Utility of gastrointestinal physiology regulated-dogs: bioavailability study of a commercial sustained-release dosage form of theophylline.


:The utility of gastrointestinal physiology regulated-dogs (regulated-dogs) was evaluated in a bioavailability study. The gastrointestinal physiology of beagle dogs was regulated with a combined-treatment of intramuscular pentagastrin and intravenous atropine sulfate. Theophylline has been regarded as a drug that is absorbed completely in the entire gastrointestinal tract but slowly in the colon for humans. A commercial sustained-release tablet (SR tablet) of theophylline and a commercial conventional tablet of aminophylline (theophylline hemiethilenediamine salt) were chosen as model preparations in this study. In the regulated-dogs, the drug absorption was almost complete for the conventional tablet. The bioavailability of the SR tablet accounted for 76% in the regulated-dogs and 71% in intact dogs relative to that of the conventional tablet in the regulated-dogs, respectively, but no significant difference was detectable between these values. An advantage of the regulated-dogs over the intact dogs was, however, revealed in the time-profiles of the cumulative percentage of theophylline absorbed from the SR tablet, suggesting a modification of drug absorption by the prolonged arrival of the tablet to the colon.


Biol Pharm Bull


Sagara K,Kawata M,Mizuta H,Shibata M




Has Abstract


1994-07-01 00:00:00












  • Characterization of two novel polysaccharides having immunological activities from the root of Panax ginseng.

    abstract::Two acidic polysaccharides, called ginsenan S-IA and ginsenan S-IIA, were isolated from the root of Panax ginseng C. A. Meyer. They were homogeneous on electrophoresis and gel chromatography, and their molecular masses were estimated to be 5.6 x 10(4) and 1.0 x 10(5), respectively. Ginsenan S-IA is composed of L-arabi...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Tomoda M,Hirabayashi K,Shimizu N,Gonda R,Ohara N,Takada K

    更新日期:1993-11-01 00:00:00

  • Partial hepatectomy enhances polyethylenimine-mediated plasmid DNA delivery.

    abstract::Polyethylenimine (PEI) is widely used for non-viral transfection in vitro and in vivo. Hepatectomy is an interesting and considerable factor modifying PEI-mediated gene expression. We investigated the gene expression in mice over time following partial hepatectomy after an intravenous injection of PEI/plasmid DNA (pDN...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Tada Y,Kitahara T,Yoshioka T,Nakamura T,Ichikawa N,Nakashima M,Nishida K,Nakamura J,Sasaki H

    更新日期:2006-08-01 00:00:00

  • Comparison of the effects of pantethine and fursultiamine on plasma gastrointestinal peptide levels in healthy volunteers.

    abstract::Pantethine and fursultiamine have been evaluated for their clinical usefulness in the treatment and prevention of uncomplicated postoperative adhesive intestinal obstruction. In recent years, the actions of drugs used to treat gastrointestinal diseases have been elucidated pharmacologically from the viewpoints of gast...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 临床试验,杂志文章


    authors: Suzuki Y,Itoh H,Abe T,Nishimura F,Sato Y,Takeyama M

    更新日期:2011-01-01 00:00:00

  • Cyclosporine nanomicelle eye drop: a novel medication for corneal graft transplantation treatment.

    abstract::Corneal transplantation has been used to treat severe eye disease for decades, but the therapeutic effect of the operation is highly compromised by immunological allograft rejection. To improve the success rate of corneal transplantation, we studied the protective effects of cyclosporine nanomicelle eye drops (CNED) o...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Zhang H,Wang L,Zhang L

    更新日期:2015-01-01 00:00:00

  • Effects of Ramelteon and Other Sleep-Promoting Drugs on Serum Low-Density Lipoprotein and Non-high-density Lipoprotein Cholesterol: A Retrospective Comparative Pilot Study.

    abstract::Melatonin has been suggested to play important roles in lipid metabolism as well as circadian rhythm; however, very few studies explored the effects of ramelteon, a selective melatonin receptor agonist, on serum lipid profiles. In this study effects of ramelteon on serum lipid profiles were explored, comparing to thos...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Torii H,Shimizu R,Tanizaki Y,Omiya Y,Yamamoto M,Kamiike S,Yasuda D,Hiraoka Y,Hashida T,Kume N

    更新日期:2018-01-01 00:00:00

  • Identification of in vitro metabolites of 2,4,6,2',4',6'-hexachlorobiphenyl from phenobarbital-treated dog liver microsomes.

    abstract::We studied in vitro metabolites of 2,4,6,2',4',6'-hexachlorobiphenyl (HCB, IUPAC PCB No. 155) produced by liver microsomes of a phenobarbital (PB)-treated beagle dog. The major metabolites were 3-hydroxy-2,4,6,2',4',6'-HCB (M-1), 4-hydroxy-2,6,2',4',6'-pentachlorobiphenyl (PenCB, M-2) and 3,4-dihydroxy-2,6,2',4',6'-Pe...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Ariyoshi N,Yoshimura H,Oguri K

