Abstract:
:Azo polymers based upon 2-hydroxyethyl methacrylate, methyl methacrylate, and methacrylic acid, and containing N,N'-bis [(methacryloyloxyethyl)oxy(carbonylamino)]azobenzene as azo aromatic agent were evaluated in vivo as coating for colon-specific drug delivery. The gastrointestinal absorption of theophylline from capsules coated with the azo polymers was examined in the proximal part of the small intestine and the cecum of male Wistar rats. The capsules were surgically inserted in the region of interest. The plasma concentration of the drug was higher when the capsules were inserted in the cecum as compared to the small intestine. The appearance of theophylline in the plasma when capsules were administered in the small intestine can be attributed to simple diffusion of the drug through the swollen polymer coating. Release and absorption from the cecum is the combined results of diffusion and degradation of the azo polymer coatings by bacterial azo reductase.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Van den Mooter G,Samyn C,Kinget Rdoi
10.1023/a:1016283027139subject
Has Abstractpub_date
1995-02-01 00:00:00pages
244-7issue
2eissn
0724-8741issn
1573-904Xjournal_volume
12pub_type
杂志文章abstract:PURPOSE:The trial-and-error approach is still predominantly used in pharmaceutical development of nanosuspensions. Physicochemical dispersion stability is a primary focus and therefore, various analytical bulk methods are commonly employed. Clearly less attention is directed to surface changes of nanoparticles even tho...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-017-2300-6
更新日期:2018-02-21 00:00:00
abstract:PURPOSE:The stability of lipid emulsions (LE) containing various cosurfactants (oleic acid, cholesterol, Tween 80, or HCO-60) was evaluated using the maximum total interaction energy, Vtmax and the energy barrier for coalescence, W. METHODS:The Vtmax and W were calculated from the zeta potential and the rate of increa...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016205203264
更新日期:1995-09-01 00:00:00
abstract:PURPOSE:A mechanism-based PK-PD model was developed to predict the time course of dopamine D(2) receptor occupancy (D(2)RO) in rat striatum following administration of olanzapine, an atypical antipsychotic drug. METHODS:A population approach was utilized to quantify both the pharmacokinetics and pharmacodynamics of ol...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-011-0477-7
更新日期:2011-10-01 00:00:00
abstract:PURPOSE:Ultrasound can be used to release a therapeutic payload encapsulated within a perfluorocarbon (PFC) emulsion via acoustic droplet vaporization (ADV), a process whereby the PFC phase is vaporized and the agent is released. ADV-generated microbubbles have been previously used to selectively occlude blood vessels ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-010-0277-5
更新日期:2010-12-01 00:00:00
abstract::The stability of an antibiotic formulation (clindamycin phosphate in dextrose), which is stable at room temperature, was assessed by nonisothermal kinetic analysis at elevated temperatures. A preliminary study, conducted to establish apparent rate order, verified the appropriateness of a first-order kinetic model. The...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015840320410
更新日期:1991-05-01 00:00:00
abstract:PURPOSE:A major challenge facing nanoparticle-based delivery of chemotherapy agents is the natural and unavoidable accumulation of these particles in healthy tissue resulting in local toxicity and dose-limiting side effects. To address this issue, we have designed and characterized a new prodrug nanoparticle with contr...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-017-2205-4
更新日期:2017-10-01 00:00:00
abstract:PURPOSE:Poly-L-arginine (PLA) enhances the paracellular permeability of the Caco-2 cell monolayer to hydrophilic macromolecules by disappearance of tight junction (TJ) proteins from cell-cell junctions. However, the mechanism of the disappearance of TJ proteins in response to PLA has been unclear. In this study, we inv...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-014-1324-4
更新日期:2014-09-01 00:00:00
abstract:PURPOSE:To evaluate the potential of several bis-ester prodrugs of the antiviral agent 9-(2-phosphonylmethoxyethyl)adenine (PMEA, adefovir) to enhance the oral absorption of PMEA. METHODS:Caco-2 monolayers were used to estimate intestinal transport and metabolism of the bis(pivaloyloxymethyl)-ester [bis(POM)-] and a s...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1011914618109
更新日期:1998-02-01 00:00:00
