Transformation of 2,2'-anhydro-1-beta-D-arabinofuranosylcytosine induced by hydrogen peroxide.


:2,2'-Anhydro-1-beta-D-arabinofuranosylcytosine (I) is a more potent and less toxic antineoplastic agent than is cytarabine (1-beta-D-arabinofuranosylcytosine) (II). The anhydronucleoside (I) was found to be readily transformed by hydrogen peroxide into 2,2'-anhydro-5-hydroxy-1-beta-D-arabinofuranosylcytosine (III) by treatment with 0.025 M hydrogen peroxide at a neutral and slightly basic pH range (pH 6-9) and at room temperature. It was converted into non-UV-absorbing substance(s) by hydrogen peroxide at an alkaline pH (pH 11). Since hydrogen peroxide is produced by redox reactions in all living cells, it may be responsible for the alteration of I. Such transformations by hydrogen peroxide were not observed with cytarabine.


J Pharm Sci


Kikugawa K




Has Abstract


1975-03-01 00:00:00














  • Rough sets in the analysis of the structure-activity relationships of antifungal imidazolium compounds.

    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


    authors: Krysiński J

    更新日期:1995-02-01 00:00:00

  • 2-(methylamino)-5-chlorobenzophenone imine: a novel product formed in base-catalyzed hydrolysis of diazepam.

    abstract::Diazepam (1), a hypnotic and anxiolytic drug in worldwide use, formed an intermediate product in a mixture of ethanol and sodium hydroxide ([NaOH] > or = 1 M). The intermediate product slowly decomposed to form 2-(methylamino)-5-chlorobenzophenone imine (2) and 2-(methylamino)-5-chlorobenzophenone (3). The amount of 2...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Yang SK,Tang R,Yang TJ,Pu QL,Bao Z

    更新日期:1996-07-01 00:00:00

  • Nonlinear enthalpy-entropy compensation for the solubility of phenacetin in dioxane-water solvent mixtures.

    abstract::The solubility of phenacetin was determined at five temperatures in solvent mixtures of aprotic-amphiprotic mixtures of dioxane and water. Enthalpy-entropy compensation analysis is used to study the effect of changing polarity of the medium on the solute. The apparent heats of solution and free energies of solution ar...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Bustamante C,Bustamante P

    更新日期:1996-10-01 00:00:00

  • Adsorption of phosphate by aluminum hydroxycarbonate.

    abstract::Phosphate is specifically adsorbed by aluminum hydroxycarbonate by anion ligand exchange. IR analysis indicated that phosphate exchanged with specifically adsorbed carbonate. Adsorption is favored by low pH and is inversely related to particle size. Adsorption of phosphate decreases the rate of acid neutralization of ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Liu JC,Feldkamp JR,White JL,Hem SL

    更新日期:1984-10-01 00:00:00

  • Development of aqueous parenteral formulations for carbamazepine through the use of modified cyclodextrins.

    abstract::The poor aqueous solubility of carbamazepine was dramatically increased via complexation with various chemically modified beta-cyclodextrins and gamma-cyclodextrins. A preparation of carbamazepine and 2-hydroxypropyl-beta-cyclodextrin was found to be stable to steam sterilization and to storage under a variety of cond...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Brewster ME,Anderson WR,Estes KS,Bodor N

    更新日期:1991-04-01 00:00:00

  • Intrinsic factor-mediated binding of cyanocobalamin to cholestyramine.

    abstract::The intrinsic factor-mediated binding of cyanocobalamin to cholestyramine was studied in vitro under varying conditions of pH, added electrolyte, and bile salt. The intrinsic factor-cyanocobalamin complex was adsorbed strongly by the resin at pH 3 in the presence of neutral salt and low concentrations of glycocholic a...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Andersen KJ,Schjønsby H

    更新日期:1978-11-01 00:00:00

  • Synthesis and irreversible beta-adrenergic blockade with a bromoacetamido derivative of betaxolol.

