Abstract：
:The transepithelial transport of arginine vasopressin (AVP) across cultured rat alveolar epithelial cell monolayers was studied. At 0.1 nM donor [125I]AVP, the radiolabel flux measured in the apical-to-basolateral (AB) direction was about 10 times greater than that in the reverse (BA) direction. HPLC analyses of the basolateral receiver fluid collected at the end of these flux measurements showed that about 97% of the total [125I]label represented subspecies of AVP, whereas the apical receiver fluid contained largely intact AVP (approximately 85% of total [125I]label). Both donor fluids contained virtually no degradation products of AVP (> 99%). In the presence of an excess 0.1 mM unlabeled AVP in the apical donor fluid, the Papp for radiolabeled AVP in the AB direction was decreased by approximately 68%, while the fraction of intact AVP in the basolateral receiver fluid was increased six-fold as compared to that observed at 0.1 nM [125I]AVP alone. Under this condition, the flux of intact AVP was approximately the same in both directions. When the concentration of apical camostat mesylate, an aminopeptidase inhibitor, was varied from 0 to 2 mM, the radiolabeled flux in the AB direction (with 0.1 nM [125I]AVP in the donor fluid) was significantly decreased in a dose-dependent manner, yielding commensurably elevated concentrations of intact AVP in the basolateral receiver fluid. In contrast, leupeptin (0.5 mM), a serine protease inhibitor, was without effect. These data, taken together, suggest that apically-presented AVP undergoes proteolysis (most likely by peptidases localized at apical cell membranes of alveolar epithelium.(ABSTRACT TRUNCATED AT 250 WORDS)
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Yamahara H,Morimoto K,Lee VH,Kim KJdoi
10.1023/a:1018918022865subject
Has Abstractpub_date
1994-11-01 00:00:00pages
1617-22issue
11eissn
0724-8741issn
1573-904Xjournal_volume
11pub_type
杂志文章abstract：:The transport of thyrotropin releasing hormone (TRH) in rabbit buccal mucosa in vitro has been investigated with respect to (a) rate and type of metabolism of TRH on mucosal and serosal sides of buccal mucosa, (b) mechanism of TRH transport including charge effect on its permeability, and (c) pathway and rate-limiting...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015883217858
更新日期：1992-09-01 00:00:00
abstract：PURPOSE:Lapatinib, a small molecule EGFR/HER2 inhibitor, partially inhibits the outgrowth of HER2+ brain metastases in preclinical models and in a subset of CNS lesions in clinical trials of HER2+ breast cancer. We investigated the ability of lapatinib to reach therapeutic concentrations in the CNS following (14)C-lapa...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-011-0601-8
更新日期：2012-03-01 00:00:00
abstract：:Cyclosporine (CsA) is commercially available for oral administration as a solution in olive oil with alcohol and an emulsifier. To improve its variable absorption and low patient acceptability, several oral formulations were prepared and tested in vitro and in vivo in dogs. A tablet formulation prepared by direct comp...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015815614959
更新日期：1991-04-01 00:00:00
abstract：PURPOSE:This study aims to conduct an impact investigation in the hydrophobic-hydrophilic balance as an important factor for dissolution improvement of a hydrophilic carrier-based solid dispersion system. METHODS:Polymeric carriers with different hydrophobic to hydrophilic ratios were used to prepare several electrosp...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-019-2734-0
更新日期：2020-01-07 00:00:00
abstract：PURPOSE:To assess the blood-brain barrier (BBB) permeability of 12 clinically-used drugs in mdr1a(+/+) and mdr1a(-/-) mice, and investigate the influence of lipophilicity, nonspecific brain tissue binding, and P-gp-mediated efflux on the rate of brain uptake. METHODS:The BBB partition coefficient (PS) was determined u...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-009-9876-4