abstract::A series of carboxyfluorescein (CF)-containing multilamellar vesicle (MLV) dispersions was prepared and extruded through polycarbonate membranes ranging in size from 0.2 to 5 microns. Vesicle dispersions were nebulized for 80 min using a Collison nebulizer, and the release of CF was monitored during nebulization. Solu...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015896121377
更新日期:1991-02-01 00:00:00
abstract:PURPOSE:The possibility of direct delivery of steroids through the skin to the trachea and the effect of iontophoresis on delivery efficacy were evaluated after the application of an ionic steroidal prodrug, prednisolone sodium succinate (PS-Na), to the throat skin. METHODS:Fluorescein sodium salt (FL-Na) and PS-Na we...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-010-0337-x
更新日期:2011-04-01 00:00:00
abstract:PURPOSE:To prepare a thermoreversible gel system able to work as a medium for crystallization at around 20°C, allowing easy retrieval of crystals by simply decreasing the gel temperature. Lactose was selected has model substance for crystallization. METHODS:Water solutions with different% of poloxamer 407, α-Lactose m...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-011-0606-3
更新日期:2012-03-01 00:00:00
abstract:PURPOSE:The purpose of this study was to determine the potential effect of probenecid on the pharmacokinetics of zalcitabine in HIV-positive patients. METHODS:Twelve patients received single oral 1.5 mg doses of zalcitabine alone and during probenecid treatment (500 mg at 8 and 2 hours before and 4 hours after zalcita...
journal_title:Pharmaceutical research
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1023/a:1016009029536
更新日期:1996-03-01 00:00:00
abstract:PURPOSE:To demonstrate that polyanhydride copolymer chemistry affects the uptake and intracellular compartmentalization of nanospheres by THP-1 human monocytic cells. METHODS:Polyanhydride nanospheres were prepared by an anti-solvent nanoprecipitation technique. Morphology and particle diameter were confirmed via scan...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-008-9760-7
更新日期:2009-03-01 00:00:00
abstract::Enoximone and piroximone are cardiotonic agents for use in patients with congestive heart failure. Electroanalytical studies revealed that the dihydroimidazolone functionality was oxidizable and that this property can be analytically useful. The compounds undergo a two-electron, irreversible oxidation in neutral to ac...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015811830830
更新日期:1991-07-01 00:00:00
abstract:PURPOSE:The cause of antibody positive pure red cell aplasia associated with the subcutaneous administration of EPREX to patients with chronic kidney failure has been determined to be due to the leaching of weakly adjuvant compounds from the uncoated rubber stoppers that were formerly used in prefilled syringes. Other ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-005-5356-7
更新日期:2005-07-01 00:00:00
abstract::This review describes the design and current development of leukotriene biosynthesis inhibitors as potential antiinflammatory agents. Knowledge of the enzymatic mechanism of 5-lipoxygenase led to specific inhibitors of this enzyme which catalyzes a key step in the leukotriene pathway. Competitive inhibitors include ir...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/A:1016381215385
更新日期:1985-11-01 00:00:00
abstract:OBJECTIVE:The objective of this work was to determine plasma protein adsorption and macrophage phagocytosis of biodegradable polyanhydride, polylactic acid and polylactic-co-glycolic acid microspheres prepared by both spray-drying and solvent evaporation techniques. METHODS:Microspheres were characterized by scanning ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1011935222652
更新日期:1998-02-01 00:00:00
abstract:PURPOSE:To develop a semi-physiological-based model describing simultaneously the time course of immature and mature B-lymphocytes after topotecan (TPT) administration to tumor-bearing rats. METHODS:Twenty-four tumor-bearing BDIX male rats received a single 6 mg/kg intra-peritoneal dose of TPT or saline. Mature and im...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-009-0025-x
更新日期:2010-03-01 00:00:00
abstract:OBJECTIVES:We recently demonstrated that fibrin-based tissue engineered blood vessels (TEV) exhibited vascular reactivity, matrix remodeling and sufficient strength for implantation into the veins of an ovine animal model, where they remained patent for 15 weeks. Here we present an approach to improve the mechanical pr...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-007-9499-6
更新日期:2008-05-01 00:00:00
