Abstract：
:The synthesis, characterization, and therapeutic evaluation of a series of partially esterified derivatives of pentetic (diethylenetriaminepentaacetic) acid are reported. These compounds were prepared in an attempt to promote increased decorporation of insoluble colloidal forms of plutonium, which are removed by pentetic acid alone. The dimethyl, diethyl, dibutyl, dioctyl, monoethyl esters were synthesized by reaction of the appropriate alcohol with the dianhydride of pentetic acid. These esters were injected intravenously into mice as their calcium chelates in saline. None of the esters was effective in removing plutonium from the liver. All esters removed approximately 20% of the plutonium in the skeleton. However, when the esters were given together with pentetic acid, only the dioctyl ester showed enhanced removal of plutonium compared to pentetic acid alone. The small increase in effectiveness and the increased acute toxicity make these esters of limited practical interest in plutonium decorporation therapy.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Guilmette RA,Parks JE,Lindenbaum Adoi
10.1002/jps.2600680219subject
Has Abstractpub_date
1979-02-01 00:00:00pages
194-6issue
2eissn
0022-3549issn
1520-6017pii
S0022-3549(15)42468-2journal_volume
68pub_type
杂志文章abstract：:Solubilities in isoctane and water were determined for several C1-phenolic esters of prostaglandin F2 alpha and prostaglandin E2 and acetates having the same phenol moiety. Linear free energy relationships for solubility among the series were observed with slopes of approximately 1. These results suggest that the cont...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600690417
更新日期：1980-04-01 00:00:00
abstract：:A novel method is described for the preparation of sterile and pyrogen-free submicron liposomes of narrow size distribution. The method is based on the formation of a homogeneous dispersion of lipids in water-soluble carrier materials. To obtain the lipid-containing solid dispersion, liposome-forming lipids and water-...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.20055
更新日期：2004-06-01 00:00:00
abstract：:Complex dosing regimens simulated in the literature using a universal dosing regimen were calculated with a general dosing program developed using the program CONSAM. The program provides a rapid method of calculating nonuniform dosing regimens for up to n = 3 compartments for any linear model. Subject data can also b...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600800406
更新日期：1991-04-01 00:00:00
abstract：:Single-walled carbon nanotubes (SWCNTs) attract great interest in biomedical applications including drug and gene delivery. In this study, we developed a novel delivery system using SWCNTs associated with designed polycationic and amphiphilic peptides. Wrapping of SWCNTs with H-(-Lys-Trp-Lys-Gly-)7-OH [(KWKG)7] result...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2016.03.031
更新日期：2016-09-01 00:00:00
abstract：:The present study aims to evaluate the in vitro and in vivo performance of ordered mesoporous silica (OMS) as a carrier for the poorly water-soluble compound fenofibrate. Fenofibrate was loaded into OMS via incipient wetness impregnation to obtain a 29% drug load and formulated into capsules. Two capsule dosage forms ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2016.05.019
更新日期：2016-08-01 00:00:00
abstract：:This edition of the Journal of Pharmaceutical Sciences is dedicated to the wonderful career of Per Artursson from the Uppsala University. My Commentary focusses on Per's major contributions to the Caco-2 cell literature over the past 30 years. Two especially influential papers have been cited more than 1000 times out ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2020.08.016
更新日期：2021-01-01 00:00:00
abstract：:Accelerated stability studies (37 degrees, 47 degrees, and 57 degrees) were conducted on buffered aqueous solutions (pH 7.4, 8.4, and 9.4) of hydrocortisone in the presence of various molar ratios of D-fructose. First-order degradation was observed. Significant improvement in hydrocortisone stability was seen in those...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600720930
更新日期：1983-09-01 00:00:00
abstract：:Approximately 30% of active pharmaceutical ingredients (APIs) experience agglomeration, granulation, and breakage during agitated drying. Currently, there is no small-scale bench tool to help assess and observe granulation behavior of APIs in the laboratory and subsequently lead to the development of a robust drying m...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.23762
更新日期：2014-01-01 00:00:00