    更新日期:1993-09-01 00:00:00

  • Effect of mizoribine on effector T cell-mediated immune responses in mice.

    abstract::T cells play a principal role in cellular immunity and govern the regulatory mechanism in humoral immunity. Therefore, T cells play a key role as either effectors or regulators in the immune network. Mizoribine (MZR), an immunosuppressive agent, suppresses both humoral and cellular immunity by acting on both T cells a...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Kamada H,Inoue N,Takaoka Y,Nakagami K,Mori H,Nagai H

    更新日期:1996-09-01 00:00:00

  • Obligatory Role of Early Ca(2+) Responses in H2O2-Induced β-Cell Apoptosis.

    abstract::Our previous study using apoptosis analysis suggested that Ca(2+) release through inositol 1,4,5-trisphosphate (IP3) receptors and the subsequent Ca(2+) influx through store-operated channels (SOCs) constitute a triggering signal for H2O2-induced β-cell apoptosis. In the present study, we further examined the obligato...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Sato T,Kaneko YK,Sawatani T,Noguchi A,Ishikawa T

    更新日期:2015-01-01 00:00:00

  • Organ specific expression of thyroid hormone receptor mRNA and protein in different human tissues.

    abstract::The major physiologic effect of thyroid hormone is thought to be initiated by the binding of T3 to the DNA binding thyroid hormone receptor (TR). The aim of this study has been to characterize the organ specific expression of thyroid hormone receptor mRNA, as well as its protein distribution and molecular weight in ma...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Shahrara S,Drvota V,Sylvén C

    更新日期:1999-10-01 00:00:00

  • Glycerol absorption by Na+-dependent carrier-mediated transport in the closed loop of the rat small intestine.

    abstract::The absorption of glycerol was examined using the closed loop of the rat small intestine in situ to clarify the transport mechanism. The absorption of glycerol, evaluated by its disappearance from the intestinal lumen, was saturable and reduced under the Na(+)-free conditions, suggesting the involvement of an Na(+)-de...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Kato T,Hayashi Y,Inoue K,Yuasa H

    更新日期:2005-03-01 00:00:00

  • Vasodilatation produced by orientin and its mechanism study.

    abstract::In this paper we investigated the vascular activity and possible mechanism of Orientin, from bamboo leaves (Phyllostachys nigra), in isolated thoracic aortic rings from New Zealand rabbit. Among the four compounds, studied, only Orientin relaxed phenylephrine-induced contractions with an IC50 value of 2.28 microM in t...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Fu XC,Wang MW,Li SP,Zhang Y,Wang HL

    更新日期:2005-01-01 00:00:00

  • First-pass metabolism of 5-fluorouracil in the perfused rat small intestine.

    abstract::The first-pass intestinal metabolism of 5-fluorouracil (5-FU) was investigated by single-pass perfusion of the rat small intestine. At the low concentration of 0.06 mg/ml, the fraction of 5-FU absorbed into (i.e., appeared in) the mesenteric venous blood (Fa,b) was about 50% smaller than the fraction absorbed (disappe...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Gu J,Yuasa H,Hayashi Y,Watanabe J

    更新日期:1998-08-01 00:00:00

  • Liposomal Delivery Systems: Design Optimization and Current Applications.

    abstract::The liposome, a closed phospholipid bilayered vesicular system, has received considerable attention as a pharmaceutical carrier of great potential over the past 30 years. The ability of liposomes to encapsulate both hydrophilic and hydrophobic drugs, coupled with their biocompatibility and biodegradability, make lipos...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章,评审


    authors: Abu Lila AS,Ishida T

    更新日期:2017-01-01 00:00:00

  • Studies on interactions between functional foods or dietary supplements and medicines. III. Effects of ginkgo biloba leaf extract on the pharmacokinetics of nifedipine in rats.

    abstract::The effects of Ginkgo biloba leaf extract (GBE), one of the most widely used herbal dietary supplements in Japan and the United States, on the pharmacokinetics of nifedipine (NFP), a typical probe of P450 (CYP) 3A, but not a substrate of the multidrug transporter P-glycoprotein (P-gp), were studied using rats. Simulta...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Yoshioka M,Ohnishi N,Sone N,Egami S,Takara K,Yokoyama T,Kuroda K

    更新日期:2004-12-01 00:00:00

  • Intracellular and extracellular redox environments surrounding redox-sensitive contrast agents under oxidative Atmosphere.