abstract:PURPOSE:This work describes the synthesis of block co-polymeric micelles, methoxy-poly(ethylene glycol)-poly(D,L-lactide) (mPEG-PLA) to encapsulate Curcumin (CUR), thereby improving the dispersibility and chemical stability of curcumin, prolonging its cellular uptake and enhancing its bioavailability. METHODS:CUR-mPEG...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-015-1830-z
更新日期:2016-04-01 00:00:00
abstract:PURPOSE:Evista (raloxifene HCl) is a nonsteroidal selective estrogen receptor modulator that displays estrogen agonist effects on bone and lipid metabolism but estrogen antagonist effects on the breast and endometrium. The potential for drug-drug interaction between raloxifene and warfarin was assessed in 15 healthy po...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1010904815275
更新日期:2001-07-01 00:00:00
abstract:PURPOSE:The aim of the study is to suppress the progress of estrogen-dependent breast cancer by inhibiting the membrane transporter, which mediates the internalization of estrone-3-sulfate as estrogen precursor in the cancer cells. METHODS:The uptake of estrone-3-sulfate by estrogen-dependent breast cancer MCF-7 cells...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-005-7096-0
更新日期:2005-10-01 00:00:00
abstract:PURPOSE:Since the adoption of highly active antiretroviral therapy, HIV disease progression has slowed across the world; however, patients are often required to take multiple medications daily of poorly bioavailable drugs via the oral route, leading to gastrointestinal irritation. Recently, long acting antiretroviral i...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-016-1936-y
更新日期:2016-08-01 00:00:00
abstract:PURPOSE:The purpose of this study was to develop a new computational fluid dynamics (CFD)-based model of the complex transport and droplet drying kinetics within a laboratory-scale spray dryer, and relate CFD-predicted drying parameters to powder aerosolization metrics from a reference dry powder inhaler (DPI). METHOD...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-020-02806-y
更新日期:2020-05-21 00:00:00
abstract:PURPOSE:To develop a non-viral gene delivery system in the form of an oil-in-water (o/w) lipid emulsion. METHOD:Cationic lipid emulsions were formulated with soybean oil, 1,2-dioleoyl-sn-glycero-3-trimethylammonium-propane (DOTAP) as a cationic emulsifier and other co-emulsifiers. The physical characteristics of the l...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1007553106681
更新日期:2000-03-01 00:00:00
abstract::To achieve time-controlled or site-specific drug delivery in the gastrointestinal tract, a sigmoidal release system (SRS) was developed, which achieved a prolonged lag time, followed by rapid release. The theophylline beads with a thick Eudragit RS film coating showed very low drug release in water, whereas the releas...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018910114436
更新日期:1994-01-01 00:00:00
abstract:PURPOSE:Many genetic disorders, including chondrodysplasias, and acquired disorders impair growth plate function, resulting in short and sometimes malformed bones. There are multiple endocrine and paracrine factors that promote chondrogenesis at the growth plate, which could potentially be used to treat these disorders...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-015-1636-z
更新日期:2015-07-01 00:00:00
abstract:PURPOSE:To investigate the effect of surface functionalization of mesoporous silica nanoparticles (MSN) on crystallization, loading, release and activity of mitoxantrone (MTX). METHODS:Thiol-, amine-, and mixed thiol/amine-functionalized MSN were synthesized and characterized by electron microscopy, thermogravimetry, ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-012-0766-9
更新日期:2012-09-01 00:00:00
abstract:PURPOSE:Bioavailability of orally administered drugs is much influenced by the behavior, performance and fate of the dosage form within the gastrointestinal (GI) tract. Therefore, MRI in vivo methods that allow for the simultaneous visualization of solid oral dosage forms and anatomical structures of the GI tract have ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1012161630481
更新日期:1997-08-01 00:00:00
abstract::We investigated the effects of increased concentrations of the solutes, salicylic acid, benzoic acid, and o-, m-, and p-methoxy benzoic acids, on the anisotropic properties of a liquid crystal solvent. The lamellar liquid crystal was composed of 37% polyoxyethylene (20) isohexadecyl ether in aqueous buffer of pH 1. Ph...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018920118631
更新日期:1993-05-01 00:00:00