A novel evaluation method of gastric mucoadhesive property in vitro and the mucoadhesive mechanism of tetracycline-sucralfate acidic complex for eradication of Helicobacter pylori.

Abstract:

PURPOSE:The gastric mucoadhesive property of tetracycline-sucralfate acidic complex (CO) was evaluated by using a novel method in vitro to compare with the in vivo test. The mucoadhesive mechanism of the acidic complex was also studied. METHODS:The gastric mucosa removed from a rat was placed covering the end of a plunger and secured in a disposable syringe. The acidic test medium was gradually infused in and then flowed out. Two different kinds of CO, tetracycline, or a physical mixture (PM) were introduced into the device to compare their mucoadhesive properties. The tetracycline content in the residue on the mucosa was measured. The results were compared with those of the in vivo test. The acidic response of CO and the protein binding capacity of a sucrose octasulfate group (SOS) in sucralfate or CO were evaluated. RESULTS:The mucoadhesive properties of CO were clearly superior to those of PM. The remaining amounts of tetracycline in each test sample, determined by the in vitro test, were in agreement with those of the in vivo test. The excellent mucoadhesive property of CO appeared to be caused by the rapid response to the acid and resulting mucoadhesive gel formation. Furthermore, the binding capacity of SOS to the protein was clearly greater than that of PM. The excessive acid treatment during the preparation of CO tended to decrease the mucoadhesive property. CONCLUSIONS:CO appeared to be potentially useful for the eradication of Helicobacter pylori because of the direct delivery of tetracycline to the gastric mucosa for an extended period of time.

journal_name

Pharm Res

journal_title

Pharmaceutical research

authors

Higo S,Ori K,Takeuchi H,Yamamoto H,Hino T,Kawashima Y

doi

10.1023/B:PHAM.0000019293.57927.7f

subject

Has Abstract

pub_date

2004-03-01 00:00:00

pages

413-9

issue

3

eissn

0724-8741

issn

1573-904X

journal_volume

21

pub_type

杂志文章
  • Optimizing iontophoretic drug delivery: identification and distribution of the charge-carrying species.

    abstract:PURPOSE:To identify and quantify, in vitro and in vivo (in humans), the charge-carrying species during transdermal iontophoresis of lidocaine hydrochloride as a function of the concentration of drug relative to that of sodium chloride in the anodal solution. METHODS:In vitro experiments in standard diffusion cells qua...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1013370529366

    authors: Marro D,Kalia YN,Delgado-Charro MB,Guy RH

    更新日期:2001-12-01 00:00:00

  • Glycine crystallization during freezing: the effects of salt form, pH, and ionic strength.

    abstract:PURPOSE:The purpose of the study is to characterize glycine crystallization during freezing of aqueous solutions as a function of the glycine salt form (i.e., neutral glycine, glycine hydrochloride, and sodium glycinate), pH, and ionic strength. METHODS:Crystallization was studied by thermal analysis, microscopy, x-ra...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1016223101872

    authors: Akers MJ,Milton N,Byrn SR,Nail SL

    更新日期:1995-10-01 00:00:00

  • A novel peptide nanomedicine against acute lung injury: GLP-1 in phospholipid micelles.

    abstract:PURPOSE:Treatment of acute lung injury (ALI) observed in Gram-negative sepsis represents an unmet medical need due to a high mortality rate and lack of effective treatment. Accordingly, we developed and characterized a novel nanomedicine against ALI. We showed that when human glucagon-like peptide 1(7-36) (GLP-1) self-...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-010-0322-4

    authors: Lim SB,Rubinstein I,Sadikot RT,Artwohl JE,Önyüksel H

    更新日期:2011-03-01 00:00:00

  • Evaluation of an enzyme-containing capsular shaped pulsatile drug delivery system.

    abstract:PURPOSE:To develop an enzymatically-controlled pulsatile drug release system based on an impermeable capsule body, which contains the drug and is closed by an erodible pectin/pectinase-plug. METHODS:The plug was prepared by direct compression of pectin and pectinase in different ratios. In addition to the disintegrati...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1018959327311

    authors: Krögel I,Bodmeier R

    更新日期:1999-09-01 00:00:00

  • Selegiline percutaneous absorption in various species and metabolism by human skin.

    abstract:PURPOSE:A Selegiline Transdermal System (STS) is under development for indications which may not be optimally or safely treated with oral selegiline. Studies were conducted to evaluate the in vitro penetration and skin metabolism of selegiline in order to better understand the toxicological findings and the observed pl...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1012051300130

    authors: Rohatagi S,Barrett JS,McDonald LJ,Morris EM,Darnow J,DiSanto AR

    更新日期:1997-01-01 00:00:00

  • Tuning the Physicochemical Characteristics of Particle-Based Carriers for Intraperitoneal Local Chemotherapy.