abstract：:Lysosomes are acidic intracellular organelles that can extensively sequester basic lipophilic drugs due to pH and membrane partitioning, and therefore may significantly influence subcellular drug concentrations. Current in vitro methods for lysosomal drug sequestration evaluation typically lack the ability to accurate...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2020.05.026
更新日期：2020-09-01 00:00:00
abstract：:Owing to proliferation of antibiotic-resistant bacteria, the use of antibiotics for livestock growth promotion is banned in many countries and alternatives to in-feed antibiotics are needed. Cinnamon essential oil exhibits strong in vitro antibacterial activity; however, direct addition of essential oils to animal fee...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2015.10.001
更新日期：2016-03-01 00:00:00
abstract：:An isothermal chromatographic (GC) method employing an SE-30 column and flame-ionization detection has been developed for the simultaneous assay of methyl, ethyl, propyl, and butyl 4-hydroxybenzoates and 4-hydroxybenzoic acid in liquid antacid formulations. The method, which uses a silica column chromatographic cleanu...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600730136
更新日期：1984-01-01 00:00:00
abstract：:Ketoconazole (KTZ) has 2 chiral centers with the therapeutically active form being a racemic mixture of 2 cis-enantiomers, namely, (2R,4S)-(+)-KTZ and (2S,4R)-(-)-KTZ. The aims of the present study were to examine the effects of (+)-KTZ, (-)-KTZ, and (±)-KTZ on aryl hydrocarbon receptor activation and subsequently CYP...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2015.12.009
更新日期：2016-03-01 00:00:00
abstract：:Surfactants stabilize proteins through two major mechanisms: (1) their preferential location at nearby interfaces, in this way precluding protein adsorption; and/or (2) their association with protein into "complexes" that prevent proteins from interacting with surfaces as well as each other. However, selection of surf...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.23908
更新日期：2014-05-01 00:00:00
abstract：:In 2005, the World Health Organization (WHO) proposed that provided an active pharmaceutical ingredient could meet certain criteria, bioequivalence could be evaluated with a set of laboratory tests, obviating the need for expensive and time-consuming pharmacokinetic studies in humans. The aim of this work was to deter...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.22349
更新日期：2011-03-01 00:00:00
abstract：:A series of mono-, di-, and trimethylated derivatives of 4-chloro- and 4-methoxybenzanilide was synthesized and evaluated for anticonvulsant activity. This series was prepared in the course of studies designed to examine the relationship between anticonvulsant effects and benzamide structure. The compounds were tested...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600790308
更新日期：1990-03-01 00:00:00
abstract：:The effects of chlorpromazine, prochlorperazine, and trifluoperazine on the pressor actions of serotonin, angiotensin, and bradykinin in the perfused vessels of full-term human placentas were investigated. A significant inhibition of the effect of serotonin was observed with trifluoperazine and chlorpromazine but not ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600651020
更新日期：1976-10-01 00:00:00
abstract：:The absorption of triazolam from pelleted drug-diet mixtures by mice under steady-state conditions was determined for doses up to 150 mg/kg/day by measuring alpha-hydroxytriazolam, the principal urinary metabolite of triazolam in the mouse, in urine samples collected over a 24-hour period. Following beta-glucuronide g...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600721020
更新日期：1983-10-01 00:00:00
abstract：:In an attempt to explain the triamterene stone diathesis, we studied the excretion and solubility of triamterene, 1, and its metabolite, the sulfate ester of the hydroxy derivative of triamterene, 3. The urinary excretion pattern and metabolism in stone formers was the same as in other chronic users of triamterene or ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600750205
更新日期：1986-02-01 00:00:00
abstract：:Microbicide intravaginal rings (IVRs) are a promising woman-controlled strategy for preventing sexual transmission of human immunodeficiency virus (HIV). An IVR was prepared and developed from polyether urethane (PU) elastomers for the sustained delivery of UC781, a highly potent nonnucleoside reverse transcriptase in...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.22781
更新日期：2012-02-01 00:00:00
