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  • Articles: DFG German National Licenses  (5)
  • HPLC chiral stationary phase  (2)
  • antimalarial agents  (2)
  • (R,S)-Ifosfamide  (1)
  • 1
    Electronic Resource
    Electronic Resource
    Measurement of Underivatized Propranolol Enantiomers in Serum Using a Cellulose –Tris(3,5 -Dimethylphenylcarbamate) High-Performance Liquid Chromatographic (HPLC) Chiral Stationary Phase (1988)
    Springer
    Pharmaceutical research 5 (1988), S. 187-189 
    Details
    ISSN: 1573-904X
    Keywords: propanolol enantiomers ; enantioselective high-performance liquid chromatography (HPLC) ; HPLC chiral stationary phase ; serum levels
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract A commercially available high-performance liquid chromatographic (HPLC) chiral stationary phase (HPLC-CSP) has been used to measure serum levels of d- and l-propranolol. The HPLC-CSP is based upon cellulose–tris(3,5-dimethylcarbamate) and is able to stereochemically resolve d- and l-propranolol without precolumn derivatization using a mobile phase composed of hexane:2-propranol:N,N-dimethyloctylamine (92:8:0.01, v/v/v). Under these conditions the observed stereochemical resolution (α) of the two enantiomers was α = 2.2. A subject's concentration–time curve of the two isomers was determined following the ingestion of 160 mg racemic propranolol.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1015921124857
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    Paper (German National Licenses)
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  • 2
    Electronic Resource
    Electronic Resource
    New Insights into the Pharmacokinetics and Metabolism of (R,S)-Ifosfamide in Cancer Patients Using a Population Pharmacokinetic-Metabolism Model (2000)
    Springer
    Pharmaceutical research 17 (2000), S. 645-652 
    Details
    ISSN: 1573-904X
    Keywords: (R,S)-Ifosfamide ; R2-, R3-, S2-, S3-DCE-IFF ; iterative-two stage analysis ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. To describe the pharmacokinetics of R- andS-Ifosfamide (IFF), and their respective 2 and 3 N-dechloroethylated (DCE)metabolites (R2-, R3-, S2, S3-DCE-IFF) in cancer patients. Methods. (R,S)-IFF was administered (1.5 g/m2)daily for 5 days in 13 cancer patients. Plasma and urine samples were collectedand analyzed using an enantioselective GC-MS method. An average of 97observations per patient were simultaneously fitted using apharmacokinetic-metabolism (PK-MB) model. A population PK analysis was performedusing an iterative 2-stage method (IT2S). Results. Auto-induction of IFF metabolism was observed over the 5day period. Increases were seen in IFF clearance (R: 4 vs 7 L/h; S: 5vs 10 L/h), and in the formation of DCE (R: 7 vs 9%; S: 14 vs 19%)and active metabolites (4-OHM-IFF; R: 71 vs 77%; S: 67 vs 71%). Anovel finding of this analysis was that the renal excretion of the DCEmetabolites was also induced. Conclusions. This population PK-MB model for (R,S)-IFF may beuseful in the optimization of patient care, and gives new insight intothe metabolism of (R,S)-IFF.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1007561727948
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  • 3
    Electronic Resource
    Electronic Resource
    Enantioselective chromatography of the antimalarial agents chloroquine, mefloquine, and enpiroline on a α1 -acid glycoprotein chiral stationary phase: Evidence for a multiple-site chiral recognition mechanism (1992)
    New York, NY [u.a.] : Wiley-Blackwell
    Chirality 4 (1992), S. 30-35 
    Details
    ISSN: 0899-0042
    Keywords: chiral liquid chromatography ; α1 -acid glycoprotein ; antimalarial agents ; Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: The effect of mobile phase pH and dimethyloctylamine (DMOA) on the retention (k') and stereoselectivity (α) of antimalarial agents mefloquine, enpiroline, and chloroquine on the α1-acid glycoprotein chiral stationary phase (AGP-CSP) was investigated. An increase of k' with increasing pH was observed while the effect on α was a function of the solute. The magnitude and direction of changes induced by DMOA depended on pH and the structure of the solute.The results of this study are consistent with a change of the conformation of the AGP between pH 5 and 7. At pH 7, the effect of DMOA on mefloquine was relatively well described by a competitive displacement from one enantioselective site. The effect on chloroquine and enpiroline suggests a multiple-site mechanism in which both competitive and allosteric interactions are involved.
    Additional Material: 3 Ill.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/chir.530040108
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    Paper (German National Licenses)
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  • 4
    Electronic Resource
    Electronic Resource
    Chiral resolution of some antimalarial agents by sub- and supercritical fluid chromatography on an (S)-naphthylurea stationary phase (1993)
    New York, NY [u.a.] : Wiley-Blackwell
    Chirality 5 (1993), S. 173-180 
    Details
    ISSN: 0899-0042
    Keywords: (S)-naphthylurea chiral stationary phase ; subcritical fluid chromatography ; supercritical fluid chromatography ; antimalarial agents ; enantiomeric separations ; Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: The behavior of mefloquine, halofantrine, enpiroline, quinine, quinidine, chloroquine and primaquine is studied by subcritical fluid chromatography on a (S)-naphthylurea column (250 mm × 4.6 mm ID) with a subcritical mobile phase composed of carbon dioxide, methanol and triethylamine (flow rate of 3 ml/min). Except for primaquine and chloroquine, each enantiomer was separated at a temperature between 40 and 60°C, and at a pressure below 15 MPa. A 98/2, v/v CO2/methanol 0.1% triethylamine mixture allowed the separation of halofantrine enantiomers while the enantiomers of the more polar metabolite (N-desbutylhalofantrine) were separated with a 80-20 v/v mixture as used for mefloquine, enpiroline, quinine and quinidine. The influence of temperature, pressure and of the nature of the mobile phase is discussed. © 1993 Wiley-Liss, Inc.
    Additional Material: 9 Ill.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/chir.530050313
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    Paper (German National Licenses)
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  • 5
    Electronic Resource
    Electronic Resource
    Immobilized serum albumin: Rapid HPLC probe of stereoselective protein-binding interactions (1990)
    New York, NY [u.a.] : Wiley-Blackwell
    Chirality 2 (1990), S. 263-268 
    Details
    ISSN: 0899-0042
    Keywords: protein binding ; stereoselectivity ; immobilized human serum albumin ; HPLC chiral stationary phase ; chiral drugs ; Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: A human serum albumin-based HPLC chiral stationary phase (HSA-CSP) has been examined as a tool to investigate binding of chiral drugs to HSA and drug-drug protein-binding interactions. Rac-oxazepam hemisuccinate (OXH) was used as a model compound and the chromatographic retention (k′) of its enantiomers was determined after addition of displacers to the mobile phase. Compounds known to bind at the same site as OXH and at different sites were tested for their displacing capacities. Competitive binding interactions between the OXH enantiomers and displacers in the mobile phase were reflected by decreases in the k′s of (R)- and (S)-OXH. The results indicate that retention on the HSA-CSP accurately reflects binding to native HSA and the technique can determine enantioselective and competitive binding interactions at specific sites on HSA. The HSA-CSP was also able to recognize separate binding areas for (S)- and (R)-OXH.
    Additional Material: 3 Ill.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/chir.530020412
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