Isomerization of ceftibuten in aqueous solution.


:The isomerization reactions of ceftibuten and ceftibuten-related compounds in aqueous solution were investigated to estimate the substitution effect on the isomerization reaction and identify the three proximal dissociation constants of ceftibuten kinetically from the pH-rate profiles. The isomerization reaction of ceftibuten-related compounds was influenced by the substituents near the double bond at the C7-side chain, and the electron-withdrawing substituent was found to increase the isomerization rate. Ceftibuten isomerized at the C7-side chain, and the isomerization rate was influenced by the dissociation of the C7-side chain carboxylic acid and aminothiazole in the acidic pH region. The dissociation constants of ceftibuten were assigned by comparing the isomerization rates of ceftibuten with its related compounds at various pH conditions, and the pKas 2.3, 3.2, and 4.5 were attributed to the 4-carboxylic acid, 7-carboxylic acid, and 7-aminothiazole, respectively.


J Pharm Sci


Hashimoto N,Hirano K




Has Abstract


1998-09-01 00:00:00














  • Effects of film coatings on tablet hardness.

    abstract::The effects of five conventional film-coating materials on tablet hardness were studied. Placebos showed apparently linear increases in hardness as coatings were applied. Completely coated samples exhibited hardness increases from 50 to 140%, with a corresponding 3% increase in tablet weight. Equations were derived re...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Stern PW

    更新日期:1976-09-01 00:00:00

  • Determination of salicylamide and five metabolites in biological fluids by high-performance liquid chromatography.

    abstract::Two high-performance liquid chromatographic (HPLC) assay procedures were developed for the determination of salicylamide and its metabolites in serum, urine, and saliva. One method involves reverse-phase ion-pair chromatography and UV detection, and is used to determine salicylamide, salicylamide glucuronide, and sali...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Morris ME,Levy G

    更新日期:1983-06-01 00:00:00

  • Determination of mianserin and metabolites in plasma by liquid chromatography with electrochemical detection.

    abstract::A procedure for the determination of mianserin, desmethylmianserin, and 8-hydroxymianserin in plasma at therapeutic concentrations by liquid chromatography with electrochemical detection is described. Following a multiple-step extraction from alkaline plasma into methyl-tert-butyl ether, the reconstituted extract was ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Suckow RF,Cooper TB,Quitkin FM,Stewart JW

    更新日期:1982-08-01 00:00:00

  • A Physiologically Based Pharmacokinetic Modeling Approach to Predict Drug-Drug Interactions of Buprenorphine After Subcutaneous Administration of CAM2038 With Perpetrators of CYP3A4.

    abstract::CAM2038, FluidCrystal injection depot, is an extended release formulation of buprenorphine given subcutaneously every 1 week (Q1W) or every 4 weeks (Q4W). The purpose of this research was to predict the magnitude of drug-drug interaction (DDI) after coadministration of a strong CYP3A4 inducer or inhibitor using physio...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Liu T,Gobburu JVS

    更新日期:2018-03-01 00:00:00

  • Automated potentiometric procedure for studying dissolution kinetics acidic drugs under sink conditions.

    abstract::An automated potentiometric procedure was used for studying in vitro dissolution kinetics of acidic drugs. Theoretical considerations indicated that the pH-stat method could be used to establish approximate sink conditions or, possibly, a perfect sink. Data obtained from dissolution studies using the pH-stat method we...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Underwood FL,Cadwallader DE

    更新日期:1978-08-01 00:00:00

  • Development and optimization of self-nanoemulsifying drug delivery system with enhanced bioavailability by Box-Behnken design and desirability function.

    abstract::The aim of our study was to characterize and optimize a self-nanoemulsifying drug delivery system (SNEDDS) formulation by a three-factor, three-level Box-Behnken design (BBD) combined with a desirability function. The independent factors were the amounts of Capryol PGMC (X(1)), Tween 20 (X(2)), and Transcutol HP (X(3)...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Marasini N,Yan YD,Poudel BK,Choi HG,Yong CS,Kim JO

    更新日期:2012-12-01 00:00:00

  • The Influence of In Vivo Metabolic Modifications on ADMET Properties of Green Tea Catechins-In Silico Analysis.

