Properties of gastroretentive sustained release tablets prepared by combination of melt/sublimation actions of L-menthol and penetration of molten polymers into tablets.

Abstract:

:A novel floating sustained release tablet having a cavity in the center was developed by utilizing the physicochemical properties of L-menthol and the penetration of molten hydrophobic polymer into tablets. A dry-coated tablet containing famotidine as a model drug in outer layer was prepared with a L-menthol core by direct compression. The tablet was placed in an oven at 80°C to remove the L-menthol core from tablet. The resulting tablet was then immersed in the molten hydrophobic polymers at 90°C. The buoyancy and drug release properties of tablets were investigated using United States Pharmacopeia (USP) 32 Apparatus 2 (paddle 100 rpm) and 900 ml of 0.01 N HCl. The L-menthol core in tablets disappeared completely through pathways in the outer layer with no drug outflows when placed in an oven for 90 min, resulting in a formation of a hollow tablet. The hollow tablets floated on the dissolution media for a short time and the drug release was rapid due to the disintegration of tablet. When the hollow tablets were immersed in molten hydrophobic polymers for 1 min, the rapid drug release was drastically retarded due to a formation of wax matrices within the shell of tablets and the tablets floated on the media for at least 6 h. When Lubri wax® was used as a polymer, the tablets showed the slowest sustained release. On the other hand, faster sustained release properties were obtained by using glyceryl monostearate (GMS) due to its low hydrophobic nature. The results obtained in this study suggested that the drug release rate from floating tablets could be controlled by both the choice of hydrophobic polymer and the combined use of hydrophobic polymers.

authors

Fukuda M,Goto A

doi

10.1248/cpb.59.1221

subject

Has Abstract

pub_date

2011-01-01 00:00:00

pages

1221-6

issue

10

eissn

0009-2363

issn

1347-5223

pii

JST.JSTAGE/cpb/59.1221

journal_volume

59

pub_type

杂志文章
  • Toxicity of dioxins: role of an absolute hardness-absolute electronegativity diagram (eta-chi diagram) as a new measure in risk assessment.

    abstract::The differences in biological activities among polychlorinated dibenzo-p-dioxins (dioxins) are strongly dependent on the substitution pattern of chlorine at various positions on the parent dibenzo-p-dioxin molecule. The absolute hardness, eta, of dioxins shows a good correlation with the potency of biological activity...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.43.1780

    authors: Kobayashi S,Sameshima K,Ishii Y,Tanaka A

    更新日期:1995-10-01 00:00:00

  • Light irradiation is a factor in the bactericidal activity of silver-loaded zeolite.

    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

    pub_type: 杂志文章

    doi:10.1248/cpb.56.692

    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

  • Scale-up of high shear granulation based on the internal stress measurement.

    abstract::Scale-up of wet granulation in a vertical high shear mixer was conducted. Pharmaceutical excipient powders composed of lactose, cornstarch and micro-crystallinecellulose, and hydroxypropylcellulose as a binder were mixed together and then granulated with purified water under various operating conditions and vessel sca...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.53.351

    authors: Watano S,Okamoto T,Sato Y,Osako Y

    更新日期:2005-04-01 00:00:00

  • Formycin A resistant mutants due to defect in adenosine transport system in Vibrio parahaemolyticus.

    abstract::An antibiotic formycin A inhibited growth of Vibrio parahaemolyticus under certain conditions, which suggested that formycin A was taken up by cells under these conditions. We found that formycin A was transported via the adenosine transport system which we previously reported as a Na(+)-coupled cotransport system. We...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.39.1325

    authors: Sakai-Tomita Y,Mitani Y,Tsuda M,Tsuchiya T

    更新日期:1991-05-01 00:00:00

  • Temperature-Dependent Formation of N-Nitrosodimethylamine during the Storage of Ranitidine Reagent Powders and Tablets.

    abstract::The purpose of this study was to elucidate the effect of high-temperature storage on the stability of ranitidine, specifically with respect to the potential formation of N-nitrosodimethylamine (NDMA), which is classified as a probable human carcinogen. Commercially available ranitidine reagent powders and formulations...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.c20-00431

    authors: Abe Y,Yamamoto E,Yoshida H,Usui A,Tomita N,Kanno H,Masada S,Yokoo H,Tsuji G,Uchiyama N,Hakamatsuka T,Demizu Y,Izutsu KI,Goda Y,Okuda H

