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 oleyl ether (absorption enhancers) and with chymostatin, bacitracin, potato carboxypeptidase inhibitor and phosphoramidon (protease inhibitors). sCT degrading enzymes had four times higher activity per total protein in membrane fraction of lung homogenates than the activity in cytosol fraction. These enzymes are thought to be serine proteases and metalloenzymes from the in vitro action profile of protease inhibitors. A good correlation between the in vitro activity of protease inhibitors and the in vivo enhancing effect on sCT activity suggested that membrane enzymes are responsible for the inactivation of sCT. Metabolic degradation and low permeability of sCT may be possible barriers to the absorption of sCT.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Kobayashi S,Kondo S,Juni Kdoi
10.1023/a:1018926007902subject
Has Abstractpub_date
1994-09-01 00:00:00pages
1239-43issue
9eissn
0724-8741issn
1573-904Xjournal_volume
11pub_type
杂志文章abstract:PURPOSE:To evaluate the effect of the size of low molecular weight hyaluronan (LMW-HA) oligomers on the targeting ability of the HA-containing copolymers to the CD44-overexpressing cells for delivering Paclitaxel (PTX) to ovarian cancer. METHODS:LMW-HA oligosaccharides of 4, 6, 8, 10, 12 and 14 sugar residues were att...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-012-0672-1
更新日期:2012-04-01 00:00:00
abstract:PURPOSE:Stable transformants expressing human multidrug resistance 1 (MDR1), monkey MDR1, canine MDR1, rat MDR1a, rat MDR1b, mouse mdr1a, and mouse mdr1b in LLC-PK1 were established to investigate species differences in P-glycoprotein (P-gp, ABCB1) mediated efflux activity. METHODS:The seven cDNAs of MDR1 from five an...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-006-0285-7
更新日期:2006-07-01 00:00:00
abstract::Turbidimetric or light scattering assays can be used to determine the extent of aggregation in protein formulations. Using low molecular weight urokinase (LMW-UK) as a model protein, the effect of polymeric additives on heat-induced aggregation was evaluated. Previous work has shown that under 60 degrees C heat treatm...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018935420680
更新日期:1994-07-01 00:00:00
abstract:PURPOSE:To gain information on the chemical stability pattern and the kinetics of the degradation of recombinant hirudin variant HV1 (rHir), a thrombin-specific inhibitor protein of 65 amino acids, in aqueous solution as a function of pH. METHODS:Stability of rHir was monitored at 50 degrees C in the framework of a cl...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1011918108849
更新日期:1998-09-01 00:00:00
abstract:PURPOSE:Low temperature sensitive liposome (LTSL) encapsulated docetaxel were combined with mild hyperthermia (40-42°C) to investigate in vivo biodistribution and efficacy against a castrate resistant prostate cancer. METHOD:Female athymic nude mice with human prostate PC-3 M-luciferase cells grown subcutaneously into...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-016-1971-8
更新日期:2016-10-01 00:00:00
abstract:PURPOSE:Several phenomena in tablets indicate that an inhomogeneous pore distribution is formed during the compaction process. Examples are lamination and the capping of corners. In order to gain an understanding of the relation between structure and compact properties, analyzing the structure in a location dependent m...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-005-5280-x
更新日期:2005-08-01 00:00:00
abstract:PURPOSE:In vitro and in vivo permeation studies were conducted to evaluate the characteristic of percutaneous administration of high hydrophilic drug L-carnitine (LC) by Functional MicroArray (FMA) painless intradermal delivery system. METHODS:In vitro study was designed to assess the effects of various skins, donor c...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-010-0109-7
更新日期:2011-01-01 00:00:00
abstract:PURPOSE:Study the radiolysis of solid-state metoclopramide hydrochloride at various absorbed doses. Elucidate the structure of the degradation products to gain information on the radiolysis mechanisms. METHODS:Solid-state metoclopramide samples were irradiated at several doses with gamma rays and high-energy electrons...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-006-0019-x
更新日期:2006-06-01 00:00:00
abstract:PURPOSE:The aim of this study was to identify new surfactants with low skin irritant properties for use in pharmaceutical and cosmetic formulations, employing cell culture as an alternative method to in vivo testing. In addition, we sought to establish whether potential cytotoxic properties were related to the size of ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/b:pham.0000041459.63362.6f
更新日期:2004-09-01 00:00:00
abstract::Gene delivery systems are designed to control the location of administered therapeutic genes within a patient's body. Successful in vivo gene transfer may require (i) the condensation of plasmid and its protection from nuclease degradation, (ii) cellular interaction and internalization of condensed plasmid, (iii) esca...