    abstract::1-[4-(2-Cyclopropylmethoxyethyl)phenoxy]-3-[1-p-(bromoacetamidophe nyl) -2-methyl-2-propylamine]-2-propranol (8), which is a derivative of the beta 1-adrenergic agent betaxolol, was synthesized. Compound 8 showed less potent beta-adrenergic blocking activity than betaxolol in an in vitro test with guinea pig tracheal ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Amlaiky N,Leclerc G

    更新日期:1985-10-01 00:00:00

  • Testosterone-independent down-regulation of Oct2 in the kidney medulla from a uranyl nitrate-induced rat model of acute renal failure: effects on distribution of a model organic cation, tetraethylammonium.

    abstract::Although acute renal failure (ARF) has been an area of extensive research in recent decades, our understanding of ARF is far from complete. Organic cations (OCs) are primarily excreted via vectorial transport by various renal organic cation transporters (OCTs). It is reasonable to assume that ARF may alter the express...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Shim WS,Park JH,Ahn SJ,Han L,Jin QR,Li H,Choi MK,Kim DD,Chung SJ,Shim CK

    更新日期:2009-02-01 00:00:00

  • Metabolism of propranolol during percutaneous absorption in human skin.

    abstract::This in vitro study evaluated the extent of the absorption and metabolism of propranolol in human skin from four sources. Between 10.4 +/- 3.1 and 36.6 +/- 2.6% of the applied dose was absorbed; however, only a small portion (between 4.1 +/- 0.9 and 16.1 +/- 1.3%) of the dose permeated through the skin. Naphthoxyaceti...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Ademola JI,Chow CA,Wester RC,Maibach HI

    更新日期:1993-08-01 00:00:00

  • Interlaboratory comparison of analytical methods for residual ethylene oxide at low concentration levels in medical device materials.

    abstract::An interlaboratory comparison of two extraction methods and one thermal desorption test method for the quantification of ethylene oxide (EO) by gas chromatography in two common medical device materials, high density polyethylene (HDPE) and plasticized polyvinyl chloride (PVC), was conducted by 15 laboratories. The thr...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Lao NT,Lu HT,Rego A,Kosakowski RH,Burgess DJ,Hume RD

    更新日期:1995-05-01 00:00:00

  • Measurement of dissociation constants (pKa values) of organic compounds by multiplexed capillary electrophoresis using aqueous and cosolvent buffers.

    abstract::Evaluation of a multiplexed capillary electrophoresis (CE) method for pK(a) measurements of organic compounds, including low solubility compounds, is presented. The method is validated on a set of 105 diverse compounds, mostly drugs, and results are compared to literature values obtained from multiple references. Two ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Shalaeva M,Kenseth J,Lombardo F,Bastin A

    更新日期:2008-07-01 00:00:00

  • Development of HPLC conditions for valid determination of hydrolysis products of cisplatin.

    abstract::In water, the antineoplastic drug cisplatin, cis-[PtCl2(NH3)2] (1) hydrolyses slowly to the aqua complexes cis-[Pt(NH3)2Cl(H2O)]+ (2) and, to a small extent, cis-[Pt(NH3)2(H2O)2]2+ (3), which are thought to play an important role in the metabolism of cisplatin. HPLC is a useful technique for monitoring 2 and 3, but on...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: El-Khateeb M,Appleton TG,Charles BG,Gahan LR

    更新日期:1999-03-01 00:00:00

  • Soft gelatin capsules II: Oxygen permeability study of capsule shells.

    abstract::A method is reported for studying the effects of several factors at room temperature on the oxygen permeability of soft gelatin capsule shell films. The method involves the use of a permeability cell assembly and the spectrophotometric determïnation of oxygen with an alkaline pyrogallic acid solution. Factors investig...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Hom FS,Veresh SA,Ebert WR

    更新日期:1975-05-01 00:00:00

  • Pharmacokinetics and disposition of a localized lymphatic polymeric hyaluronan conjugate of cisplatin in rodents.

    abstract::Cisplatin (CDDP) is an effective anticancer agent for many solid tumors but has significant systemic toxicity limiting its use in many patients. We have designed a loco-regional delivery system to increase platinum levels in the lymphatics, where early metastasis is most likely to occur, while reducing systemic toxici...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Cai S,Xie Y,Davies NM,Cohen MS,Forrest ML

    更新日期:2010-06-01 00:00:00

  • Per Artursson's Major Contributions to the Caco-2 Cell Literature in Pharmaceutical Sciences.