    更新日期:2020-10-01 00:00:00

  • Studies on antiulcer drugs. I. Synthesis and antiulcer activities of imidazo[1,2-alpha]pyridinyl-2-oxobenzoxazolidines-3-oxo-2H-1,4-benzoxaz ines and related compounds.

    abstract::A series of imidazo[1,2-alpha]pyridinyl-2-oxobenzoxazolidines (4a-i), -3-oxo-2H-1,4-benzoxazines (5a-q), their thio-analogues (4j-p and 5r-t) and 5,6,7,8-tetrahydroimidazo[1,2-alpha]pyridinyl derivatives (8 and 9) were synthesized and tested for anti-stress ulcer activity in rats. Several compounds were found to be mo...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.39.2937

    authors: Katsura Y,Nishino S,Takasugi H

    更新日期:1991-11-01 00:00:00

  • Conjugated 1 beta-hydroxycholic acid in the urine of newborns and pregnant women measured by radioimmunoassay using antisera raised against N-(1 beta-hydroxycholyl)-2-aminopropionic acid-bovine serum albumin conjugate.

    abstract::Anti-tauro 1 beta-hydroxycholic acid antisera were prepared by immunizing rabbits with N-(1 beta,3 alpha, 7 alpha, 12 alpha-tetrahydroxy-5 beta-cholan-24-oyl)-2- aminopropionic acid-bovine serum albumin (BSA) conjugate. The antisera raised had high affinity (1.25-1.46 x 10(9) M-1) and specificity for conjugated 1 beta...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.40.1835

    authors: Ikegawa S,Murai T,Yoshimura T,Tohma M

    更新日期:1992-07-01 00:00:00

  • A novel analytical method for pharmaceutical polymorphs by terahertz spectroscopy and the optimization of crystal form at the discovery stage.

    abstract::A novel analytical method for the determination of pharmaceutical polymorphs was developed using terahertz spectroscopy. It was found out that each polymorph of a substance showed a specific terahertz absorption spectrum. In particular, analysis of the second derivative spectrum was enormously beneficial in the discri...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.58.76

    authors: Ikeda Y,Ishihara Y,Moriwaki T,Kato E,Terada K

    更新日期:2010-01-01 00:00:00

  • Synthesis and evaluation of water-soluble non-prodrug analogs of docetaxel bearing sec-aminoethyl group at the C-10 position.

    abstract::To develop non-prodrugs of taxoids with satisfactory stability in vivo, high water-solubility, and potent antitumor activity, we prepared several 10-O-sec-aminoethyl docetaxel analogs (3) and evaluated their cytotoxicity against mouse leukemia and human tumor cell lines, microtubule disassembly-inhibitory activity, an...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.46.770

    authors: Uoto K,Takenoshita H,Yoshino T,Hirota Y,Ando S,Mitsui I,Terasawa H,Soga T

    更新日期:1998-05-01 00:00:00

  • Novel acyl-CoA: cholesterol acyltransferase inhibitor: indoline-based sulfamide derivatives with low lipophilicity and protein binding ratio.

    abstract::To find a novel acyl-CoA: cholesterol acyltransferase inhibitor, a series of sulfamide derivatives were synthesized and evaluated. Compound 1d, in which carboxymethyl moiety at the 5-position of Pactimibe was replaced by a sulfamoylamino group, showed 150-fold more potent anti-foam cell formation activity (IC(50): 0.0...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.58.1057

    authors: Takahashi K,Ohta M,Shoji Y,Kasai M,Kunishiro K,Miike T,Kanda M,Shirahase H

    更新日期:2010-08-01 00:00:00

  • New antitumor bicyclic hexapeptides, RA-XI, -XII, -XIII and -XIV from Rubia cordifolia.

    abstract::Four new bicyclic hexapeptides, named as RA-XI, -XII, XIII and -XIV were isolated from Rubia cordifolia and showed potent antitumor activities against P-388. The structures were elucidated from spectroscopic and chemical evidences. RA-XII, XIII and -XIV were proved to be unique bicyclic hexapeptidic glucosides. ...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.40.1352

    authors: Morita H,Yamamiya T,Takeya K,Itokawa H

    更新日期:1992-05-01 00:00:00

  • Structure of three new carotenoids with a 3-methoxy-5-keto-5,6-seco-4,6-cyclo-beta end group from the seeds of Pittosporum tobira.

