Abstract：
:The possibility tht metronidazole exerts several of its biological actions via interaction with important metal ions was investigated. NMR spectroscopy and polarography (ac) were used to test for any interaction, to locate the probable sites for complexation, and to determine the molecular stoichiometry of any complexes formed. Of the series of divalent metal ions tests, only cupric ion showed detectable interaction with metronidazole. The predominant site of interaction of cupric ion was the unsubstituted nitrogen atom (N-3) on the metronidazole molecule. The stoichiometry of the complex was (Cu-(metronidazole)4)+2. A likely structure for the complex is presented.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Chien YW,Lambert HJ,Sanvordeker DRdoi
10.1002/jps.2600640613subject
Has Abstractpub_date
1975-06-01 00:00:00pages
957-60issue
6eissn
0022-3549issn
1520-6017pii
S0022-3549(15)40267-9journal_volume
64pub_type
杂志文章abstract：:Successful development of stable solid protein formulations usually requires the addition of one or several excipients to achieve optimal stability. In these products, there is a potential risk of an inhomogeneous distribution of the various ingredients, specifically the ratio of protein and stabilizer may vary. Such ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章,评审
doi：10.1016/j.xphs.2019.10.010
更新日期：2020-01-01 00:00:00
abstract：:Nasal administration as a means of delivering therapeutic agents preferentially to the brain has gained significant recent interest. While some substrates appear to be delivered directly to the brain via this route, the mechanisms governing overall brain uptake and exposure remain unclear. Some substrates utilize the ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章,评审
doi：10.1002/jps.20318
更新日期：2005-06-01 00:00:00
abstract：:Mathematical relationships describing the delivery of drug to a target organ after intra-arterial, intravenous, and oral administration are presented. This discussion clearly demonstrates that administration into a blood vessel leading to the target organ often is superior to intravenous administration. However, this ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600701214
更新日期：1981-12-01 00:00:00
abstract：:Clinical lots of recombinant human platelet-activating factor acetylhydrolase (rhPAF-AH) were prepared in a lyophilized formulation. After reconstitution with sterile water for injection to form an aqueous solution (10 mM sodium citrate, 7.5 w/v% sucrose, and 0.1 w/v% Pluronic-F68, pH 6.5), a few visible, slowly growi...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.20237
更新日期：2005-02-01 00:00:00
abstract：:Although insulin receptor is expressed at the human blood-brain barrier (BBB), the physiological and pathologic roles of insulin signaling in biologic responses at the BBB remain unclear. Here, we investigate insulin signaling at the human BBB using human cerebral microvascular endothelial cell line (hCMEC/D3) as a we...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2017.04.036
更新日期：2017-09-01 00:00:00
abstract：:A multidisciplinary team approach to identify pharmaceutical impurities is presented in this article. It includes a representative example of the methodology. The first step is to analyze the sample by LC-MS. If the structure of the unknown impurity cannot be conclusively determined by LC-MS, LC-NMR is employed. If th...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.20120
更新日期：2004-09-01 00:00:00
abstract：:Microparticles are of considerable interest for drug delivery, vaccination and diagnostic imaging. In order to obtain microparticles with long circulation times, or to provide the prerequisite for tissue specific targeting through decoration with suitable ligands, their surfaces need to be modified such that they beco...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章,评审
doi：10.1002/jps.21350
更新日期：2008-11-01 00:00:00
abstract：:The solubility of ergotamine tartrate in aqueous solutions of tartaric acid, citric acid, hydrochloric acid, and caffeine and the dissolution rate of ergotamine tartrate in aqueous mixtures containing hydrochloric acid, caffeine, citric acid, or sodium acetate were studied. The Noyes-Whitney model of dissolution is us...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600690723
更新日期：1980-07-01 00:00:00
abstract：:SARS-CoV-2 utilizes the IMPα/β1 heterodimer to enter host cell nuclei after gaining cellular access through the ACE2 receptor. Ivermectin has shown antiviral activity by inhibiting the formation of the importin-α (IMPα) and IMPβ1 subunits as well as dissociating the IMPα/β1 heterodimer and has in vitro efficacy agains...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2020.08.024
更新日期：2020-12-01 00:00:00
abstract：:A consistent account of the assumptions of the well-stirred perfusion limited model leads to the equation for the organ tissue that does not coincide with that often presented in books and papers. The difference in pharmacokinetic profiles calculated by the valid and the commonly used equations could be quite signific...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.21798
更新日期：2010-01-01 00:00:00
abstract：:A set of seventeen nonsteroidal antiinflammatory drugs (NSAIDs), consisting of structurally unrelated carboxylic acids and piroxicam, was examined by high-performance liquid chromatography (HPLC) on an immobilized artificial membrane (IAM) column that is a solid-phase model of fluid membranes. The chromatographic capa...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1021/js960233h
更新日期：1997-02-01 00:00:00
abstract：:The purpose of this study was to examine the external predictability of an in vitro-in vivo correlation (IVIVC) for a metoprolol hydrophilic matrix extended-release formulation, with an acceptable internal predictability, in the presence of a range of formulation/manufacturing changes. In addition, this report evaluat...