更新日期：2009-07-01 00:00:00
abstract：PURPOSE:1. The assessment of the role of hair follicles and sweat glands in skin resistance and percutaneous iontophoretic flux of 9-desglycinamide, 8-arginine vasopressin (DGAVP) by comparing two skin species: human stratum corneum which contained hair follicles, sweat and sebaceous glands, and shed snake skin which l...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016243706415
更新日期：1995-10-01 00:00:00
abstract：PURPOSE:To dynamically analyze the processes of oral absorption and hepatobiliary distribution of telmisartan using positron emission tomography (PET). METHODS:(11)C-labeled telmisartan ([(11)C]TEL) was orally administered to rats with or without non-radiolabeled telmisartan (0.5, and 10 mg/kg). PET scanning of abdomi...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-012-0768-7
更新日期：2012-09-01 00:00:00
abstract：:The new generation of nanotechnology-based drug formulations is challenging the accepted ways of cancer treatment. Multi-functional nanomaterial constructs have the capability to be delivered directly to the tumor site and eradicate cancer cells selectively, while sparing healthy cells. Tailoring of the nano-construct...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-010-0214-7
更新日期：2011-02-01 00:00:00
abstract：PURPOSE:Present study assessed the influence of gallate esterification on the anti-cancer activity of procyanidin B2 (B2) in androgen-dependent human prostate carcinoma LNCaP cells employing B2-3,3'-di-O-gallate (B2-G(2)), two mono-gallate esters B2-3-O-gallate (B2-3G) and B2-3'-O-gallate (B2-3'G) and the parent compou...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-009-0037-6
更新日期：2010-04-01 00:00:00
abstract：PURPOSE:To develop a statistical model for predicting effect of food on the extent of absorption (area under the curve of time-plasma concentration profile, AUC) of drugs based on physicochemical properties. MATERIALS AND METHODS:Logistic regression was applied to establish the relationship between the effect of food ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-007-9236-1
更新日期：2007-06-01 00:00:00
abstract：PURPOSE:Non-small cell lung cancer is the leading cause of cancer related deaths globally. Considering the side effects and diminishing chemosensitivity to chemotherapy, novel treatment approaches are sought. Hence, we aim to develop a liposomal co-delivery system of pDNA expressing shRNA against PFKFB3 (pshPFKFB3) and...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-017-2244-x
更新日期：2017-11-01 00:00:00
abstract：PURPOSE:SN-38, a potent chemotherapeutic drug, has not been used clinically because of its severe side effects and poor solubility. In this work, we aimed to evaluate the effect of dose and multiple injections of SN-38-loaded polymeric depots on antitumor efficacy and toxicity in vivo. METHODS:Preparation and characte...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-016-2011-4
更新日期：2016-12-01 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：:A new method of analysis for the antihypertensive drug, hydralazine, is introduced. The assay involves the addition of p-nitrobenzaldehyde to blood samples containing hydralazine, to form a stable Schiff's base, hydralazine p-nitrobenzaldehyde hydrazone. The derivative is extracted from the blood into hexane and the s...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015915812987
更新日期：1988-06-01 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：: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:Microphysiological systems (MPS), also known as "organs-on-chips" or "tissue chips," leverage recent advances in cell biology, tissue engineering, and microfabrication to create in vitro models of human organs and tissues. These systems offer promising solutions for modeling human physiology and disease in vitr...