    abstract::Three new carotenoids with a 3-methoxy-5-keto-5,6-seco-4,6-cyclo-beta end group (1-3) have been isolated from the seeds of Pittosporum tobira. Their structures were elucidated by detailed analyses of nuclear magnetic resonance and UV data. ...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.49.985

    authors: Fujiwara Y,Maruwaka H,Toki F,Hashimoto K,Maoka T

    更新日期:2001-08-01 00:00:00

  • Synthesis, nematicidal and antimicrobial activity of 3-(5-3-methyl-5-[(3-methyl-7-5-[2-(aryl)-4-oxo-1,3-thiazolan-3-yl]-1,3,4-thiadiazol-2-ylbenzo[b]furan-5-yl)methyl]benzo[b]furan-7-yl-1,3,4-thiadiazol-2-yl)-2-(aryl)-1,3-thiazolan-4-one.

    abstract::A new series of 3-(5-3-methyl-5-[(3-methyl-7-5-[2-(aryl)-4-oxo-1,3-thiazolan-3-yl]-1,3,4-thiadiazol-2-ylbenzo[b]furan-5-yl)methyl]benzo[b]furan-7-yl-1,3,4-thiadiazol-2-yl)-2-(aryl)-1,3-thiazolan-4-one 5a-j has been synthesized by the reaction of N2-[(E)-1-(4-methylphenyl)methylidene]-5-(3-methyl-5-[3-methyl-7-(5-[(E)-...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.58.805

    authors: Reddy CS,Rao DC,Yakub V,Nagaraj A

    更新日期:2010-06-01 00:00:00

  • Three unusual 22-beta-O-23-hydroxy-(5 alpha)-spirostanol glycosides from the fruits of Solanum torvum.

    abstract::Three novel 22-beta-O-spirostanol oligoglycosides, torvosides J (1), K (2) and L (3) have been isolated from the fruits of Solanum torvum SWARTZ and their chemical structures have been characterized based on the spectroscopic means. They are worth of note as rare 22-beta-O-spirostanol glycosides. ...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.53.1122

    authors: Iida Y,Yanai Y,Ono M,Ikeda T,Nohara T

    更新日期:2005-09-01 00:00:00

  • Chiral Calcium-Catalyzed Asymmetric Epoxidation Reactions Using Hydrogen Peroxide as the Terminal Oxidant.

    abstract::Asymmetric epoxidation reactions of chalcone derivatives catalyzed by chiral calcium complexes using hydrogen peroxide were developed. The epoxidation reactions proceeded smoothly to afford the desired products in good yields with good enantioselectivities. This is the first example of chiral calcium-catalyzed asymmet...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.c18-00485

    authors: Yamashita Y,Macor JA,Fushimi S,Tsubogo T,Kobayashi S

    更新日期:2018-01-01 00:00:00

  • Design, Synthesis and Biological Evaluation of Novel Pyrazole Sulfonamide Derivatives as Potential AHAS Inhibitors.

    abstract::Acetohydroxy acid synthase (AHAS; EC 2.2.1.6, also referred to as acetolactate synthase, ALS) has been considered as an attractive target for the design of herbicides. In this work, an optimized pyrazole sulfonamide base scaffold was designed and introduced to derive novel potential AHAS inhibitors by introducing a py...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.c17-00761

    authors: Lv XH,Ren ZL,Liu H,Li HD,Li QS,Wang L,Zhang LS,Yao XK,Cao HQ

    更新日期:2018-01-01 00:00:00

  • Isolation of flavonoids from Populus nigra as delta 4-3-ketosteroid (5 alpha) reductase inhibitors.

    abstract::Inhibitors of delta 4-3-ketosteroid (5 alpha) reductase, which had been prepared from rat prostate and converted testosterone to 5 alpha-dihydrotestosterone and 4-androstene-3,17-dione, were isolated from 50% ethanol extract of Populus nigra. They were identified as pinobanksin (I, 3,5,7-trihydroxyflavanone), 3,7-dime...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.37.3128

    authors: Komoda Y

    更新日期:1989-11-01 00:00:00

  • Antiulcer activities of glycyrrhetinic acid derivatives in experimental gastric lesion models.

