clinical trial that used xanomeline, an M1/M4...

journal_title：Chemical & pharmaceutical bulletin

authors： Takai K,Enomoto T

更新日期：2018-01-01 00:00:00

abstract：:In order to synthesize four stereoisomers of cystathionine (CYT), D- and L-homocysteines (D- and L-Hcy) were synthesized from methionine (Met) by a facile procedure. L-Met was reacted with dichloroacetic acid in concentrated hydrochloric acid under reflux to give (4S)-1,3-thiazane-2,4-dicarboxylic acid hydrochloride [...

journal_title：Chemical & pharmaceutical bulletin

authors： Shiraiwa T,Nakagawa K,Kanemoto N,Kinda T,Yamamoto H

更新日期：2002-08-01 00:00:00

abstract：:Gambir, the aqueous extract from Uncaria gambir (Rubiaceae), has been used as an astringent medicine in Asian countries. Investigation of the constituents in the extract led to the isolation of four chalcane-flavan dimers, gambiriin A1 (6), A2 (7), B1 (8), and B2 (9), in addition to (+)-catechin (1), (+)-epicatechin (...

journal_title：Chemical & pharmaceutical bulletin

authors： Taniguchi S,Kuroda K,Doi K,Tanabe M,Shibata T,Yoshida T,Hatano T

更新日期：2007-02-01 00:00:00

abstract：:α,β-Unsaturated amides were incorporated as viable dipolarophiles in a catalytic asymmetric 1,3-dipolar cycloaddition of azomethine imines. The use of a 7-azaindoline auxiliary was essential to acquire sufficient reactivity with excellent diastereoselectivity, likely due to the chelating activation of the amide by the...

journal_title：Chemical & pharmaceutical bulletin

authors： Li Z,Kumagai N,Shibasaki M

更新日期：2020-01-01 00:00:00

abstract：:Two series of new pyridines bearing thiazoline (3a--n) and thiazolidinone (5a--e) moieties were prepared via the cyclization of the corresponding substituted pyridyl thiourea (2a--g) with an appropriately substituted phenacyl bromide or chloroacetic acid, respectively. The antimicrobial activity was determined for rep...

journal_title：Chemical & pharmaceutical bulletin

authors： Hassan HY,el-Koussi NA,Farghaly ZS

更新日期：1998-05-01 00:00:00

abstract：:Arginine-vasopressin (AVP) was acylated with various acyl azides (2a-j) in pH 9.1 buffer to give AVP derivatives (11a-j) modified at the tyrosine side chain with a carbohydrate via a spacer arm. Glycoconjugates of AVP modified at the N-terminal amide (12a-e) were also synthesized from AVP and carboxylic acids (3a-e) u...

journal_title：Chemical & pharmaceutical bulletin

authors： Susaki H,Suzuki K,Ikeda M,Yamada H,Watanabe HK

更新日期：1998-10-01 00:00:00

abstract：:A gas chromatography-selected ion monitoring procedure with chemical ionization is described for the determination of bromovalerylurea (BVU) in human plasma. BVU was extracted with ether after addition of 2-bromo-2-methylpropylurea as an internal standard. The lower limit of BVU quantification by this method was 2 ng/...

journal_title：Chemical & pharmaceutical bulletin

authors： Kokatsu J,Yomoda R,Suwa T

更新日期：1992-06-01 00:00:00

abstract：:Three new norlanostane-type triterpene glycosides, scillanostasides A, B, and C, and two new lanostane-type triterpene glycosides, scillanostasides D and E, were isolated from the bulbs of Scilla scilloides Druce (Liliaceae) along with one known norlanostane-type triterpene heptaglycoside, scillascilloside G-1. Their ...

journal_title：Chemical & pharmaceutical bulletin

authors： Ono M,Toyohisa D,Morishita T,Horita H,Yasuda S,Nishida Y,Tanaka T,Okawa M,Kinjo J,Yoshimitsu H,Nohara T

更新日期：2011-01-01 00:00:00

abstract：:Interaction between Mn2+ ion and the two forms of DNA duplex (supercoiled and linearized pUC119 DNA) in solution has been examined by isothermal titration calorimetry. Although DNA condensation reaction heat was observed at 323 K, this was not the case at 298 K. DNA condensation was entropically driven and supercoiled...

