Abstract:
:Exposure of 4-methoxy-2-(3-phenyl-2-propynyl)phenol (CO/1828) to air and light (accelerated by temperature) yields 1-(2-hydroxy-5- methoxyphenyl)-3-phenylpropynone as the major degradation product. With extraction, this product rapidly degrades to 5-methoxyaurone and 6-methoxyflavone. In addition, a mixture of dimeric and heterodimeric compounds that are not fully identified was observed. These results indicate the formation of a reactive ortho-quinone methide as an unstable intermediate. This hypothesis is supported by evidence that the aurone slowly isomerizes into the flavone in control samples. Identification of compounds was accomplished with mass spectrometry, nuclear magnetic resonance spectrometry, UV-high-performance liquid chromatography, and comparison with authentic samples.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Schiavi M,Serafini S,Italia A,Villa M,Fronza G,Selva Adoi
10.1002/jps.2600810818subject
Has Abstractpub_date
1992-08-01 00:00:00pages
812-4issue
8eissn
0022-3549issn
1520-6017pii
S0022-3549(15)48911-7journal_volume
81pub_type
杂志文章abstract::Amphiphilic cyclodextrins (CDs) are biocompatible derivatives of natural CDs and are able to form nanoparticles or polyplexes spontaneously. In this study, nanoparticles prepared from nonionic (6OCaproβCD) or cationic amphiphilic CD (PC βCDC6) were used comparatively to develop nanoparticles intended for breast cancer...
journal_title:Journal of pharmaceutical sciences
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abstract::This investigation was designed to quantitate and compare in the rat the oral absorption characteristics of micronized griseofulvin from a corn oil-in-water emulsion dosage form containing suspended drug and a control aqueous suspension after single-dose (50 mg/kg) and multiple-dose (50 mg/kg every 12 hr for five dose...
journal_title:Journal of pharmaceutical sciences
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doi:10.1002/jps.2600640910
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abstract::The in vivo dissolution of many poorly soluble drugs is enhanced by the action of surfactants secreted into the upper gastrointestinal (GI) tract. These substances may act by solubilizing individual drug molecules into two separate liquid phases: the free aqueous phase and a micellar phase in which the drug is incorpo...
journal_title:Journal of pharmaceutical sciences
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abstract::The solvent-free melt electrospinning (MES) method was developed to prepare a drug delivery system with fast release of carvedilol (CAR), a drug with poor water solubility. To the authors knowledge, this is the first report for preparing drug-loaded melt electrospun fibers. Cationic methacrylate copolymer of Eudragit®...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.23374
更新日期:2013-02-01 00:00:00
abstract::In the present study, a previously described sulfenamide prodrug of a basic antidiabetic drug, metformin, was evaluated further. This sulfenamide prodrug was designed to improve the permeability and consequently the oral absorption and bioavailability (F) of the highly water-soluble metformin. Bioactivation of the pro...
journal_title:Journal of pharmaceutical sciences
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abstract::The interaction of cyclosporin A (CsA) with dimethyl-alpha- and -beta-cyclodextrins (DM-alpha-CyD and DM-beta-CyD) was investigated by the solubility method, electrospray ionization mass spectrometry (ESI-MS) and 1H-nuclear magnetic resonance spectroscopy (1H NMR). The extremely low solubility (1.9 x 10(-5) M at 25 de...
journal_title:Journal of pharmaceutical sciences
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更新日期:1999-01-01 00:00:00
abstract::Two natural products isolated from the plant Daphne genkwa have been shown to possess antileukemic activity in mice. Genkwadaphnin and yuanhuacine were observed to inhibit DNA and protein synthesis in P-388 leukemic cells. A detailed study of the effects of these two diterpene esters on protein synthesis of leukemic c...
journal_title:Journal of pharmaceutical sciences
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doi:10.1002/jps.2600711208
更新日期:1982-12-01 00:00:00
abstract::Sol-to-gel systems of ciprofloxacin hydrochloride were prepared utilizing the phase transition properties of hydroxy propyl methyl cellulose K 15 M grade (HPMC) and carbopol 934. The sol-to-gel systems were sterilized by gamma radiation and/or filtration. The sol-to-gel systems were evaluated for rheological character...
journal_title:Journal of pharmaceutical sciences
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abstract::Nadolol was extracted from tablet excipients with an acidic potassium chloride solution. The drug was oxidized with periodic acid, and the resulting aldehyde was reacted with 2,4-dinitrophenylhydrazine to form the corresponding hydrazone. Excess reagent was removed with a cupric chloride solution. The hydrazone was ex...
journal_title:Journal of pharmaceutical sciences
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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
doi:10.1002/jps.2600840225
更新日期:1995-02-01 00:00:00
abstract::By using data from a sample of 1767 community pharmacies, a total cost function was estimated by a polynomial regression of total cost on output. The Cobb-Douglas production function was estimated by a multiple linear regression of natural logarithmic transformations of output on natural logarithmic transformation of ...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600650208
更新日期:1976-02-01 00:00:00
abstract::A high-performance liquid chromatographic method was developed for the simultaneous determination of azobenzene, hydrazobenzene, and four other decomposition products in phenylbutazone injectable formulations. Separation was achieved on a C18 column, with 0.1 M Tris-citrate buffer (pH 5.25) and acetonitrile (52:48), a...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600731211
更新日期:1984-12-01 00:00:00
abstract::In many manufacturing and research areas, the ability to accurately monitor and characterize nanoparticles is becoming increasingly important. Nanoparticle tracking analysis is rapidly becoming a standard method for this characterization, yet several key factors in data acquisition and analysis may affect results. Nan...