journal_title：Pharmaceutical research
pub_type： 杂志文章,评审
doi：10.1007/s11095-019-2742-0
更新日期：2019-12-17 00:00:00
abstract：PURPOSE:The gadopentetic acid (Gd-DTPA)-loaded chitosan nanoparticles (Gd-nanoCPs) were prepared for gadolinium neutron-capture therapy (Gd-NCT) and characterized and evaluated as a device for intratumoral (i.t.) injection. METHODS:Gd-nanoCPs were prepared by a novel emulsion-droplet coalescence technique. The effects...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018995124527
更新日期：1999-12-01 00:00:00
abstract：:Molecular dynamics simulations and the generation of ad hoc chemical libraries are playing an increasingly important and recognized role in structure-based virtual screening. These approaches are important for treating target flexibility and improving the drug discovery pipeline. In this article I will comment on thes...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-013-1012-9
更新日期：2013-05-01 00:00:00
abstract：:Penetration of various compounds through shed snake skin was measured in vitro to examine the effect of lipophilicity and molecular size of a compound on permeability through this model membrane. The permeabilities were found to be controlled by the lipophilicity and the molecular size of the permeant. The smaller and...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015902308676
更新日期：1990-12-01 00:00:00
abstract：PURPOSE:Drug particle physical properties are critical for the efficiency of a drug delivered to the lung. The purpose of this study was to produce ultrafine sumatriptan succinate particles for inhalation. METHODS:Sumatriptan succinate particles were produced via reactive precipitation without any surfactants. Several...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-008-9586-3
更新日期：2008-09-01 00:00:00
abstract：:The Office of Generic Drugs has ensured the high quality of generic products based upon two requirements: pharmaceutical equivalence and bioequivalence to the reference listed drug (RLD). This paradigm has been used with success toward ensuring quality generic drug products that provide the same therapeutic benefit as...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-011-0397-6
更新日期：2011-07-01 00:00:00
abstract：:Four lipophilic, low molecular weight drugs solubilized in phosphatidylcholine-bile salt mixed micelles were injected s.c. into the hind legs of sheep and their cumulative recoveries in lymph draining from the site of application were determined. Surprisingly, the cumulative recoveries (percentage of dose) varied betw...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015807913934
更新日期：1991-10-01 00:00:00
abstract：PURPOSE:To develop an isolated perfused rat liver (IPRL) model with low baseline levels of tumor necrosis factor (TNF)-alpha in the outlet perfusate to study the effects of immunostimulants and immunosuppressants on the release of TNF-alpha from this organ. METHODS:Isolated rat livers were perfused with a buffer conta...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1013603331899
更新日期：2002-01-01 00:00:00
abstract：PURPOSE:We reported that suramin produced chemosensitization at nontoxic doses. This benefit was lost at the approximately 10-fold higher, maximally tolerated doses (MTD). The aim of the current study was to identify in patients the chemosensitizing suramin dose that delivers 10-50 microM plasma concentrations over 48 ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-006-0165-1
更新日期：2006-06-01 00:00:00
abstract：:Determination of methadone (MET) in biological fluids can serve to adjust dosages in patients suffering from cancer pain or participating in methadone maintenance programs. We developed a gas chromatographic assay using nitrogen-phosphorus detection. The method involves a single-step extraction from alkalized plasma, ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018904825958
更新日期：1993-03-01 00:00:00
abstract：:A colorless, parallelepiped crystal of methyl (2R,3S)-N-benzoyl-3-phenylisoserinate belonging to the space group P2(1) with a = 5.414(4), b = 7.813(1), c = 17.802(7) A, beta = 90.87(4) degrees, Z = 2, V = 752.9 A3, Dcalc = 1.32 g cm-3, and mu calc = 1.02 cm-1 was selected and the structure solved using direct methods....
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015863814901
更新日期：1991-07-01 00:00:00
abstract：PURPOSE:The lack of water-solubility hampers the use of many potent pharmaceuticals. Polymeric micelles are self-assembled nanocarriers with versatile properties that can be engineered to solubilize, target, and release hydrophobic drugs in a controlled-release fashion. Unfortunately, their large-scale use is limited b...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/b:pham.0000029284.40637.69
更新日期：2004-06-01 00:00:00
abstract：PURPOSE:The objective of this study was to determine the pharmacokinetics and safety for NX1838 following injection into the vitreous humor of rhesus monkeys. METHODS:Plasma and vitreous humor pharmacokinetics were determined following a single bilateral 0.25, 0.50, 1.0, 1.5, or 2.0 mg/eye dose. In addition, the pharm...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1007657109012
更新日期：2000-12-01 00:00:00
abstract：PURPOSE:To test the hypothesis of surface displacement as the underlying mechanism for IgG stabilization by polysorbates and HPβCD against surface-induced aggregation. METHODS:Adsorption/desorption-kinetics of IgG-polysorbate 80/-HPβCD were monitored. Maximum bubble pressure method was used for processes within second...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-012-0854-x
更新日期：2013-01-01 00:00:00