    abstract::Over the last few decades, intraperitoneal (IP) local drug delivery, providing high drug concentrations with prolonged retention in the peritoneal cavity, has opened a new horizon for the management of life-threatening peritoneal disorders, such as peritoneal carcinomatosis (PC). However, clinical translation of this ...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章,评审

    doi:10.1007/s11095-020-02818-8

    authors: Alavi S,Haeri A,Mahlooji I,Dadashzadeh S

    更新日期:2020-06-03 00:00:00

  • Release of plasmid DNA-encoding IL-10 from PLGA microparticles facilitates long-term reversal of neuropathic pain following a single intrathecal administration.

    abstract:PURPOSE:Interleukin-10 (IL-10) is an anti-inflammatory molecule that has achieved interest as a therapeutic for neuropathic pain. In this work, the potential of plasmid DNA-encoding IL-10 (pDNA-IL-10) slowly released from biodegradable microparticles to provide long-term pain relief in an animal model of neuropathic pa...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-010-0077-y

    authors: Soderquist RG,Sloane EM,Loram LC,Harrison JA,Dengler EC,Johnson SM,Amer LD,Young CS,Lewis MT,Poole S,Frank MG,Watkins LR,Milligan ED,Mahoney MJ

    更新日期:2010-05-01 00:00:00

  • Effects of configuration around the chiral carbon atoms on the crystal properties of ephedrinium and pseudoephedrinium salicylates.

    abstract::The physicochemical properties and crystal structures of the crystalline salts formed by the interaction of an achiral anion, salicylate, with homochiral and racemic ephedrinium and pseudoephedrinium cations were determined. The interaction of ephedrinium or pseudoephedrinium with salicylate in aqueous solution yielde...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1018945401484

    authors: Duddu SP,Grant DJ

    更新日期:1994-11-01 00:00:00

  • Tilorone: a Broad-Spectrum Antiviral Invented in the USA and Commercialized in Russia and beyond.

    abstract::For the last 50 years we have known of a broad-spectrum agent tilorone dihydrochloride (Tilorone). This is a small-molecule orally bioavailable drug that was originally discovered in the USA and is currently used clinically as an antiviral in Russia and the Ukraine. Over the years there have been numerous clinical and...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-020-02799-8

    authors: Ekins S,Lane TR,Madrid PB

    更新日期:2020-03-25 00:00:00

  • A fractal approach to heterogeneous drug distribution: calcium pharmacokinetics.

    abstract:PURPOSE:To point out the importance of heterogeneity in drug distribution processes and develop a noncompartmental approach for the description of the distribution of drug in the body. METHODS:A dichotomous branching network of vessels for the arterial tree connected to a similar venous network was used to describe th...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1016031129053

    authors: Macheras P

    更新日期:1996-05-01 00:00:00

  • Design and characterization of a novel fluorinated magnetic resonance imaging agent for functional analysis of bile Acid transporter activity.

    abstract:PURPOSE:To synthesize a trifluorinated bile acid that can be used for (19)F magnetic resonance imaging (MRI) of bile acid enterohepatic circulation, characterize its in vitro transporter affinity, stability, and (19)F-MRI signal, and assess its ability to concentrate in the gallbladder of C57BL/6 mice. METHODS:Target ...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-012-0963-6

    authors: Vivian D,Cheng K,Khurana S,Xu S,Whiterock V,Witter D,Lentz KA,Santone KS,Raufman JP,Polli JE

    更新日期:2013-05-01 00:00:00

  • Vaccine delivery to the oral cavity using coated microneedles induces systemic and mucosal immunity.

    abstract:PURPOSE:The objective of this study is to evaluate the feasibility of using coated microneedles to deliver vaccines into the oral cavity to induce systemic and mucosal immune responses. METHOD:Microneedles were coated with sulforhodamine, ovalbumin and two HIV antigens. Coated microneedles were inserted into the inner...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-014-1335-1

    authors: Ma Y,Tao W,Krebs SJ,Sutton WF,Haigwood NL,Gill HS

    更新日期:2014-09-01 00:00:00

  • Enhanced delivery of 5-iodo-2'-deoxyuridine to the brain parenchyma.

    abstract::5'-Ester derivatives of 5-iodo-2'-deoxyuridine (IDU) with varying degrees of lipophilicity were examined to evaluate the effectiveness of lipophilic ester prodrugs for enhanced and sustained delivery of IDU to the brain parenchyma. Approximately 1.0% (1.0 +/- 0.19; n = 4) of the total radioactivity was found in the br...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1015803922401

    authors: Ghosh MK,Mitra AK

    更新日期:1992-09-01 00:00:00

  • Synergistic effect of formulated plasmid and needle-free injection for genetic vaccines.