journal_title:Journal of pharmaceutical sciences
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doi:10.1016/j.xphs.2016.02.005
更新日期:2016-04-01 00:00:00
abstract::A quantitative high-pressure liquid chromatographic method, using a reversed-phase column coupled to a fluorescence detector, was developed to determine salicylic acid in bulk aspirin and plain and buffered aspirin tablets. The aspirin was dissolved, filtered, and injected into the chromatograph; the fluorescence of t...
journal_title:Journal of pharmaceutical sciences
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abstract::Levetiracetam therapy is often associated with high levels of individual variation in the recommended dose required to achieve preferential treatment. Thus, a reliable and dynamic regulation system to accurately tailor dose is necessary. The main objective of this study is to explore and prepare a dose-flexible contro...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1016/j.xphs.2018.10.001
更新日期:2019-02-01 00:00:00
abstract::The aim of this study to administer hydrocortisone (HC) percutaneously in the form of polymeric nanoparticles (NPs) to alleviate its transcutaneous absorption, and to derive additional wound-healing benefits of chitosan. HC-loaded NPs had varied particle sizes, zeta potentials, and entrapment efficiencies, when drug-t...
journal_title:Journal of pharmaceutical sciences
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doi:10.1002/jps.23446
更新日期:2013-03-01 00:00:00
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
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abstract::Protein immunogenicity is intensively researched by academics, biopharmaceutical companies, and authorities as it can compromise the safety and efficacy of a biopharmaceutical drug. So far, the exact protein aggregate properties inducing immune responses are not known. Possible protein-related factors could be size, c...
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abstract::Modifications of antibacterial activity have been demonstrated using combinations of two antibacterials from trimethoprim, sulfonamides (sulfadiazine, sulfamerazine, and silver sulfadiazine), silver nitrate, and dibromopropamidine isethionate, either formulated in a cream base or dissolved in peptone water. The creams...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600800912
更新日期:1991-09-01 00:00:00
abstract::This study was designed to examine the effect of benzalkonium chloride/ethylenediaminetetraacetic acid (BAK/EDTA) on the ocular bioavailability (Focular) of ketorolac tromethamine after ocular instillation to normal and de-epithelialized corneas of rabbits both in vitro and in vivo. The in vitro Focular of the formula...
journal_title:Journal of pharmaceutical sciences
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doi:10.1021/js9504189
更新日期:1996-04-01 00:00:00
abstract::Recent oxidation events on monoclonal antibody candidates prompted us to investigate the mechanism of oxidation of Met, Trp, and His residues and to search for suitable stabilizers. By using parathyroid hormone (1-34), PTH, as a model protein and various oxidants, aided by liquid chromatography, peptide mapping, and m...
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pub_type: 杂志文章
doi:10.1002/jps.21746
更新日期:2009-12-01 00:00:00
abstract::Continuing work on the interaction of inorganic additives with nonionic surfactants in aqueous solution dealt with their effect on the CMC and surface tension. The surfactants were octoxynol and polyoxyethylated oleyl alcohol, containing an average of 9.5 and 10 ethylene oxide units, respectively. Their CMC values wer...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600650706
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abstract::The rising popularity of microwaves for drying, material processing and quality sensing has fuelled the need for knowledge concerning dielectric properties of common pharmaceutical materials. This article represents one of the few reports on the density and moisture content dependence of the dielectric properties of p...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.21872
更新日期:2010-02-01 00:00:00
abstract::The complete pH-rate profile of the hydrolysis reaction of aspirin, requiring many experiments in the past, was obtained by a single variable-parameter kinetic experiment carried out by varying the hydrogen ion concentration. The experiment was carried out spectrophotometrically, reading automatically absorbance, pH, ...
journal_title:Journal of pharmaceutical sciences
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abstract::The penetration of benzyl alcohol (BA) through split-thickness cadaver skin was measured in nonoccluded Franz cells placed in a fume hood. BA, dissolved in a small volume of ethanol and spiked with (14)C radiolabel, was applied to skin at nine doses ranging from 0.9 to 10600 microg/cm(2). The percentage of radioactivi...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.20513
更新日期:2006-02-01 00:00:00
abstract::The effects of cyclazocine, a narcotic agonist/antagonist, on the uptake, metabolism, and turnover of norepinephrine in rat brains were studied. Cyclazocine significantly depressed the accumulation of intracisternally administered [3H]norepinephrine and the formation of 3,4-[3H]dihydroxymandelic acid but did not alter...
journal_title:Journal of pharmaceutical sciences
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abstract::Condensations of carbon disulfide were carried out with amino, chloro, and diamino heterocycles to give condensed ring thiazoline-2-thiones and imidazoline-2-thiones, with cyanomethyl heterocycles to give dithio acid derivatives, and with heterocyclic sulfonamides to give sulfonyldithiocarbamates. Of several examples ...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600640823
更新日期:1975-08-01 00:00:00
abstract::Corneal penetration studies were conducted in unanesthetized albino rabbits using various organic compounds representing both polar and nonpolar species. Very low molecular weight compounds demonstrate rapid uptake into the aqueous humor despite the lipid-like barrier imposed by the corneal epithelium. Evidence that t...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600770103
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abstract::The affinity chromatographic technique was used to study the interaction of bovine serum albumin and salicylic acid at 3.3 +/- 1.1 degrees. Beaded agarose gel, on which the albumin was immobilized by covalent linkage, was packed in a column as an affinity adsorbent. Frontal analysis was performed on this column to eva...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600670737
更新日期:1978-07-01 00:00:00