Stereoselective pharmacokinetics and inversion of suprofen enantiomers in humans.


:The stereoselective pharmacokinetics of suprofen enantiomers has been studied in humans by means of stable isotope-labeled pseudoracemate-diastereomer methodology. After a single oral dose of a near equimolar mixture of unlabeled-(R)-(-)- and [2H3]-(S)-(+)-suprofen [or unlabeled-(S)- and [2H3]-(R)-suprofen] to three healthy male subjects, the plasma concentrations of drug were determined by a stereospecific gas chromatography-mass spectrometry method. Racemic [2H7]suprofen was used as an internal standard. The method involved chiral derivatization with (S)-(-)-1-(naphthyl)ethylamine to form the diastereomeric amide. The plasma concentrations were consistently higher for the (R)-isomer than the (S)-isomer. No significant difference in the elimination half-life of the enantiomers was observed. An average of 6.8% of an administered dose of the (R)-isomer was stereospecifically inverted to the (S)-isomer. There was no measurable inversion of the (S)- to (R)-isomer. The present stable isotope-labeled pseudoracemate-diastereomer methodology has made it possible to evaluate the pharmacokinetics of each enantiomer, including the estimation of chiral inversion after administration of the racemic mixture.


J Pharm Sci


Shinohara Y,Magara H,Baba S




Has Abstract


1991-11-01 00:00:00














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    abstract::By the use of NMR spectroscopy, the highly colored reaction products formed by ouabain or digitoxin in with 1,3,5-trinitrobenzene or 2,4,6-trinitroanisole in the presence of alkali (as used for the determination of these glycosides) are shown to be Meisenheimer complexes. The complexes are produced by attachment of a ...

    journal_title:Journal of pharmaceutical sciences

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    authors: Burns LB,Stedman RJ,Tuckerman MM

    更新日期:1977-05-01 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

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

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  • Safety and Biosimilarity of ior®LeukoCIM Compared to Neupogen® Based on Toxicity, Pharmacodynamic, and Pharmacokinetic Studies in the Sprague-Dawley Rat.

    abstract::This study examined the safety, pharmacodynamic and pharmacokinetic similarity of the human recombinant filgrastim products ior®LeukoCIM and Neupogen® following a 28-day repeated subcutaneous dose administration in male and female Sprague-Dawley rats with a 14-day recovery period. Safety profiling was based on clinica...

    journal_title:Journal of pharmaceutical sciences

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    authors: Licollari A,Riddle K,Taylor SR,Ledon N,Bolger GT

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    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Fleming R,Guy RH,Hadgraft J

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  • Simultaneous determination of methyl, ethyl, propyl, and butyl 4-hydroxybenzoates and 4-hydroxybenzoic acid in liquid antacid formulations by gas chromatography.

    abstract::An isothermal chromatographic (GC) method employing an SE-30 column and flame-ionization detection has been developed for the simultaneous assay of methyl, ethyl, propyl, and butyl 4-hydroxybenzoates and 4-hydroxybenzoic acid in liquid antacid formulations. The method, which uses a silica column chromatographic cleanu...

    journal_title:Journal of pharmaceutical sciences

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    authors: Schieffer GW,Palermo PJ,Pollard-Walker S

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  • Application of salivary concentration data to pharmacokinetic studies with antipyrine.

    abstract::The concentrations of antipyrine in plasma and saliva were equivalent in normal volunteers and in patients with acute viral hepatitis following oral doses of antipyrine. Estimates of clearance, volume of distribution, and half-life made from either plasma or saliva samples were not statistically different in these sub...

    journal_title:Journal of pharmaceutical sciences

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    authors: Meffin PJ,Williams RL,Blaschke TF,Rowland M

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    journal_title:Journal of pharmaceutical sciences

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  • Comparison of the pharmacokinetics of dolasetron and its major active metabolite, reduced dolasetron, in dog.

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  • Stabilization of human papillomavirus virus-like particles by non-ionic surfactants.

    abstract::Human papillomavirus (HPV) virus-like-particles (VLPs) produced by recombinant expression systems are promising vaccine candidates for prevention of cervical cancers as well as genital warts. At high protein concentrations, HPV VLPs, comprised of the viral capsid protein L1 and expressed and purified from yeast, are p...

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    journal_title:Journal of pharmaceutical sciences

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    journal_title:Journal of pharmaceutical sciences

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    journal_title:Journal of pharmaceutical sciences

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    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Vladescu I,Lieleg O,Jang S,Ribbeck K

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    pub_type: 杂志文章


    authors: Strauch S,Jantratid E,Stahl M,Rägo L,Dressman JB

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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: Hori R,Komada F,Okumura K

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