Abstract：
:Anhydrotetracycline (AHTC), one of the major toxic decomposition products of the antibiotic tetracycline, contains several potential binding sites to metal ions. The acidity constants of the ligand were calculated in aqueous medium (I = 0.1 M) at 25 and 37 degrees C. We found pKa1 = 3.23 +/- 0.08, pKa2 = 5.94 +/- 0.09, and pKa3 = 8.48 +/- 0.02 at 25 degrees C and pKa1 = 3.12 +/- 0.09, pKa2 = 5.86 +/- 0.03, and pKa3 = 8.38 +/- 0.04 at 37 degrees C. The coordination of AHTC to Cu(II) and Ni(II) ions was studied in the solid state as well as in buffered aqueous solution at pH 10.0. At this pH, the formation of the two CuL2 and CuL species was indicated (log beta 1 = 8.41 +/- 0.04 and log beta 2 = 12.55 +/- 0.05), but only the formation of the NiL complex (log beta = 5.74 +/- 0.04) was identified. Spectroscopic data confirm the previous assignment of the C11 and C12 oxygens as the coordination sites, yielding six-membered ring chelates and excluding complexation through any of the potential binding positions on ring A.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
de Siqueira JM,Carvalho S,Paniago EB,Tosi L,Beraldo Hdoi
10.1002/jps.2600830306subject
Has Abstractpub_date
1994-03-01 00:00:00pages
291-5issue
3eissn
0022-3549issn
1520-6017pii
S0022-3549(15)49377-3journal_volume
83pub_type
杂志文章abstract：:Biopolymer-based hydrogels such as mucus and the basal lamina play a key role in biology, where they control the exchange of material between different compartments. They also pose a barrier that needs to be overcome for successful drug delivery. Characterizing the permeability properties of such hydrogels is mandator...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
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abstract：:The relationship between chemical structure and antifungal activity of quaternary imidazolium compounds is analyzed. The compounds are described by a set of condition attributes concerning structure and by a decision attribute concerning activity. The description builds up an information system. The smallest set of co...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
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更新日期：1995-02-01 00:00:00
abstract：:A physiological flow model was developed for the distribution of sulfathiazole residues in various tissues in swine. The approach was compartmental, in which the compartments and equilibrium constants had physiological meaning. Differential equations were developed, and appropriate parameter values and initial conditi...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600731107
更新日期：1984-11-01 00:00:00
abstract：:The aim of this study was to evaluate a strategy based on static and dynamic physiologically based pharmacokinetic (PBPK) modeling for the prediction of metabolite and parent drug area under the time-concentration curve ratio (AUCm/AUCp) and their PK profiles in humans using in vitro data when active transport process...
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更新日期：2017-09-01 00:00:00
abstract：:High-field (300 MHz) 1H NMR spectral analyses are reported for various sodium or calcium heparin products available on the Canadian market. Dermatan sulfate (chondroitin sulfate B) was detected as a contaminant in virtually all of these products. Its content varied among the suppliers from less than 1 to 15%, and also...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600780205
更新日期：1989-02-01 00:00:00
abstract：:The objective of this study was to determine the relative importance of metabolism by cytochrome P450 (CYP) enzymes versus efflux by P-glycoprotein (P-gp) in restricting the intestinal mucosal permeation of cyclic prodrugs (AOA-DADLE, CA-DADLE, OMCA-DADLE) of the opioid peptide DADLE (H-Tyr-D-Ala-Gly-Phe-D-Leu-OH). AO...
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journal_title：Journal of pharmaceutical sciences
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更新日期：2006-02-01 00:00:00
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abstract：:A highly sensitive assay for the measurement of all-trans-retinoic acid (tretinoin) and 13-cis-retinoic acid (isotretinoin) has been developed. Collected plasma samples were protein precipitated with 2-propanol followed by solid phase extraction. The retinoic acids were subsequently derivatized to their pentafluoroben...
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abstract：:A difference spectrophotometric analytical method was developed for the selective determination of p-hydroxybenzoic acid in the presence of its alkyl esters without prior separation. Based on the spectral shift to a shorter wavelength accompanyint carboxyl dissociation, the procedure measures as little as 2% of this a...
journal_title：Journal of pharmaceutical sciences
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更新日期：1978-06-01 00:00:00
abstract：:In this study, black phosphorus nanosheets (BPNSs) were incorporated into a hydrogel formed from dibenzaldehyde-functionalized polymer (DF-PEG) and polyaspartylhydrazide (PAHy) polymer to create an injectable and pH-sensitive DF-PEG-PAHy/BPNSs hydrogel, which can be used as a smart depot for synergistic chemo-photothe...
journal_title：Journal of pharmaceutical sciences
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pub_type： 杂志文章
doi：10.1002/jps.2600680143
更新日期：1979-01-01 00:00:00
abstract：:The purpose of the present study was to examine whether the intestinal absorption of low-permeability drugs could be improved by utilization of the intestinal influx transporter PEPT1. We investigated whether peptide derivatives of poorly absorbable nonamino acid-like drugs might be substrates of PEPT1, using rebamipi...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.21551
更新日期：2009-05-01 00:00:00
abstract：:The binding of Cu2+ and Ni2+ to bovine, dog, and human serum albumin has been studied by the 35Cl NMR probe technique. The number of primary copper sites were estimated to be 1.3 for human serum albumin, 3.1 for bovine serum albumin, and 6.6 for dog serum albumin. A similar number of primary nickel sites was determine...