    abstract::Glycyrrhetinic acid (Ia) and eighteen related derivatives were examined for antiulcer activity using stress-induced gastric lesions (restraint plus water immersion at 25 degrees C) in mice and rats as screening tests. Among the compounds tested, dihemiphthalate derivatives of 18 alpha- or 18 beta-olean-12-ene-3 beta,3...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.37.2500

    authors: Yano S,Harada M,Watanabe K,Nakamaru K,Hatakeyama Y,Shibata S,Takahashi K,Mori T,Hirabayashi K,Takeda M

    更新日期:1989-09-01 00:00:00

  • Preparation of benzo[b]furans having five-membered heterocycles at the 2-position and 2-(4-Alkylcarbamoylbuta-1,3-dienyl)benzo[b]furans, and their cysteinyl leukotriene receptor (cysLT1, cysLT2) inhibitory activity.

    abstract::A series of benzo[b]furan derivatives having a five-membered heterocyclic substituent at the 2-position were prepared from 2-(1-chloro-2-formylvinyl)benzo[b]furans (2) and 2-(4-alkylcarbamoylbuta-1,3-dienyl)benzo[b]furans. These 2-heterocyclic benzo[b]furans were evaluated for their cysteinyl leukotriene receptor (cys...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.c12-00560

    authors: Akai Y,Tabuchi Y,Ando K,Ito A,Sakata Y,Kawasaki I,Ohishi T,Yamashita M,Ohta S,Nishide K,Ohishi Y

    更新日期:2012-01-01 00:00:00

  • Amino acids and peptides. XXVII. Solid phase synthesis of fibrinogen-related peptides with disulfide bond formed on solid support.

    abstract::Fibrinogen-related peptides, monomeric cyclic peptides through a disulfide bond [cyclo(H-Cys-Arg-Gly-Asp-Phe-Cys-NH2), cyclo(H-Cys-Arg-Gly-Asp-Phe-Cys-Gly-NH2), cyclo(H-Cys-Arg-Gly-Asp-Cys-NH2) and cyclo(H-Cys-Arg-Gly-Asp-Cys-Gly-NH2)], were prepared by the solid phase method with disulfide bond formation on the solid...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.44.1107

    authors: Kakiuchi M,Izuno Y,Maeda M,Ueda K,Fujiwara K,Kunitada S,Kawasaki K

    更新日期:1996-05-01 00:00:00

  • Presence of the basement membrane component--heparan sulfate proteoglycan--in bovine lens capsules.

    abstract::Heparan sulfate proteoglycan was extracted from bovine lens capsules by 0.45 M NaCl/2 M urea and purified using ion-exchange chromatography and gel filtration. The proteoglycan was found to consist of protein and carbohydrate in a ratio of 75 to 25. The estimated average molecular weight of the heparan sulfate proteog...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.39.1059

    authors: Onodera S

    更新日期:1991-04-01 00:00:00

  • Preparation of Cocoa Powder-Containing Orally Disintegrating Tablets of Rebamipide (Rebamipide Chocolet) and Evaluation of Their Clinical Palatability.

    abstract::Orally disintegrating tablets (ODTs), which are administered without water, are beneficial for elderly patients and patients with dysphagia. Masking the unpleasant taste of a drug is an important factor associated with adherence of patients consuming ODTs. We prepared cocoa powder-containing ODTs of bitter-tasting reb...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.c18-00629

    authors: Takano H,Uchida S,Kashiwagura Y,Tanaka S,Hakamata A,Odagiri K,Inui N,Watanabe H,Namiki N

    更新日期:2019-01-01 00:00:00

  • New megastigmane glucosides from Excoecaria cochinchinensis LOUR. var. cochinchinensis.

    abstract::Two new megastigmane glucosides, called excoecariosides A and B were isolated from the leaves of a medicinal Vietnamese plant, Excoecaria cochinchinensis LOUR. var. cochinchinensis (Euphorbiaceae) together with seven known compounds. Their structures were elucidated by spectroscopic analyses and chemical reactions inc...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.53.1600

    authors: Giang PM,Son PT,Matsunami K,Otsuka H

    更新日期:2005-12-01 00:00:00

  • In vitro transport of sodium diclofenac across rat abdominal skin: effect of selection of oleaginous component and the addition of alcohols to the vehicle.