    abstract:PURPOSE:A plasmid-based gene expression system was complexed with protective, interactive, and non-condensing (PINC) polymer system and administered with Medi-Jector, a needle-free injection device (NFID), to achieve high and sustained levels of antigen-specific antibodies in blood circulation. METHODS:Human growth ho...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1018834305079

    authors: Anwer K,Earle KA,Shi M,Wang J,Mumper RJ,Proctor B,Jansa K,Ledebur HC,Davis S,Eaglstein W,Rolland AP

    更新日期:1999-06-01 00:00:00

  • Molecular structure and dynamics of cis(Z)-and trans(E)-flupenthixol and clopenthixol.

    abstract::The three-dimensional structures and molecular electrostatic potentials of the cis(Z) and trans(E)-isomers of flupenthixol and clopenthixol were examined by computer graphics and molecular mechanical and quantum mechanical calculations, and their internal molecular motions were studied by molecular dynamics simulation...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1015842926345

    authors: Sylte I,Dahl SG

    更新日期:1991-04-01 00:00:00

  • p-Aminohippurate transport at the apical membrane in the OK kidney epithelial cell line.

    abstract:PURPOSE:We investigated the characteristics of transport of an organic anion, p-aminohippurate (PAH), at the apical membrane in a kidney epithelial cell line OK. METHODS:Efflux and uptake of [14C]PAH across the apical membrane were measured using OK cell monolayers grown on microporous membrane filters. RESULTS:PAH e...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1021437306990

    authors: Habu Y,Yano I,Hashimoto Y,Saito H,Inui K

    更新日期:2002-12-01 00:00:00

  • Stability and solubility of celecoxib-PVP amorphous dispersions: a molecular perspective.

    abstract:PURPOSE:The purpose of the current study is to evaluate the solubility advantage offered by celecoxib (CEL) amorphous systems and to characterize and correlate the physical and thermodynamic properties of CEL and its amorphous molecular dispersions containing poly(vinylpyrrolidone) (PVP). METHODS:The measurement of cr...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/b:pham.0000045226.42859.b8

    authors: Gupta P,Kakumanu VK,Bansal AK

    更新日期:2004-10-01 00:00:00

  • In Silico Predictions of Human Skin Permeability using Nonlinear Quantitative Structure-Property Relationship Models.

    abstract:PURPOSE:Predicting human skin permeability of chemical compounds accurately and efficiently is useful for developing dermatological medicines and cosmetics. However, previous work have two problems; 1) quality of databases used, and 2) methods for prediction models. In this paper, we attempt to solve these two problems...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-015-1629-y

    authors: Baba H,Takahara J,Mamitsuka H

    更新日期:2015-07-01 00:00:00

  • Effects of excipients on protein conformation in lyophilized solids by hydrogen/deuterium exchange mass spectrometry.

    abstract:PURPOSE:Excipients are added to lyophilized protein drug formulations to protect the protein during processing and storage, but the mechanisms are poorly understood. Here, hydrogen/deuterium (H/D) exchange with mass spectrometry was used to assess protein conformation and excipient interactions in lyophilized solids. ...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-007-9365-6

    authors: Li Y,Williams TD,Topp EM

    更新日期:2008-02-01 00:00:00

  • Exploring Variation in Known Pharmacogenetic Variants and its Association with Drug Response in Different Mexican Populations.

    abstract:PURPOSE:Information on genetic variants that affect the pharmacokinetics and pharmacodynamics (PK/PD) of drugs in different populations from Mexico is still an ongoing endeavor. Here, we investigate allele frequencies on pharmacogenetic targets in Mexican Mestizos and Natives from three different States and its associa...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-016-1990-5

    authors: Gonzalez-Covarrubias V,Martínez-Magaña JJ,Coronado-Sosa R,Villegas-Torres B,Genis-Mendoza AD,Canales-Herrerias P,Nicolini H,Soberón X

    更新日期:2016-11-01 00:00:00

  • Enhanced oral delivery of curcumin from N-trimethyl chitosan surface-modified solid lipid nanoparticles: pharmacokinetic and brain distribution evaluations.

    abstract:PURPOSE:Solid lipid nanoparticles (SLNs) have been proposed as a colloidal carrier system that could enhance the oral bioavailability of curcumin. However, a burst release of the loaded drug, which occurs in acidic environments, has been a main obstacle to the oral delivery of curcumin by using SLNs as a carrier system...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-014-1469-1

    authors: Ramalingam P,Ko YT

    更新日期:2015-02-01 00:00:00

  • Scale of health: indices of safety and efficacy in the evolving environment of large biological datasets.

    abstract::The interdependent relationship between pharmacology and toxicology is fundamental to the concepts of efficacy and safety of both drugs and xenobiotics. The traditional concept of establishing efficacious and tolerated doses to define a 'therapeutic window' appears simplistic in the context of an exponentially increas...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章,评审

    doi:10.1007/s11095-014-1415-2

    authors: Sayes CM,Staats H,Hickey AJ

    更新日期:2014-09-01 00:00:00

  • Route of administration and sex differences in the pharmacokinetics of aspirin, administered as its lysine salt.