    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


    authors: Brayden DJ

    更新日期:2021-01-01 00:00:00

  • Enhanced transdermal delivery of sex hormones in swine with a novel topical aerosol.

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    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Morgan TM,Parr RA,Reed BL,Finnin BC

    更新日期:1998-10-01 00:00:00

  • Investigation of PEG crystallization in frozen PEG-sucrose-water solutions: II. Characterization of the equilibrium behavior during freeze-thawing.

    abstract::Our objective was to characterize, by DSC and XRD, the equilibrium thermal behavior of frozen aqueous solutions containing polyethylene glycol (PEG) and sucrose. Aqueous solutions of (i) PEG (2.5-50% w/w), (ii) sucrose (10% w/v) with different concentrations of PEG (1-20% w/v), and (iii) PEG (2% or 10% w/v) with diffe...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Bhatnagar BS,Martin SM,Teagarden DL,Shalaev EY,Suryanarayanan R

    更新日期:2010-11-01 00:00:00

  • Determination of norethindrone stability on red delicious apples.

    abstract::A stability-indicating assay procedure for the determination of norethindrone on the surface of Red Delicious apple slices was developed. The apple slice is homogenized in pH 10 borate buffer solution and norethindrone is then partitioned into chloroform using a diffusion chamber that has a membrane that is permeable ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Mayberry DO,Kowblansky M,Lane PA,Wray PE

    更新日期:1990-08-01 00:00:00

  • A novel calmodulin antagonist O-(4-ethoxyl-butyl)-berbamine overcomes multidrug resistance in drug-resistant MCF-7/ADR breast carcinoma cells.

    abstract::Multidrug resistance (MDR) mediated by the overexpression of the drug efflux protein P-glycoprotein is one of the major obstacles to successful cancer chemotherapy. The development of safe and effective MDR-reversing agents is an important approach to addressing this problem clinically. In this study, we evaluated the...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Liu R,Zhang Y,Chen Y,Qi J,Ren S,Xushi MY,Yang C,Zhu H,Xiong D

    更新日期:2010-07-01 00:00:00

  • Determination of ketoprofen by direct injection of deproteinized body fluids into a high-pressure liquid chromatographic system.

    abstract::A rapid, sensitive, and specific determination of ketoprofen in human and animal deproteinized body fluids by reversed-phase high-pressure liquid chromatography is presented. The acid is detectable in amounts as low as 0.1 microgram/ml. Limits of error are in the range of +/- 5.1% of the sample mean. ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Ballerini R,Cambi A,Del Soldato P,Melani F,Meli A

    更新日期:1979-03-01 00:00:00

  • Degradation of paclitaxel and related compounds in aqueous solutions I: epimerization.

    abstract::Paclitaxel and other taxanes have complex structures including the presence of numerous hydrolytically sensitive ester groups and a chiral center that readily undergoes epimerization thus making their kinetics complex. The present study attempts to understand the mechanism of epimerization at the 7-position of paclita...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Tian J,Stella VJ

    更新日期:2008-03-01 00:00:00

  • Microstructure of calcium stearate matrix pellets: a function of the drying process.

    abstract::Drying is a common pharmaceutical process, whose potential to modify the final drug and/or dosage form properties is often underestimated. In the present study, pellets consisting of the matrix former calcium stearate (CaSt) incorporating the active pharmaceutical ingredient ibuprofen were prepared via wet extrusion a...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Schrank S,Kann B,Windbergs M,Glasser BJ,Zimmer A,Khinast J,Roblegg E