journal_title：Chemical & pharmaceutical bulletin

authors： Utsuno K

更新日期：2008-03-01 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：:Allylamine (ALAM) film was plasma-polymerized on a flat glass (referred to as ALAM(GLA): GLA refers to a flat glass plate) for use as a solid phase in two-site immunoradiometric assay (two-site IRMA). Adsorption of F(ab')2 anti-human immunoglobulin G [formula: see text] to ALAM(GLA) was larger than adsorption on a pol...

journal_title：Chemical & pharmaceutical bulletin

authors： Muratsugu M,Kurosawa S,Mori Y,Kamo N

更新日期：1992-02-01 00:00:00

abstract：:1,4-Oxazepine formation reactions of 1,8-naphthyridine derivatives (1-4) with peroxy acid have been studied using a semiempirical MO method (AM1) and an ab initio molecular orbital method (Gaussian 94). The energies of molecules involved in the reaction paths were calculated and the transition states related to experi...

journal_title：Chemical & pharmaceutical bulletin

authors： Matsuzaki H,Takeuchi I,Hamada Y,Hatano K

更新日期：2000-05-01 00:00:00

abstract：:The methanolic extracts from the wood and bark of Cotylelobium melanoxylon were found to inhibit plasma glucose elevation after sucrose loading in rats and triglyceride elevation after olive oil loading in mice. A new stilbene dimer, melanoxylin A, together with the known stilbene dimers [(+)-ampelopsin F, (+)-isoampe...

journal_title：Chemical & pharmaceutical bulletin

authors： Matsuda H,Asao Y,Nakamura S,Hamao M,Sugimoto S,Hongo M,Pongpiriyadacha Y,Yoshikawa M

更新日期：2009-05-01 00:00:00

abstract：:Three new hydronaphthalenone derivatives (1-3) and one new dihydroramulosin derivative (4), were isolated from the endophytic fungus PSU-N24 together with eight known compounds. Their structures were elucidated by spectroscopic methods. Griseofulvin (9) displayed strong antifungal activity against Microsporum gypseum ...

journal_title：Chemical & pharmaceutical bulletin

authors： Sommart U,Rukachaisirikul V,Sukpondma Y,Phongpaichit S,Sakayaroj J,Kirtikara K

更新日期：2008-12-01 00:00:00

abstract：:We have examined the lipid peroxide levels in aclacinomycin (ACM)-treated mice by using adriamycin (ADR) as a comparative drug. There was no increase in the lipid peroxide level of the heart at either 3h or 4d after ACM administration (15 mg/kg, i.p.), although the level in the heart of ADR-treated mice was elevated t...

journal_title：Chemical & pharmaceutical bulletin

authors： Sazuka Y,Yoshikawa K,Tanizawa H,Takino Y

更新日期：1989-12-01 00:00:00

abstract：:The generation of a different type of beta-kallikrein, designated C beta-kallikrein, from alpha-kallikrein by chymotryptic action was ascertained by the following observations: 1) When alpha-kallikrein was incubated with chymotrypsin, an increase of esterolytic activity of kallikrein was observed. 2) In sodium dodecyl...

journal_title：Chemical & pharmaceutical bulletin

authors： Kamada M,Ikekita M,Kurahashi T,Aoki K,Kizuki K,Moriya H,Sweeley CC,Kamo M,Tsugita A

更新日期：1990-04-01 00:00:00

abstract：:The metabolic pathway of butylated hydroxytoluene (BHT) to the ring-oxygenated metabolites 2,6-di-tert-butylhydroquinone (BHQ) and 2,6-di-tert-butyl-p-benzoquinone (BBQ) was examined in rats. After intraperitoneal administration of 3,5-di-tert-butyl-4-hydroxybenzoic acid (BHT-acid), which had been regarded as one of t...

journal_title：Chemical & pharmaceutical bulletin

authors： Yamamoto K,Tajima K,Takemura M,Mizutani T

更新日期：1991-02-01 00:00:00

abstract：:The oxalate salts and free bases of fentanyl and N-[1-(2-phenylethyl)-4-piperidyl]-N-(1-phenyl-4-pyrazolyl)propanamide, a new lead compound for long-acting analgesia, have been characterized by (1)H- and (13)C-NMR spectroscopy. The crystal structure of the hydrochloride of N-[1-(2-phenylethyl)-4-piperidyl]-N-(1-phenyl...

journal_title：Chemical & pharmaceutical bulletin

authors： Jimeno ML,Alkorta I,Cano C,Jagerovic N,Goya P,Elguero J,Foces-Foces C

更新日期：2003-08-01 00:00:00