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    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Matić S,Jadrijević-Mladar Takač M,Barbarić M,Lučić B,Gall Trošelj K,Stepanić V

    更新日期:2018-11-01 00:00:00

  • Pseudopolymorphism and phase stability in four solid forms of (6R,7R)-7-[2-(5-amino-1,2,4-thiadiazol-3-yl)-(Z)-2-methoxy- iminoacetamid]-3- [(4-carbamoyl-1-quinuclidinio)methyl]-8-oxo-5-thia-1-azabicyclo - [4,2,0]oct-2-ene-2-carboxylate (E1040).

    abstract::(6R,7R)-7-[2-(5-Amino-1,2,4-thiadiazol-3-yl)-(Z)-2-methoxy- iminoacetamid]-3- [(4-carbamoyl-1-quinuclidinio)methyl]-8-oxo-5-thia-1-azabicyclo [4,2,0]oct-2-ene-2-carboxylate (1; E1040) was isolated as alpha-(decahydrate), beta-(pentahydrate), and gamma-form (anhydrate) crystals and the X-ray amorphous form. The relatio...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Ashizawa K,Uchikawa K,Hattori T,Ishibashi Y,Sato T,Miyake Y

    更新日期:1989-11-01 00:00:00

  • In vitro binding of chloroquine to rat muscle preparations.

    abstract::Chloroquine (7-chloro-4-[[4-(diethylamino)-1-methylbutyl]amino]quinoline; CQ) accumulates in the insoluble fraction of rat muscle homogenates with an equilibrium distribution ratio of 7.8 L/kg. This is of a similar magnitude to muscle:plasma ratios observed in vivo. Uptake is approximately linear, even up to concentra...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: MacIntyre AC,Cutler DJ

    更新日期:1986-11-01 00:00:00

  • Ophthalmic Econazole Hydrogels for the Treatment of Fungal Keratitis.

    abstract::Econazole is a feasible alternative treatment in the management of fungal keratitis. Nevertheless, its low water solubility is considered the main limitation to the incorporation into ophthalmic formulations. In this work, econazole nitrate is solubilized by using cyclodextrins to achieve an optimum therapeutic concen...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Díaz-Tomé V,Luaces-Rodríguez A,Silva-Rodríguez J,Blanco-Dorado S,García-Quintanilla L,Llovo-Taboada J,Blanco-Méndez J,García-Otero X,Varela-Fernández R,Herranz M,Gil-Martínez M,Lamas MJ,González-Barcia M,Otero-Espinar FJ,Fern

    更新日期:2018-05-01 00:00:00

  • Physical stability of nonviral plasmid-based therapeutics.

    abstract::Nonviral, plasmid-based therapeutics are a new class of pharmaceutical agents that offer the potential to cure many diseases that are currently considered untreatable. While nonviral vectors have shown promise in clinical trials, their physical instability in liquid formulations represents a major barrier to the devel...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章,评审


    authors: Anchordoquy TJ,Koe GS

    更新日期:2000-03-01 00:00:00

  • Autoxidation of tetrazepam in tablets: prediction of degradation impurities from the oxidative behavior in solution.

    abstract::The major route of degradation of tetrazepam (1) is oxidation to 7-chloro-5-(3-keto-cyclohexen-1-yl)-1,3-dihydro-1-methyl-2H-1, 4-benzodiazepin-2-one (3) via the stable 7-chloro-5-(3-hydroperoxy-cyclohexen-1-yl)-1,3-dihydro-1-methyl-2H -1, 4 benzodiazepin-2-one (2). Minor degradation products are 7-chloro-5-(1,2-epoxy...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Boccardi G,Deleuze C,Gachon M,Palmisano G,Vergnaud JP

    更新日期:1992-02-01 00:00:00

  • Rapid GLC determination of fusaric acid in biological fluids.

    abstract::A simple, sensitive GLC assay was developed for fusaric acid, the active metabolite of bupicomide, to follow the disposition of this investigational antihypertensive agent in patients undergoing therapy. Fusaric acid is efficiently extracted from biological samples, derivatized by on-column methylation, and chromatogr...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Fung KK,Koda RT,Maronde RF,Cohen JL

    更新日期:1976-04-01 00:00:00

  • Moisture sorption kinetics for water-soluble substances. I: Theoretical considerations of heat transport control.

    abstract::A model based on heat transport control was developed to describe the uptake of water on a deliquescent solid in an atmosphere of pure water vapor. The model assumes the presence of a saturated liquid film on the surface of the solid. The decrease in the vapor pressure of water over the surface, brought about by the c...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Van Campen L,Amidon GL,Zografi G

    更新日期:1983-12-01 00:00:00

  • Uptake of acetazolamide by human erythrocytes in vitro.