journal_title：Journal of pharmaceutical sciences
pub_type： 临床试验,杂志文章,随机对照试验
doi：10.1002/1520-6017(200010)89:10<1354::aid-jps13>3.0
更新日期：2000-10-01 00:00:00
abstract：:A GLC method was developed for the determination of ethylene oxide and its two reaction products, ethylene chlorohydrin and ethylene glycol, in ophthalmic solutions at the levels recently proposed by the Food and Drug Administration. The method requires no extractions, sample preparations, or elaborate trapping and co...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600681223
更新日期：1979-12-01 00:00:00
abstract：:Antibody therapeutics with poor solubility in the subcutaneous matrix may carry unintended risks when administered to patients. The objective of this work was to estimate the risk of antibodies that precipitate in vitro at neutral pH by determining the impact of poor solubility on distribution of the drug from the inj...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2019.01.015
更新日期：2019-06-01 00:00:00
abstract：:Optical coherence tomography (OCT) is a recently developed optical technique that produces depth profiles of three-dimensional objects. It is a nondestructive interferometric method responding to refractive index variation in the sample under study and can reach a penetration depth of a few millimetres. OCT employs ne...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.21844
更新日期：2010-01-01 00:00:00
abstract：:Pharmacokinetic profiles of pentylenetetrazol in the dog were studied following rapid intravenous and oral administrations of a convulsant dose (15-20 mg/kg). Plasma level-time curves after a rapid intravenous injection showed biexponential decline, indicating that the disposition of this drug in the dog follows a two...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600650720
更新日期：1976-07-01 00:00:00
abstract：:Dolasetron mesilate (Anzemet) ((2 alpha, 6 alpha, 8 alpha, 9a beta)-octahydro-3-oxo-2,6-methano-2H-quinolizin-8-yl-1 H-indole-3-carboxylate monomethane-sulfonate) is a 5-HT3 receptor antagonist, which is in development for the treatment of chemotherapy-induced emesis. The ketone moiety of dolasetron is rapidly reduced...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1021/js960041m
更新日期：1996-07-01 00:00:00
abstract：:Metronidazole and four derivatives were studied in vitro to investigate the differences in the extent of their binding to plasma proteins. Modification at the terminal portion of the alkyl side chain resulted in wide differences in the extent of binding. Molecular orbital calculations were performed by the CNDO and MI...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600641111
更新日期：1975-11-01 00:00:00
abstract：:Increasing costs of research and development in the pharmaceutical industry has necessitated a growing interest in the early prediction of human pharmacokinetics of drug candidates. Of growing interest is the need to understand oral absorption, the most common route of small molecule drug administration. The fraction ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2018.03.015
更新日期：2018-07-01 00:00:00
abstract：:The stereochemistries of geometric isomers of 4-(2-bromo-1,2-diphenylvinyl)phenol, 4-(2-bromo-1,2-diphenylvinyl)anisole, and 2-[p-(2-bromo-1,2-diphenylvinyl)phenoxy]triethylamine were determined by conversion of the phenolic analog to the ethers and subsequent comparison of physical properties with those of 2-[p-(2-ch...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600651036
更新日期：1976-10-01 00:00:00
abstract：:Mycophenolate mofetil (MPM), a new immunosuppressant, is the morpholinoethyl ester of mycophenolic acid (MPA). The distribution in blood and pharmacokinetics of MPA after administration of MPM were examined. The plasma to erythrocyte concentration ratio was low (0.10-0.15). MPA existed in rat plasma as the highly boun...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1021/js9502480