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pub_type： 杂志文章
doi：10.1002/jps.2600740116
更新日期：1985-01-01 00:00:00
abstract：:N-Acetyl-DL-penicillamine (IIIb), a structural analog of N-acetyl-L-cysteine (IIIa), did not protect mice from lethal doses of acetaminophen (I), whereas IIIa offered protection. This lack of efficacy of IIIb probably is due to the decreased nucleophilicity of its sulfhydryl group compared to that of IIIa, the probabl...
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pub_type： 杂志文章
doi：10.1002/jps.2600690905
更新日期：1980-09-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600650115
更新日期：1976-01-01 00:00:00
abstract：:After intravenous administration of MK-826, a new carbapenem antibiotic, the compound exhibited nonlinear pharmacokinetics in rats and monkeys. In both species, time-averaged plasma clearance (based on total concentrations) increased about 5-fold over the 10- to 180-mg/kg dose range. MK-826 was extensively plasma prot...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1021/js980232k
更新日期：1999-02-01 00:00:00
abstract：:We have developed a hydrogel patch, which could promote antigen penetration through stratum corneum (SC), and have demonstrated its safety and efficacy in animals and humans. For the availability improvement of our system, it is important to develop a device, which enhances antigen penetration through SC more efficien...
journal_title：Journal of pharmaceutical sciences
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更新日期：2013-06-01 00:00:00
abstract：:99mTc-N-(3-bromo-2,4,6-trimethylacetanilide)iminodiacetat e (I) and 99mTc-N-pyridoxyl-5-methyl-tryptophan (II) have been described as having optimal properties as hepatobiliary radiopharmaceuticals. This study compared specificity for hepatobiliary excretion, blood disappearance, rates of biliary appearance, and pharm...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600731259
更新日期：1984-12-01 00:00:00
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doi：10.1002/jps.2600820619
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pub_type： 杂志文章
doi：10.1002/jps.22144
更新日期：2010-10-01 00:00:00
abstract：:This work compares the conformational stability, backbone flexibility, and aggregation propensity of monomer and dimer fractions of an IgG1 monoclonal antibody (mAb) generated on UVA light exposure for up to 72 h collected by preparative size-exclusion chromatography, compared with unstressed control. UVA light exposu...
journal_title：Journal of pharmaceutical sciences
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journal_title：Journal of pharmaceutical sciences
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更新日期：2018-04-01 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：:The in vitro uptake study was performed using the isolated cells of human oral mucosa, buccal and the dorsum of the tongue, to investigate the mechanisms of glucose uptake. The uptake of D-glucose was much larger in cells of the dorsum of the tongue than in buccal cells and was inhibited more extensively by 2-deoxy-D-...
journal_title：Journal of pharmaceutical sciences
pub_type： 临床试验,杂志文章
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更新日期：1999-08-01 00:00:00
abstract：:Certain disulfide analogues of cystamine were prepared and evaluated for the ability to inhibit gamma-glutamylcysteine synthetase (GCS), the rate-limiting enzyme in glutathione synthesis. The compound SAPH-3 disulfide (2a) was found to be the most effective inactivator of GCS reported to date. Studies of structural an...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600800404
更新日期：1991-04-01 00:00:00
abstract：:Alginate microparticles incorporating hydrocortisone hemisuccinate were produced by aerosolization and homogenization methods to investigate their potential for colonic drug delivery. Microparticle stabilization was achieved by CaCl2 crosslinking solution (0.5 M and 1 M), and drug loading was accomplished by diffusion...
journal_title：Journal of pharmaceutical sciences
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doi：10.1016/j.xphs.2016.08.015
更新日期：2017-01-01 00:00:00
abstract：:The area under the plasma concentration-time curve (AUC) was measured after an intravenous injection of sodium salicylate and after intragastric administration of aspirin, using either an intermittent sampling and the trapezoid rule (AUC-trapezoid) or the recently introduced constant blood withdrawal method (AUC-integ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600670644
更新日期：1978-06-01 00:00:00
abstract：:Spray-dried dispersions (SDDs) are an important technology for enhancing the oral bioavailability of poorly water-soluble drugs. To design an effective oral SDD formulation, the key rate-determining step(s) for oral drug absorption must be understood. This work combined in vivo and in vitro tests with in silico modeli...
journal_title：Journal of pharmaceutical sciences
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doi：10.1016/j.xphs.2018.09.031
更新日期：2019-01-01 00:00:00