    abstract::The in vitro percutaneous transport of sodium diclofenac from various oil vehicles was examined using rat abdominal skin as a model skin membrane. The overall transport of diclofenac through the skin from the oleaginous vehicles was very poor because of a poor solubility of sodium diclofenac in nonpolar oils. To incre...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.39.154

    authors: Takahashi K,Tamagawa S,Katagi T,Yoshitomi H,Kamada A,Rytting JH,Nishihata T,Mizuno N

    更新日期:1991-01-01 00:00:00

  • Regioselective intramolecular [3+2] annulation of allene-nitrones.

    abstract::The regioselective intramolecular 1,3-dipolar cycloaddition of the phenylsulfonylallene-nitrone derivatives has been developed. This reaction showed that the distal double bond of the allene exclusively reacted with the nitrone group to produce the bicyclic isoxazolidine derivatives regardless of the substitution patt...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.60.381

    authors: Inagaki F,Kobayashi H,Mukai C

    更新日期:2012-01-01 00:00:00

  • Russuphelin A, a new cytotoxic substance from the mushroom Russula subnigricans Hongo.

    abstract::A new cytotoxic substance, designated russuphelin A (1), has been isolated from the mushroom Russula subnigricans Hongo (Basidiomycetes). The structure was elucidated as 2,6-bis(2,6-dichloro-4-hydroxyphenyloxy)-1,4-dimethoxy-benzene on the basis of spectroscopic data and confirmed by total synthesis. ...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.40.3185

    authors: Takahashi A,Agatsuma T,Matsuda M,Ohta T,Nunozawa T,Endo T,Nozoe S

    更新日期:1992-12-01 00:00:00

  • Application of the Lewis acid-Lewis base bifunctional asymmetric catalysts to pharmaceutical syntheses: stereoselective chiral building block syntheses of human immunodeficiency virus (HIV) protease inhibitor and beta3-adenergic receptor agonist.

    abstract::Chiral building block syntheses of promising drugs were achieved using two types of catalytic stereoselective cyanosilylations of aldehydes promoted by Lewis acid-Lewis base bifunctional catalysts 1 and 2 as the key steps (diastereoselective cyanosilylation of amino aldehyde and enantioselective cyanosilylation). In t...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.51.702

    authors: Nogami H,Kanai M,Shibasaki M

    更新日期:2003-06-01 00:00:00

  • First synthesis of a alpha-trifluoromethyl allenol ether via the Julia-Lythgoe process.

    abstract::Alpha-trifluoromethyl allenol ethers 9a-e were prepared in moderate to good yields by the Julia-Lythgoe process using beta-ethoxy-beta-trifluoromethyl vinylic sulfone 3. Several reactions of 9c were examined to give alpha,beta-unsaturated trifluoromethyl ketone derivatives 11 and 12. ...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.48.1395

    authors: Yoshimatsu M,Hibino M

    更新日期:2000-09-01 00:00:00

  • Preparations of cyclic sulfoxide derivatives and their evaluation as transdermal penetration enhancers.

    abstract::Novel cyclic sulfoxides, such as 2-octyl, 2-dodecyl and 2-hexadecyltetrahydrothiophene-1-oxide were prepared by the alkylation of tetrahydrothiophene-1-oxide. Additionally, 2-methyl, 2-ethyl and 2-propyl-5-dodecyltetrahydro-thiophene-1-oxide were conducted by further alkylation. Their enhancing activity on the penetra...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.40.1961

    authors: Aoyagi T,Yamamura M,Matsui K,Nagase Y

    更新日期:1992-07-01 00:00:00

  • Six new cyclic peptides from the roots of Gypsophila oldhamiana.

    abstract::Six new cyclic peptides, gypsophin A-F (1-6), were isolated from Gypsophila oldhamiana. Their structures were elucidated by extensive NMR and chemical degradation. Compound 3 exhibited moderate activity of antiplatelet aggregation in vitro. ...

    journal_title:Chemical & pharmaceutical bulletin

    pub_type: 杂志文章

    doi:10.1248/cpb.c12-01094

    authors: Wang G,Luo JG,Yang MH,Wang XB,Kong LY

    更新日期:2013-01-01 00:00:00