Abstract:
:The present review discusses drugs and counter ions suitable for ion pair transport (IPT). Ion pairing is shown to effectively increase the lipophilicity and transport rate of polar drugs across lipid membranes. The proposed mechanisms of IPT are discussed in detail. A marked change in drug properties upon ion pair formation is necessary to improve the bioavailability of hydrophilic ionizable drugs.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Neubert Rdoi
10.1023/a:1015963128124subject
Has Abstractpub_date
1989-09-01 00:00:00pages
743-7issue
9eissn
0724-8741issn
1573-904Xjournal_volume
6pub_type
杂志文章,评审abstract::To evaluate the effects of a neutron activation radiolabeling technique on an enteric-coated multiparticulate formulation of erythromycin, test quantities were produced under industrial pilot scale conditions. The pellets contained the stable isotope erbium oxide (Er-170), which was later converted by neutron activati...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015826229323
更新日期:1990-03-01 00:00:00
abstract:PURPOSE:The use of dendrimers for biomedical applications has emerged with promising results. 2G-NN16 is a carbosilane dendrimer with sixteen positive charges per molecule tested to be capable to bind and release antisense oligonucleotides (ODNs) and small interference RNA (siRNA) in vitro. In spite of low cytotoxicity...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-008-9776-z
更新日期:2009-03-01 00:00:00
abstract:PURPOSE:Grapefruit juice (GJ) is known to increase the oral bioavailability of many CYP3A-substrates by inhibiting intestinal phase-I metabolism. However, the magnitude of AUC increase is often insignificant and highly variable. Since we earlier suggested that CYP3A and P-glycoprotein (P-gp) form a concerted barrier to...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1011902625609
更新日期:1999-04-01 00:00:00
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
更新日期:2004-10-01 00:00:00
abstract:PURPOSE:The purpose of this study was to clarify the localization and function of the ATP-binding cassette transporter G2 (ABCG2; BCRP/MXR/ABCP) in retinal capillary endothelial cells, which form the inner blood-retinal barrier, as an efflux transport system. METHODS:The expression was determined by reverse transcript...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-006-0067-2
更新日期:2006-06-01 00:00:00
abstract:PURPOSE:This study addresses the effect of freezing and thawing on a therapeutic monoclonal antibody (mAb) solution and the corresponding buffer formulation. Particle formation, crystallization behaviour, morphology changes and cryo-concentration effects were studied after varying the freezing and thawing rates, buffer...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-018-2378-5
更新日期:2018-03-19 00:00:00
abstract::The influence of the jejunal bloodflow on the absorption of theophylline was investigated. The bloodflow through a segment under investigation was varied by changing the systemic blood pressure by means of a donor blood infusion into the jugular vein or by an infusion of isoprenaline or levarterenol into a femoral vei...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/A:1016374508542
更新日期:1984-01-01 00:00:00
abstract::Lecithin-stabilized triglyceride emulsions are subject to hydrolysis by pancreatic lipase. The time profiles of these reactions are characterized by a lag-phase and a zero-order phase. Lag phases are more pronounced with long-chain triglycerides. Ca2+ is effective in reducing the lag-phase and activating lipase. Kinet...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015956104500
更新日期:1989-06-01 00:00:00
abstract::A sensitive radioreceptor assay (RRA) to determine the serum concentrations of fentanyl, pentazocine and morphine was developed on the basis of the drug's competition with a labeled tracer ((3)H-naloxone) for the membrane bound opioid receptor in rat brain homogenates. The binding data were computer-fitted to a standa...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/A:1016369229440
更新日期:1984-09-01 00:00:00
abstract::Growing tumors develop additional new blood vessels to meet the demand for adequate nutrients and oxygen, a process called angiogenesis. Cancer is a highly complex disease promoted by excess angiogenesis; interfering with this process poses for an attractive approach for controlling tumor growth. This hypothesis led t...
journal_title:Pharmaceutical research
pub_type: 杂志文章,评审
doi:10.1007/s11095-008-9634-z
更新日期:2008-12-01 00:00:00
abstract::The use of microdialysis sampling to study the binding of drugs to plasma proteins was evaluated. Microdialysis sampling is accomplished by placing a short length of dialysis fiber in the sample and perfusing the fiber with a vehicle. Small molecules in the sample, such as drugs, diffuse into the fiber and are transpo...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015955503708
更新日期:1990-10-01 00:00:00
abstract:PURPOSE:Type I collagen accumulates during liver fibrosis primarily because α-complex protein-2 (αCP(2)), encoded by the poly(rC) binding protein 2 (PCBP2) gene, binds to the 3' end of the collagen mRNA and increases its half-life. This study aimed to reverse the pro-fibrogenic effect of alcohol on hepatic stellate cel...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-011-0475-9
更新日期:2011-12-01 00:00:00
abstract:PURPOSE:This study investigated the penetration of lidocaine around and through a sutured incision following the application of iontophoretic and passive patches in the CD Hairless rat. MATERIALS AND METHODS:Concentrations in localized areas (suture, dermis, subcutaneous, and vascular) were determined using microdialy...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-007-9490-2
更新日期:2008-08-01 00:00:00
abstract:PURPOSE:The purpose of this study was to evaluate the feasibility of delivering vapreotide, a somatostatin analogue, by transdermal iontophoresis. METHODS:In vitro experiments were conducted using dermatomed porcine ear skin and heat-separated epidermis. In addition to quantifying vapreotide transport into and across ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-005-5276-6
更新日期:2005-08-01 00:00:00
abstract:PURPOSE:The aim of this study is to investigate the effects of 50% ethyl acetate extracts of grapefruit juice (GFJ) and orange juice (OJ) on the transport activity of P-glycoprotein (P-gp) in the rat small intestine. METHODS:The efflux of P-gp substrates from rat everted sac in the absence or presence of verapamil, GF...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016100715125
更新日期:2002-06-01 00:00:00
abstract::Indomethacin microspheres based on a combination of ethylcellulose and polyethyleneglycol were prepared using the solvent evaporation process. Release profiles of ensemble and individual microspheres were measured. Both were found to follow first-order kinetics, in contrast to what was expected. This was attributed to...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015917023949
更新日期:1988-03-01 00:00:00
abstract::The mechanical properties of dry and wet polymeric films prepared from various aqueous polymeric dispersions were evaluated by a puncture test. They were studied with respect to type of polymer dispersion [cellulosic: Aquacoat and Surelease; acrylic: Eudragit NE, L, RS, and RL 30 D], plasticizer type (water-soluble or...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018942127524
更新日期:1994-06-01 00:00:00
abstract::Nanoparticles, including lipopolyamines leading to lipoplexes, liposomes, and polyplexes are targeted drug carrier systems in the current search for a successful delivery system for polynucleic acids. This review is focused on the impact of gene and siRNA delivery for studies of efficacy, pharmacodynamics, and pharmac...