更新日期：1996-03-01 00:00:00
abstract：:Vitamin E tocopherol polyethylene glycol succinate (TPGS) is a non-ionic surface active agent, known to enhance the bioavailability of lipophilic compounds via wettability, solubility, and in some cases permeability enhancement. MK-0536 is an anti-retroviral drug with poor wettability and solubility and a high dose. B...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.24585
更新日期：2015-11-01 00:00:00
abstract：:The structural integrity and conformational stability of various IgG1-Fc proteins produced from the yeast Pichia pastoris with different glycosylation site occupancy (di-, mono-, and nonglycosylated) were determined. In addition, the physical stability profiles of three different forms of nonglycosylated Fc molecules ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.23975
更新日期：2014-06-01 00:00:00
abstract：:A fully automated system for dissolution rate analysis of potassium in slow release tablets is described. Aliquots are removed after 1, 2, and 4 hr from six samples, and potassium is analyzed in a flame photometer at 768 nm. A complete study of six samples takes 5.5 hr. The system may be run overnight. During the time...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600650308
更新日期：1976-03-01 00:00:00
abstract：:The crystal structure of the common therapeutic agent, the pentahydrated sodium salt of L-thyroxine hormone (3-[4-(4-hydroxy-3,5-diiodophenoxy)-3,5-diiodophenyl]-L-alanine), has been determined and discussed in relation to the drug's stability. The stoichiometry and absolute configuration (-)-C(8)S-[C15H10I4NO4]-.Na+....
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.20155
更新日期：2004-12-01 00:00:00
abstract：:In an attempt to explain the mechanism of protein stabilization conferred by detergents, we investigated the effect of Tween 80 on aggregation of bovine serum albumin (BSA) using circular dichroism (CD) and native gel electrophoresis. CD thermal scans showed that BSA denatures at about 54 degrees C in 20 mM Tris, pH 7...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/(SICI)1520-6017(200005)89:5<646::AID-JPS10
更新日期：2000-05-01 00:00:00
abstract：:The storage of drug substance at subzero temperatures mitigates potential risks associated with liquid storage, such as degradation and shipping stress, making it the best solution for long-term storage. However, slower (generally uncontrolled) rates of freezing and thawing of drug substance in conventional large stor...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2017.03.019
更新日期：2017-08-01 00:00:00
abstract：:The problem of optimizing ocular bioavailability of topically applied ophthalmic drugs is discussed. A formula for drug concentration in the tear film is derived using well-known pharmacokinetic relationships and a first-order drug decay model for the tear film. The time integral of the tear film concentration is then...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600800113
更新日期：1991-01-01 00:00:00
abstract：:Currently, the EMEA, FDA, and WHO as regulatory authorities accept rapidly dissolving (>85% dissolved in 30 min) biopharmaceutics classification system (BCS) I drug products for biowaiver candidates. In the draft EMEA guideline the requirement has been set tighter, that is, the drug product should be very rapidly diss...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.21879
更新日期：2010-02-01 00:00:00
abstract：:New dihydropyridine in equilibrium pyridinium salt-type redox carrier systems were developed in which the drug is linked via the ring nitrogen atom of nicotinamide. The rate of oxidation of the dihydropyridine forms, and thus the overall and brain-specific distribution of the corresponding 3-carbamoyl-1-carbamoylalkyl...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600740304
更新日期：1985-03-01 00:00:00