    更新日期:2013-11-01 00:00:00

  • A rapid HPLC method for the quantification of tyrothricin, menthol, and benzocaine in pharmaceutical formulations.

    abstract::A rapid, sensitive, and accurate reversed-phase HPLC method has been developed for the analysis and quantification of pharmaceutical formulations containing tyrothricin (1), an antibiotic used in antiseptic buccal compressed tablets for local application. The assay has been carried out under isocratic conditions, usin...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Caraballo I,Fernandez-Arevalo M,Holgado MA,Vela MT,Rabasco AM

    更新日期:1994-08-01 00:00:00

  • Derivative and graphical procedures for correction of irrelevant UV spectrophotometric absorption in changeable matrixes.

    abstract::The application of direct zero-order UV spectrophotometric and graphical or derivative background correction methods to selected pharmaceutical preparations shows their relative advantages in different situations. The assay of the active components in a changeable matrix is a problem with formulations having a limited...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Traveset J,Such V,Gonzalo R,Gelpi E

    更新日期:1980-06-01 00:00:00

  • Transport Mechanism of Nicotine in Primary Cultured Alveolar Epithelial Cells.

    abstract::Nicotine is absorbed from the lungs into the systemic circulation during cigarette smoking. However, there is little information concerning the transport mechanism of nicotine in alveolar epithelial cells. In this study, we characterized the uptake of nicotine in rat primary cultured type II (TII) and transdifferentia...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Takano M,Nagahiro M,Yumoto R

    更新日期:2016-02-01 00:00:00

  • The Degradation Chemistry of GSK2879552: Salt Selection and Microenvironmental pH Modulation to Stabilize a Cyclopropyl Amine.

    abstract::The cyclopropyl amine moiety in GSK2879552 (1) degrades hydrolytically in high pH conditions. This degradation pathway was observed during long-term stability studies and impacted the shelf life of the drug product. This article describes the work to identify the degradation impurities, elucidate the degradation mecha...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Campbell JM,Lee M,Clawson J,Kennedy-Gabb S,Bethune S,Janiga A,Kindon L,Leach KP

    更新日期:2019-09-01 00:00:00

  • Determination of bacmecillinam, an amdinocillin prodrug, in human and canine whole blood by reversed-phase liquid chromatography.

    abstract::Bacmecillinam is an amdinocillin prodrug designed to be easily hydrolyzed in biological materials, so special procedures were developed for the collection of blood specimens. Whole blood was collected in tubes containing bacampicillin as an adsorption inhibitor and kept at -70 degrees; the extracting solvent, hexane-m...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Westerlund D,Pettersson B,Carlqvist J

    更新日期:1982-10-01 00:00:00

  • 2-Acetylpyridine thiosemicarbazones XI: 2-(alpha-Hydroxyacetyl)pyridine thiosemicarbazones as antimalarial and antibacterial agents.

    abstract::A series of 2-(alpha-hydroxyacetyl)pyridine thiosemicarbazones was synthesized as potential antimalarial and antibacterial agents. Their synthesis was achieved by the condensation of N4-mono- or N4,N4-disubstituted thiosemicarbazides with 2-(alpha-hydroxyacetyl)pyridine. The latter was prepared by selective bromine ox...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Klayman DL,Lin AJ,Hoch JM,Scovill JP,Lambros C,Dobek AS

    更新日期:1984-12-01 00:00:00

  • Cholesterol-Targeted Anticancer and Apoptotic Effects of Anionic and Polycationic Amphiphilic Cyclodextrin Nanoparticles.

    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

    pub_type: 杂志文章


    authors: Varan G,Öncül S,Ercan A,Benito JM,Ortiz Mellet C,Bilensoy E

    更新日期:2016-10-01 00:00:00

  • Structural stability of vault particles.

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    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Esfandiary R,Kickhoefer VA,Rome LH,Joshi SB,Middaugh CR

    更新日期:2009-04-01 00:00:00