    abstract::One thousand milligrams of aspirin, as its lysine salt was administered intravenously, orally, and intramuscularly to nine male and nine female young healthy adult volunteers. After intravenous injection mean (+/- SD) values of clearance, steady-state volume of distribution, and terminal half-life were 12.2 +/- 2.2 ml...

    journal_title:Pharmaceutical research

    pub_type: 临床试验,杂志文章

    doi:10.1023/a:1015978104017

    authors: Aarons L,Hopkins K,Rowland M,Brossel S,Thiercelin JF

    更新日期:1989-08-01 00:00:00

  • Reversal of signs of induced cotton effects of dicumarol-alpha 1-acid glycoprotein systems by phenothiazine neuroleptics through ternary complexation.

    abstract::The interaction of dicumarol and phenothiazine neuroleptics binding to alpha 1-acid glycoprotein (AGP) was investigated by circular dichroism (CD) and equilibrium dialysis. The induced CD spectra of the dicumarol-AGP complex were affected differently by the different substituents of the phenothiazine molecule. The sig...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1015880327911

    authors: Miyoshi T,Yamamichi R,Maruyama T,Otagiri M

    更新日期:1992-07-01 00:00:00

  • Pharmaceutical properties of loracarbef: the remarkable solution stability of an oral 1-carba-1-dethiacephalosporin antibiotic.

    abstract::Loracarbef is an oral 1-carba-1-dethiacephalosporin antibiotic structurally related to cefaclor. Like many beta-lactam antibiotics, loracarbef exists in several hydrated crystalline forms. The pH-solubility profile curve for loracarbef monohydrate is U-shaped, resembling those of other zwitterionic cephalosporins. Lor...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1018949709797

    authors: Pasini CE,Indelicato JM

    更新日期:1992-02-01 00:00:00

  • Crystallization kinetics of amorphous griseofulvin by pattern fitting procedure using X-ray diffraction data.

    abstract:PURPOSE:A pattern fitting procedure using X-ray powder diffraction patterns was applied to study the crystallization kinetics of amorphous griseofulvin. From the optimized parameters obtained by pattern fitting, a change in the quantity and quality of griseofulvin crystals with crystallization was also investigated. M...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-006-9204-1

    authors: Yamamura S,Takahira R,Momose Y

    更新日期:2007-05-01 00:00:00

  • High Content Solid Dispersions for Dose Window Extension: A Basis for Design Flexibility in Fused Deposition Modelling.

    abstract:PURPOSE:This study uses high drug content solid dispersions for dose window extension beyond current demonstrations using fused deposition modelling (FDM) to; i) accommodate pharmaceutically relevant doses of drugs of varying potencies at acceptable dosage form sizes and ii) enable enhanced dose flexibility via modular...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-019-2720-6

    authors: Govender R,Abrahmsén-Alami S,Folestad S,Larsson A

    更新日期:2019-12-17 00:00:00

  • Effect of cyclodextrins on protein binding of drugs: the diflunisal/hydroxypropyl-beta-cyclodextrin model case.

    abstract::The binding of diflunisal to hydroxypropyl-beta-cyclodextrin (HP beta CD), bovine serum albumin (BSA), human serum albumin (HSA), normal human plasma, and mixed solutions of HP beta CD/protein was studied at 25 degrees C, pH 7.4, by potentiometry using an electrode selective to diflunisal. The experimental data for di...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1018901912619

    authors: Sideris EE,Koupparis MA,Macheras PE

    更新日期:1994-01-01 00:00:00

  • Differential molar heat capacities to test ideal solubility estimations.

    abstract:PURPOSE:Calculation of the ideal solubility of a crystalline solute in a liquid solvent requires knowledge of the difference in the molar heat capacity at constant pressure of the solid and the supercooled liquid forms of the solute, delta Cp. Since this parameter is not usually known, two assumptions have been used to...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1012148910975

    authors: Neau SH,Bhandarkar SV,Hellmuth EW

    更新日期:1997-05-01 00:00:00

  • Changes of Blood-Brain Barrier and Brain Parenchymal Protein Expression Levels of Mice under Different Insulin-Resistance Conditions Induced by High-Fat Diet.

    abstract:PURPOSE:The purpose of the present study was to investigate changes of blood-brain barrier (BBB) and brain parenchymal protein expression due to type II diabetes mellitus (T2DM) induced by a high-fat diet (HFD) by using SWATH-based quantitative proteomics. METHODS:Mice were fed a HFD for 2 or 10 weeks, and then SWATH-...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-019-2674-8

    authors: Ogata S,Ito S,Masuda T,Ohtsuki S

    更新日期:2019-07-31 00:00:00