Abstract:
:A sensitive activity assay for high volume evaluation of human renin inhibitory peptides (RIPs) in rat sera (range 2-80 ng/ml) was developed based on the low affinity of RIPs to rat renin and their high affinity to human renin. The utility of this activity assay was tested by measuring concentrations of a human RIP, U-71,038 (BOC-Pro-Phe-N-MeHis-Leu psi [CHOHCH2]Val-Ile-Amp), in rat sera, determined by the activity assay, by a sensitive radioimmunoassay (RIA), and by tracking tritiated drug. Rats were given radiolabeled drug as an intravenous bolus, and blood samples were collected at various times after dosing. The serum level of U-71,038 equivalents was determined by the three techniques. Whole blood was also counted for total radioactivity to evaluate the potential for U-71,038 incorporation into red blood cells. Results from the three serum assays indicate good agreement between the calculated U-71,038 equivalents for the 30 min and 1 hr collection times. The 2 and 4 hr collection times show excellent agreement for the activity assay and RIA; [3H]-U-71,038 determinations gave substantially higher values. Serum levels for U-71,038 determined 30 min after dosing averaged less than 300 ng equivalents/ml suggesting that less than 1% of the administered dose was in the systemic circulation at that time. Thus, U-71,038 was rapidly cleared. At the 4 hr collection time, the level of U-71,038 equivalents, as determined by activity assay and RIA, was ten times the in vitro IC50 for the renin inhibitory activity of U-71,038.(ABSTRACT TRUNCATED AT 250 WORDS)
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Ruwart MJ,Sharma SK,Harris DW,Lakings DB,Rush BD,Wilkinson KF,Cornette JC,Evans DB,Friis JM,Cook KJdoi
10.1023/a:1015883709275subject
Has Abstract,Author List Incompletepub_date
1990-04-01 00:00:00pages
407-10issue
4eissn
0724-8741issn
1573-904Xjournal_volume
7pub_type
杂志文章abstract:PURPOSE:Generation of valuable information about the biphasic geometrical configuration of porcine stratum corneum from Very Small Angle Neutron Scattering (VSANS) data and investigation of its effect on the corresponding effective diffusivity. METHODS:Spectra of porcine stratum corneum are mathematically transformed ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1026453628800
更新日期:2000-09-01 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::The glass transition temperature of an amorphous pharmaceutical solid is a critical physical property which can dramatically influence its chemical stability, physical stability, and viscoelastic properties. Water frequently acts as a potent plasticizer for such materials, and since many amorphous solids spontaneously...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018941810744
更新日期:1994-04-01 00:00:00
abstract::The effects of process and storage conditions of solid-state emulsions were studied. Oil-in-water emulsions may be prepared from solid state emulsions by adding an aqueous phase to the solid. Solid-state emulsions are prepared by processing an oil phase and an aqueous solution of matrix material via a solvent removal ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018983227234
更新日期:1993-07-01 00:00:00
abstract:PURPOSE:HSP90 (Heat shock protein 90kD) has been validated as a therapeutic target in Castrate Resistant Prostate Cancer. Unfortunately, HSP90 inhibitors suffer from dose-limiting toxicities that hinder their clinical applications. Previously developed polymeric delivery systems for HSP90 inhibitors had either low drug...