    abstract::The binding of acetazolamide to human erythrocytes was studied in vitro. Blood and plasma samples were analyzed by electron-capture GLC. At 37 degrees, drug equilibrated between plasma and erythrocytes in approximately 40 min. The effect of plasma concentration on the steady-state level of drug within the erythrocytes...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Wallace SM,Reigelman S

    更新日期:1977-05-01 00:00:00

  • Determination of a quaternary mixture of vitamins B6, B1, and B12 and uridine 5'-triphosphate, by derivative spectrophotometry.

    abstract::A new method for determining a quaternary mixture of vitamins B6, B1, and B12 and uridine 5'-triphosphate (UPT) using second-derivative spectrophotometry is described. Calibration graphs were linear up to 30 micrograms/mL of vitamin B6 at 307 nm (r = 0.9999) and vitamin B1 at 282.7 nm (r = 0.9997) and up to 35 microgr...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Morelli B

    更新日期:1995-01-01 00:00:00

  • Antitumor agents LV: Effects of genkwadaphnin and yuanhuacine on nucleic acid synthesis of P-388 lymphocytic leukemia cells.

    abstract::The diterpene esters, genkwadaphnin and yuanhuacine, have been shown to possess significant antileukemic activity in the P-388 screen. The major metabolic effects of the diterpene esters were on DNA and protein synthesis. The effects on DNA synthesis in vitro were evoked at a lower concentration than that required for...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Hall IH,Kasai R,Wu RY,Tagahara K,Lee KH

    更新日期:1982-11-01 00:00:00

  • The Effect of Genetic Polymorphism on the Inhibition of Azole Antifungal Agents Against CYP2C9-Mediated Metabolism.

    abstract::We investigated the effect of cytochrome P450 (CYP) 2C9 polymorphism on the inhibition of methylhydroxylation activity of tolbutamide, a typical CYP2C9 substrate, by triazole antifungal agents, fluconazole and voriconazole. Although the Michaelis constants (Km), maximal velocities (Vmax), and Vmax/Km values for CYP2C9...

    journal_title:Journal of pharmaceutical sciences

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    authors: Niwa T,Hata T

    更新日期:2016-03-01 00:00:00

  • Preformulation study of pelrinone hydrochloride.

    abstract::Pelrinone HCl is essentially nonhygroscopic. The pH-solubility profile exhibits a U-shaped curve, while the octanol-water partition coefficient-pH profile shows a bell-shaped curve. Two ionizable functions, with a pKa1 value of 4.71 and a pKa2 value of 8.94, produce the cationic and anionic forms, respectively. A weak...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Hajdu J,Adams G,Lee HK

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  • Crystal Structures and Vapor-Induced Crystalline Transformation of 7-Ethyl-10-Hydroxycamptothecin Pseudopolymorphs.

    abstract::Solvent-induced 3 frameworks (the monohydrate, methanol solvate, and dimethyl formamide [DMF] solvate) of an anticancer drug, 7-ethyl-10-hydroxycamptothecin (SN38), were constructed. The crystal structures of the 3 pseudopolymorphs were characterized by single-crystal X-ray diffraction technique for the first time. Cr...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Fang L,Wang L,Yao C,Song S,Wu Z,Tao X

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  • Assessing OATP1B1- and OATP1B3-Mediated Drug-Drug Interaction Potential of Vemurafenib Using R-Value and Physiologically-Based Pharmacokinetic Models.

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    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Kayesh R,Farasyn T,Crowe A,Liu Q,Pahwa S,Alam K,Neuhoff S,Hatley O,Ding K,Yue W

    更新日期:2021-01-01 00:00:00

  • Radioimmunoassay for terfenadine in human plasma.

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    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Cook CE,Williams DL,Myers M,Tallent CR,Leeson GA,Okerholm RA,Wright GJ

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    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: De Bruyn T,Fattah S,Stieger B,Augustijns P,Annaert P

    更新日期:2011-11-01 00:00:00

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    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Schott H,Han SK

    更新日期:1977-02-01 00:00:00

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    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: May EL,Jacobson AE

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    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Rao VM,Haslam JL,Stella VJ

    更新日期:2001-07-01 00:00:00

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    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

  • Drug delivery trends in clinical trials and translational medicine: Updated analysis of database.

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    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


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    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Bartusik-Czubek E,Toboła P,Czubek B,Bednarek M,Balcerek J,Pietrucha T,Jaros S

    更新日期:2021-01-20 00:00:00

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    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Pace AL,Wong RL,Zhang YT,Kao YH,Wang YJ

    更新日期:2013-06-01 00:00:00