    abstract::In vivo redox reactions of nitroxyl contrast agents in bile and blood under an oxidative atmosphere were investigated using normal healthy Wistar rats. Differences in intracellular and extracellular volumes in redox environments are discussed. Pharmacokinetic profiles of two nitroxyl contrast agents, 3-carbamoyl-2,2,5...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Okajo A,Ui I,Manda S,Nakanishi I,Matsumoto K,Anzai K,Endo K

    更新日期:2009-04-01 00:00:00

  • Telekin induces apoptosis associated with the mitochondria-mediated pathway in human hepatocellular carcinoma cells.

    abstract::Telekin, a eudesmane-type sesquiterpene lactone compound isolated from Chinese folk medicine Carpesium divaricatum, has been reported to strongly inhibit the proliferation of cancer cells. In this study, the involvement of a mitochondria-mediated pathway in the pro-apoptotic action of telekin was investigated in human...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Zheng B,Wu L,Ma L,Liu S,Li L,Xie W,Li X

    更新日期:2013-01-01 00:00:00

  • Synergistic enhancement of nitrite on lysophospholipid-mediated cytolysis.

    abstract::Nitrogen oxide, which is produced by activated macrophages, has been demonstrated to possess anti-tumor activity. We report herein the synergistic effect of sodium nitrite (NO2-) and/or sodium nitroprusside (SNP) on lysophospholipid (LysoPL)-mediated cytolysis. The incubation of 51Cr-labeled mouse melanoma (B16) cells...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Kanematsu M,Takagi K,Suketa Y

    更新日期:1994-01-01 00:00:00

  • Methanol extract of Xanthium strumarium L. possesses anti-inflammatory and anti-nociceptive activities.

    abstract::As an attempt to identify bioactive natural products with anti-inflammatory activity, we evaluated the effects of the methanol extract of the semen of Xanthium strumarium L. (MEXS) on lipopolysaccharide (LPS)-induced nitric oxide (NO), prostaglandin E2 (PGE2) and tumor necrosis factor-alpha (TNF-alpha) production in R...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Kim IT,Park YM,Won JH,Jung HJ,Park HJ,Choi JW,Lee KT

    更新日期:2005-01-01 00:00:00

  • Influence of coadministered antiepileptic drugs on serum phenobarbital concentrations in epileptic patients: quantitative analysis based on a suitable transforming factor.

    abstract::This study investigated most suitable transforming factor related to the daily Phenobarbital dose (D) providing a steady-state serum concentration (Ct) and analyzed the influences of concomitant antiepileptic drugs on Ct quantitatively. Data obtained by routine therapeutic drug monitoring from a total of 326 epileptic...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章,多中心研究


    authors: Fukuoka N,Tsukamoto T,Uno J,Kimura M,Morita S

    更新日期:2004-12-01 00:00:00

  • Effect of psychotropic drugs on the 21-hydroxylation of neurosteroids, progesterone and allopregnanolone, catalyzed by rat CYP2D4 and human CYP2D6 in the brain.

    abstract::We determined the effects of psychotropic drugs on the cytochrome P450 2D (CYP2D)-mediated 21-hydroxylation of progesterone (PROG) and allopregnanolone (ALLO) with the goal of clarifying whether neurosteroid levels are affected by psychotropic drugs in the brain. PROG or ALLO was incubated with rat CYP2D4 or human CYP...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Niwa T,Okada K,Hiroi T,Imaoka S,Narimatsu S,Funae Y

    更新日期:2008-03-01 00:00:00

  • Panaxydol Derived from Panax ginseng Inhibits G1 Cell Cycle Progression in Non-small Cell Lung Cancer via Upregulation of Intracellular Ca2+ Levels.

    abstract::Panaxydol, a polyacetylenic compound derived from Panax ginseng has been reported to suppress the growth of cancer cells. However, the molecular mechanisms underlying cell cycle arrest by this compound in non-small cell lung cancer (NSCLC) are unknown. Our study found that panaxydol treatment induced cell cycle arrest...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Lee JH,Leem DG,Chung KS,Kim KT,Choi SY,Lee KT

    更新日期:2018-01-01 00:00:00

  • O/W lipid emulsions for parenteral drug delivery. I. Pharmacokinetics of the oil particles and incorporated sudan II.

    abstract::The potential usefulness of oil in water (O/W) lipid emulsions as parenteral drug delivery system for lipophilic drugs was examined in tumor-bearing rats. A model lipophilic drug, sudan II (PCoct = 226000), was formulated in five lipid emulsions consisting of soybean oil and various surfactants. Compared with HCO-60 m...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Sakaeda T,Takahashi K,Nishihara Y,Hirano K

    更新日期:1994-11-01 00:00:00

  • Purification and determination of the chemical structure of the tyrosinase inhibitor produced by Trichoderma viride strain H1-7 from a marine environment.