abstract：:In this study, the effects of structurally related organic impurities on the molecular dynamics of amorphous sulfamethazine were evaluated using thermal analysis. Sulfanilamide (SNA), sulfamerazine (SMR), and sulfadimethoxine were used as virtual impurities of sulfamethazine. The amorphous state was prepared in situ i...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2016.12.008
更新日期：2017-04-01 00:00:00
abstract：:A high-performance liquid chromatographic method for the determination of (Z)- and (E)-doxepin hydrochloride isomers was developed. The analysis employs a column packed with spherical silica microparticles (5-6 mum), and a mobile phase of acetonitrile-chloroform-diethylamine (750:250:0.2) permits baseline resolution a...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600681133
更新日期：1979-11-01 00:00:00
abstract：:Baclofen, a widely used antispastic agent, has been found to exist in two crystalline forms, the anhydrate and monohydrate. The aim of this study was (1) to identify and characterize these two solid phases of baclofen, and (2) to examine the processing-induced phase transformations associated with wet granulation of b...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.20894
更新日期：2007-09-01 00:00:00
abstract：:Solubilization of nonpolar drugs constitutes one of the most important tasks in parenteral formulations design. This study investigates and assesses the solubility enhancement of Fluasterone by various techniques including cosolvency, micellization, and complexation. Of the solubilizing agents used, the modified beta-...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1021/js9901413
更新日期：1999-10-01 00:00:00
abstract：:In this study, the influence of the preparation technique (ball milling, spray drying, and film casting) of a supersaturated amorphous dispersion on the quality of solubility determinations of indomethacin in polyvinylpyrrolidone was investigated by means of statistical analysis. After annealing of the amorphous dispe...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.24207
更新日期：2015-01-01 00:00:00
abstract：:A reported fluorometric method to determine tetracycline in biological material was modified to determine low levels of the antibiotics when using only small amounts of starting material. The method is applicable to tissue distribution studies in small experimental animals and also can be used for serial determination...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600700218
更新日期：1981-02-01 00:00:00
abstract：:The P-glycoprotein (Pgp), a drug efflux pump, is expressed in intestinal epithelial cells, where it constitutes a barrier against xenobiotics. In inflammatory bowel disease, a dysregulation in the production of tumor necrosis factor (TNF)alpha and interferon (IFN)gamma, and an alteration of Pgp expression and activity...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.20072
更新日期：2004-06-01 00:00:00
abstract：:Various multiparticulate dissolution models that assume a log-normal particle-size distribution are fitted by nonlinear least-squares regression to data from the dissolution of micronized glyburide. Estimates of parameters describing the effective initial particle-size distribution are obtained, together with estimate...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600660603
更新日期：1977-06-01 00:00:00
abstract：:Brain cancers are among the most lethal tumors due to their rapid development and poor prognosis. Despite the existing potential of novel therapeutic strategies for the treatment of brain cancer, the major remaining challenge associated with clinical translation is the lack of effective and safe delivery strategies to...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章,评审
doi：10.1016/j.xphs.2017.08.009
更新日期：2017-12-01 00:00:00
abstract：:Topical lidocaine has been recently marketed as a new treatment for post-herpetic neuralgia. The aim of our study was to characterize the absorption profile of and systemic exposure to lidocaine from patch and gel formulations in normal volunteers, patients with post-herpetic neuralgia, and patients with acute herpes ...
journal_title：Journal of pharmaceutical sciences
pub_type： 临床试验,杂志文章
doi：10.1002/jps.10133
更新日期：2002-05-01 00:00:00
abstract：:The concentrations of antipyrine in plasma and saliva were equivalent in normal volunteers and in patients with acute viral hepatitis following oral doses of antipyrine. Estimates of clearance, volume of distribution, and half-life made from either plasma or saliva samples were not statistically different in these sub...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600660140
更新日期：1977-01-01 00:00:00