journal_title:Pharmaceutical research
pub_type: 杂志文章
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更新日期:2017-12-01 00:00:00
abstract:PURPOSE:To determine the extent of lateral spread and stratum corneum (SC) penetration of caffeine (CAF), hydrocortisone (HC) and ibuprofen (IBU) using a novel concentric tape stripping technique. METHOD:Ethanolic solutions of CAF, HC or IBU were applied to the forearm of 8 volunteers. At various time points, 10 succe...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-012-0731-7
更新日期:2012-08-01 00:00:00
abstract::An oral formulation of controlled-release isosorbide-5-nitrate pellets has been used to investigate the location of pellets in the gastrointestinal (GI) tract and, in parallel, to measure the drug absorption from these locations. Using the method of gamma scintigraphy the transit times and spreading of pellets in the ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016423404636
更新日期:1987-12-01 00:00:00
abstract:PURPOSE:The aim of this study was to examine if sparging with CO2(g) could be used to establish stable biorelevant bicarbonate buffers, in aqueous medium, for use in dissolution characterization of low-solubility ionizable drugs. METHODS:Preparation of the bicarbonate-containing dissolution medium was monitored by use...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1026147620304
更新日期:2003-10-01 00:00:00
abstract:PURPOSE:This study demonstrates the nasal administration (NA) of nanoemulsions complexed with the plasmid encoding for IDUA protein (pIDUA) as an attempt to reach the brain aiming at MPS I gene therapy. METHODS:Formulations composed of DOPE, DOTAP, MCT (NE), and DSPE-PEG (NE-PEG) were prepared by high-pressure homogen...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-018-2503-5
更新日期:2018-09-26 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-014-1489-x
更新日期:2015-02-01 00:00:00
abstract:PURPOSE:To study the miscibility of proteins and polymer excipients in frozen solutions and freeze-dried solids as protein formulation models. METHODS:Thermal profiles of frozen solutions and freeze-dried solids containing various proteins (lysozyme, ovalbumin, BSA), nonionic polymers (Ficoll, polyvinylpyrrolidone [PV...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1026412107574
更新日期:2000-10-01 00:00:00
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 plu...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/B:PHAM.0000019293.57927.7f
更新日期:2004-03-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-015-1693-3
更新日期:2015-10-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-018-2544-9
更新日期:2018-11-26 00:00:00
abstract:PURPOSE:We investigated optimum formulation characteristics in the nasal absorption of salmon calcitonin (sCT) by incorporation of acylcarnitines. METHODS:Nasal sCT formulations were administered to anesthetized rats. Plasma calcium level was measured and pharmacological bioavailability (P.bioav) was calculated. RESU...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016051600828
更新日期:1996-05-01 00:00:00
abstract::A new magnetic microsphere carrier has been formulated that may localize drugs by both biochemical and physical means. The microspheres, prepared from the polysaccharide chitosan, are designed to bind to anionic glycosaminoglycan receptors on the surface of capillary endothelial cells. The microspheres were formulated...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015978704810
更新日期:1988-05-01 00:00:00
abstract:PURPOSE:To assess the efficacy of the novel clinical formulation of fenretinide (LAU-7b) for the treatment of allergic asthma. To study the association between LAU-7b treatment in allergic asthma and the modulation of very long chain ceramides (VLCC). METHODS:We used two allergens (OVA and HDM) to induce asthma in mou...
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pub_type: 杂志文章
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更新日期:2020-01-08 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-010-0190-y
更新日期:2010-09-01 00:00:00
abstract::Effects of protease inhibitors and absorption enhancers on the absorption of salmon calcitonin (sCT) were evaluated after intratracheal coadministration to rats using the plasma Ca level as an index. Remarkable absorption enhancement could be attained with unsaturated fatty acids such as oleic acid and polyoxyethylene...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018926007902
更新日期:1994-09-01 00:00:00
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journal_title:Pharmaceutical research
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doi:10.1023/a:1015931431817
更新日期:1989-05-01 00:00:00
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更新日期:2012-10-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018930718979
更新日期:1994-01-01 00:00:00
abstract:PURPOSE:Comparison of the dissociation kinetics of rapid-acting insulins lispro, aspart, glulisine and human insulin under physiologically relevant conditions. METHODS:Dissociation kinetics after dilution were monitored directly in terms of the average molecular mass using combined static and dynamic light scattering....
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-017-2233-0
更新日期:2017-11-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-013-1188-z
更新日期:2014-03-01 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
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更新日期:2014-01-01 00:00:00
abstract:PURPOSE:The purpose of the present study is to explore whether a poly-L-arginine (poly-L-Arg)-induced increase in tight junctions (TJ) permeability of fluorescein isothiocyanate-labeled dextran (MW 4.4 kDa, FD-4) is associated with the Ca2+-dependent signaling and occurs following the phosphorylation/dephosphorylation ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/b:pham.0000003383.86238.d1
更新日期:2003-11-01 00:00:00
abstract:PURPOSE:To identify materials and processes which effect supersaturation of the GI milieu for low solubility drugs in order to increase oral bioavailability. METHODS:A variety of small and polymeric molecules were screened for their ability to inhibit drug precipitation in supersaturated solutions. The best polymeric ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-009-9852-z
更新日期:2009-06-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1023250900462
更新日期:2003-04-01 00:00:00
abstract::Intranasal route continues to be one of the main focuses of drug delivery research. Although it is generally perceived that the nasal route could avoid the first-pass metabolism in liver and gastrointestinal tract, the role of metabolic conversions in systemic and brain-targeted deliveries of the parent compounds and ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
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更新日期:2010-07-01 00:00:00
abstract::The bioavailability of a new sustained-release potassium chloride (KCl) tablet, designed for once-a-day dosing, was compared to a KCl elixir using urinary excretion data. The study utilized 25 male volunteers dosed in a crossover design in a dietary/activity-controlled environment. The regimens consisted of a total of...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016438413297
更新日期:1987-10-01 00:00:00