journal_title:Pharmaceutical research
pub_type: 杂志文章,评审
doi:10.1007/s11095-008-9646-8
更新日期:2009-01-01 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:PURPOSE:Cynarin, a potential immunosuppressant that blocks the interaction between the CD28 of T-cell receptor and CD80 of antigen presenting cells, was found in Echinacea purpurea by a new pharmaceutical screening method: After Flowing Through Immobilized Receptor (AFTIR; Dong et al., J Med Chem, 49: 1845-1854, 2006)....
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-008-9754-5
更新日期:2009-02-01 00:00:00
abstract::Aucubin, a promising hepatoprotecting iridoid glucoside, was given intravenously (iv), orally (po), intraperitoneally (ip), and hepatoportally (pv) to rats. A linear pharmacokinetic behavior was obtained after iv administation of 400-400 mg/kg of aucubin. The half-life of aucubin in the postdistributive phase (t1/2, b...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015821527621
更新日期:1991-08-01 00:00:00
abstract:PURPOSE:This study seeks to develop fiber membranes for local sustained delivery of 25-hydroxyvitamin D3 to induce the expression and secretion of LL-37 at or near the surgical site, which provides a novel therapeutic approach to minimize the risk of infections. METHODS:25-hydroxyvitamin D3 loaded poly(L-lactide) (PLA...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-015-1667-5
更新日期:2015-09-01 00:00:00
abstract:PURPOSE:Doxorubicin was chemically conjugated to a terminal end group of poly(D,L-lactic-co-glycolic acid) [PLGA] and the doxorubicin-PLGA conjugate was formulated into nanoparticles to sustain the release of doxorubicin. METHODS:A hydroxyl terminal group of PLGA was activated by p-nitrophenyl chloroformate and reacte...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018908421434
更新日期:1999-07-01 00:00:00
abstract:PURPOSE:The intratumoral heterogeneity observed in breast cancer (BC), in particular with regard to cell surface receptor expression, can hinder the success of many targeted cancer therapies. The development of novel therapeutic agents that target more than one receptor can overcome this inherent property of tumors and...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-019-2684-6
更新日期:2020-01-21 00:00:00
abstract:PURPOSE:The study was performed for clarifying the mechanism of interaction between indoxyl sulfate (IS), a typical uremic toxin bound to site II, and site I-ligands when bound to human serum albumin (HSA). The effect of the N to B transition on the interactions was also examined. METHODS:Quantitative investigation of...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1011014629551
更新日期:2001-04-01 00:00:00
abstract:PURPOSE:One of the major hurdles facing nanomedicines is the antibody production against nanoparticles that subsequently results in their opsonization and clearance by macrophages. The objective of this research was to examine and identify the sequence of a low-immunogenic peptide based on recombinant elastin-like poly...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-015-1683-5
更新日期:2015-09-01 00:00:00
abstract:PURPOSE:We have evaluated a new process, involving solution-enhanced dispersion by supercritical fluids (SEDS), for the production of polymeric microparticles. METHODS:The biodegradable polymers, Poly (DL-lactide-co-glycolide): copolymer composition 50:50 (DL-PLG), Poly (L-lactide) (L-PLA), Poly (DL-lactide) (DL-PLA) ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018868423309
更新日期:1999-05-01 00:00:00
abstract::Sulfasalazine, 60 mg/kg, was administered orally to groups of rats (n = 4) along with 1, 5, or 10 mg/kg of riboflavin. Plasma and urine were assayed for 5-aminosalicylic acid, acetyl-5-aminosalicylic acid, sulfapyridine, and acetyl-sulfapyridine using an HPLC method. The mean percent of dose recovered as total metabol...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015938706685
更新日期:1989-12-01 00:00:00
abstract:PURPOSE:To monitor the biodistribution of IgG1 aggregates upon subcutaneous (SC) and intravenous (IV) administration in mice and measure their propensity to stimulate an early immune response. METHODS:A human mAb (IgG1) was fluorescently labeled, aggregated by agitation stress and injected in SKH1 mice through SC and ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-013-1154-9
更新日期:2014-01-01 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