    abstract::Tyrosinase is a key enzyme in the synthesis of melanin and is widely distributed in animals, plants, and microorganisms. As excessive melanin production causes not only hyperpigmenting effects on human skin but also melanosis in various foods, an inhibitor of tyrosinase has become of interest lately from a practical p...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Tsuchiya T,Yamada K,Minoura K,Miyamoto K,Usami Y,Kobayashi T,Hamada-Sato N,Imada C,Tsujibo H

    更新日期:2008-08-01 00:00:00

  • Adhesion of enterohemorrhagic Escherichia coli O157:H7 to the intestinal epithelia is essential for inducing secretory IgA antibody production in the intestine of mice.

    abstract::We examined whether adherence of enterohemorrhagic Escherichia coli (EHEC) O157:H7 to intestinal epithelial cells contributed to the induction of secretory immunoglobulin A (IgA) antibody production in mice. Wild-type EHEC O157:H7 and its mutants deficient in the espA, sepL, tir and eae genes, encoding adherent factor...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Nagano K,Taguchi K,Tokoro S,Tatsuno I,Mori H

    更新日期:2014-01-01 00:00:00

  • Quercetin but not quercitrin ameliorates tumor necrosis factor-alpha-induced insulin resistance in C2C12 skeletal muscle cells.

    abstract::Skeletal muscle is a major site for glucose metabolism and its injury by cytokines can induce insulin resistance leading to type 2 diabetes. It has been suggested that quercetin may act as an anti-diabetic agent, however, the effects of quercetin on insulin resistance in skeletal muscle remain unknown. We aimed to inv...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Dai X,Ding Y,Zhang Z,Cai X,Bao L,Li Y

    更新日期:2013-01-01 00:00:00

  • Cytotoxic activity of bryonolic acid isolated from transformed hairy roots of Trichosanthes kirilowii var. japonica.

    abstract::Bryonolic acid was isolated in high yield from transformed hairy root cultures of Trichosanthes kirilowii var. Japonica. Bryonolic acid exhibited cytotoxic activity to various tumor cells in vitro, independent of cell type. Normal cells such as rat hepatocytes are less sensitive to bryonolic acid. The appearance of a ...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Kondo T,Inoue M,Mizukami H,Ogihara Y

    更新日期:1995-05-01 00:00:00

  • TJN-331 improves anti-glomerular basement membrane nephritis by inhibiting the production of intraglomerular transforming growth factor-beta1.

    abstract::Transforming growth factor-beta1 (TGF-beta1) plays an important role in the development of glomerulonephritis. The study of experimental glomerulonephritis in rats was performed to examine the antinephritic effects of TJN-331, a new herbally-derived chemical compound. To clarify the action of TJN-331 ((E)-N-(3,4-dimet...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Saegusa Y,Sadakane C,Koseki J,Hasegawa Y,Shindo S,Maruyama H,Takeda S,Takeda H,Hattori T

    更新日期:2010-01-01 00:00:00

  • ECa 233 Suppresses LPS-Induced Proinflammatory Responses in Macrophages via Suppressing ERK1/2, p38 MAPK and Akt Pathways.

    abstract::A current anti-inflammatory agent often targets the prevention of inflammatory disorder development. The standardized Centella asiatica ECa 233 extract has been previously reported for anti-inflammatory effect. This study aimed to investigate its anti-inflammatory effect and mechanisms of ECa 233 in lipopolysaccharide...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Sukketsiri W,Tanasawet S,Moolsap F,Tantisira MH,Hutamekalin P,Tipmanee V

    更新日期:2019-01-01 00:00:00

  • Induction of CD4+ regulatory T cells by TPA in mice: contra-suppression by CD8+ T cells.

    abstract::Among the eight inbred mouse strains employed in our preceding report, 12-O-tetradecanoylphorbol 13-acetate (TPA) painting alone induced CD4+ regulatory T (Tr) cells in four strains (e.g., C3H/He) at 6-8 weeks of age, but not in the remaining strains (e.g., C57BL/6, BALB/c). In the present study, the effect of growth ...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Negoro T,Satoh K,Iinuma F,Tobe T,Watanabe M

    更新日期:2002-02-01 00:00:00

  • Site-directed mutagenesis of the serotonin 5-Hydroxytryptamine2c receptor: identification of amino acids responsible for sarpogrelate binding.

    abstract::Site-directed mutagenesis was used to investigate the molecular interactions involved in sarpogrelate binding to the human 5-Hydroxytryptamine(5-HT)2C receptor. Based on molecular modeling studies, Aspartic acid (Asp)155[3.32] in transmembrane region III and Serine(Ser)361[7.46] in transmembrane region VII of the 5-HT...

    journal_title:Biological & pharmaceutical bulletin

    pub_type: 杂志文章


    authors: Muntasir HA,Takahashi J,Rashid M,Ahmed M,Komiyama T,Hossain M,Kawakami J,Nashimoto M,Nagatomo T

    更新日期:2006-08-01 00:00:00