journal_title:Pharmaceutical research
pub_type: 杂志文章,评审
doi:10.1023/a:1012187414126
更新日期:1997-07-01 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:The organic cation transporters (OCTs) and multidrug and toxin extrusions (MATEs) together are regarded as an organic cation transport system critical to the disposition and response of many organic cationic drugs. Patient response to the analgesic morphine, a characterized substrate for human OCT1, is highly v...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-018-2526-y
更新日期:2018-10-25 00:00:00
abstract:PURPOSE:The aim of the present study was to design a new mucosal drug delivery system composed of liposomes dispersed within a bioadhesive hydrogel containing methyl-beta-cyclodextrin (Me(beta)CD) for controlled drug release. METHODS:A hydrophilic model molecule, inulin, was encapsulated within positively charged and ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-005-4591-2
更新日期:2005-06-01 00:00:00
abstract:PURPOSE:Covalent binding between N-acetyl-L-cysteine (NAC) and albumin was evaluated kinetically by conducting in vitro experiments. METHOD:After 14C-NAC was incubated with human or rat serum, the solution was analyzed by anion-exchange HPLC. The albumin-bound 14C-NAC was quantified by measuring the radioactivity in t...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1020749211745
更新日期:2002-11-01 00:00:00
abstract:PURPOSE:Penetration enhancers (PEs) enhancing efficacy depends on two processes: PEs release from patches and action on skin. Compared with their action on skin, PEs release process was poorly understood. Therefore, the purpose of this study was to make a mechanistic understanding of PEs release from acrylic pressure-s...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-020-02901-0
更新日期:2020-08-13 00:00:00
abstract:PURPOSE:In this study, a new modified nanoprecipitation approach that more efficient and simpler than conventional approach was developed to synthesize D-alpha-Tocopheryl polyethylene glycol 1000 succinate stabilized liposome-PLGA hybrid nanoparticle, loaded with simvastatin (ST-TLPN). METHODS:The optimum formulation ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-018-2485-3
更新日期:2018-08-30 00:00:00
abstract:PURPOSE:Orthorhombic crystals of paracetamol exhibit good technological properties during compression. The purpose of this study was to investigate the compression behavior of this substance and to compare it to that of monoclinic paracetamol. From the crystal structure, it could be hypothesized that sliding planes are...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1011954800246
更新日期:1998-07-01 00:00:00
abstract:PURPOSE:Generalizations based upon behavior of small molecules have established that a crystalline solid is generally much more stable toward chemical degradation than is the amorphous solid. This study examines the validity of this generalization for proteins using biosynthetic human insulin as the model protein. MET...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1012164520429
更新日期:1997-10-01 00:00:00
abstract:PURPOSE:This study was aimed to investigate the effects of a phenolic antioxidant, butylated hydroxyanisole (BHA) and its metabolite, tert-butylhydroquinone (tBHQ) on the induction of HO-1, NQO1 and Nrf2 proteins and their regulatory mechanisms in primary-cultured hepatocytes. METHODS:After exposure of BHA and tBHQ to...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-006-9094-2
更新日期:2006-11-01 00:00:00
abstract:PURPOSE:Topoisomerase II (Topo II) preferentially cuts DNA at alternating purine-pyrimidine repeats. Different Topo II poisons may affect Topo II to produce distinct drug-specific DNA cleavage patterns. GL331 is a new podophyllotoxin derivative exhibiting potent Topo II-poisoning activity. Therefore, the sequence selec...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1011048831698
更新日期:2001-06-01 00:00:00
abstract::Human serum albumin (HSA) was encapsulated in a 50:50 copolymer of DL-lactide/glycolide in the form of microspheres. These microspheres were used as a model formulation to study the feasibility of controlling the release of large proteins over a 20- to 30-day period. We show that HSA can be successfully incorporated i...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015948829632
更新日期:1990-11-01 00:00:00
abstract::An empirical mass-transfer model for enteric-coating dissolution that uses in vivo dissolution data to characterize the pH-dependent solubility properties of the polymer film and a mass-transfer coefficient determined from in vivo dissolution or disintegration studies is developed. Once the in vivo mass-transfer coeff...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018986827350
更新日期:1993-02-01 00:00:00
abstract::A new high-performance liquid chromatographic (HPLC) assay suitable for pharmacokinetic studies of enantiomers of fenoprofen (FEN) was developed. Following the addition of internal standard (IS; racemic ketoprofen), the plasma or urine constituents are extracted into a mixture of isooctane:isopropanol (95:5), back ext...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015867513045
更新日期:1988-01-01 00:00:00
abstract:PURPOSE:Typical methods to study pMDI sprays employ particle sizing or visible light diagnostics, which suffer in regions of high spray density. X-ray techniques can be applied to pharmaceutical sprays to obtain information unattainable by conventional particle sizing and light-based techniques. METHODS:We present a t...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-016-1869-5
更新日期:2016-05-01 00:00:00
abstract:PURPOSE:The prognosis for glioma patients is poor, and development of new treatments is critical. Previously, we engineered polymer-based vaccines that control GM-CSF, CpG-oligonucleotide, and tumor-lysate presentation to regulate immune cell trafficking and activation, which promoted potent immune responses against pe...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-010-0361-x
更新日期:2011-05-01 00:00:00
abstract:PURPOSE:To elucidate the catalytic mechanism of the esterase-like activity of serum albumin (SA), the reactivity of SA from six species was investigated using p-nitrophenyl esters as model substrates. METHODS:The effect of pH and the energetic and thermodynamic profiles of SA were determined for all species for p-nitr...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/b:pham.0000016241.84630.06
更新日期:2004-02-01 00:00:00
abstract:PURPOSE:To investigate the properties of phenylboronic acid-functional poly(amido amine) polymers (BA-PAA) in forming multilayered thin films with poly(vinyl alcohol) (PVA) and chondroitin sulfate (ChS), and to evaluate their compatibility with COS-7 cells. METHODS:Copolymers of phenylboronic acid-functional poly(amid...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-015-1688-0
更新日期:2015-09-01 00:00:00
abstract:PURPOSE:To quantitatively compare in vitro dissolution data in biorelevant and compendial media, to investigate whether in vitro differences are reflected in the simulated plasma profile and to specify under which circumstances prediction of the plasma profile of orally administered lipophilic drugs can be achieved. M...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1011071401306
更新日期:2001-03-01 00:00:00
abstract::Magnetic nanoparticles are useful as contrast agents for magnetic resonance imaging (MRI). Paramagnetic contrast agents have been used for a long time, but more recently superparamagnetic iron oxide nanoparticles (SPIOs) have been discovered to influence MRI contrast as well. In contrast to paramagnetic contrast agent...
journal_title:Pharmaceutical research
pub_type: 杂志文章,评审
doi:10.1007/s11095-012-0711-y
更新日期:2012-05-01 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