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  • cyclosporine  (2)
  • 2-Azoniaallene salts  (1)
  • Inorganic Chemistry  (1)
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  • 1
    Digitale Medien
    Digitale Medien
    Improved Dose Linearity of Cyclosporine Pharmacokinetics from a Microemulsion Formulation (1994)
    Springer
    Pharmaceutical research 11 (1994), S. 301-304 
    Details
    ISSN: 1573-904X
    Schlagwort(e): cyclosporine ; dose proportionality ; pharmacokinetics ; formulation
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie
    Notizen: Abstract The pharmacokinetic dose proportionality and relative bioavailability of cyclosporine from a microemulsion formulation (Sandimmune Neoral) were compared to those of the commercial formulation (Sandimmune) over the dosage range 200 to 800 mg. Single oral administrations were given as soft gelatin capsules in an open randomized study with 48 healthy volunteers. Whole-blood cyclosporine concentrations were determined by a specific monoclonal radio-immunoassay. In comparison to Sandimmune, the absorption rate (maximum concentration) and systemic availability (area under the curve) of cyclosporine were greater for Sandimmune Neoral at all dose levels investigated. The area under the curve for Sandimmune increased in a less than proportional manner with respect to dose, whereas that for Sandimmune Neoral was consistent with linear pharmacokinetics. Because of this difference, no global assessment of relative bioavailability could be performed. The relative bioavailability of cyclosporine from Sandimmune Neoral ranged from 174 to 239% compared to Sandimmune, depending on the dose level. The improvements in oral bioavailability and dose linearity of cyclosporine exposure after administration as Sandimmune Neoral should facilitate more accurate dosage titration in the clinical setting.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1023/A:1018923912135
    Standort Signatur Erwartet Verfügbarkeit
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  • 2
    Digitale Medien
    Digitale Medien
    Influence of a Fat-Rich Meal on the Pharmacokinetics of a New Oral Formulation of Cyclosporine in a Crossover Comparison with the Market Formulation (1994)
    Springer
    Pharmaceutical research 11 (1994), S. 151-155 
    Details
    ISSN: 1573-904X
    Schlagwort(e): cyclosporine ; food effect ; pharmacokinetics ; formulation
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie
    Notizen: Abstract The influence of a fat-rich meal on the pharmacokinetics of cyclosporine from a new oral formulation (Sandimmune Neoral) was compared in a randomized, four-way crossover study to the currently marketed formulation (Sandimmune) in 24 healthy male volunteers. Single oral doses of 300 mg Sandimmune and 180 mg Sandimmune Neoral were each administered once under fasting conditions and once 30 min after starting a high-fat meal. Serial blood samples were obtained over a 48-hr period after each administration, and whole-blood cyclosporine concentrations were determined by a specific monoclonal radioimmunoassay method. Food had a marked effect on cyclosporine absorption from Sandimmune manifested by a nearly doubled time to reach the peak concentration and a 37% increase in the area under the curve. This was associated with significant elevations in subsequent whole-blood cyclosporine concentrations compared to the fasting administration. For Sandimmune Neoral the influence was less pronounced. The maximum concentration was decreased by 26%, without a relevant change in the time to reach the peak; the area under the curve showed a slight reduction of 15%. The relatively minor influence of a fat-rich meal on the absorption of cyclosporine from Sandimmune Neoral is advantageous when individualizing a dosage regimen under clinical and out-patient administration conditions.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1023/A:1018922517162
    Standort Signatur Erwartet Verfügbarkeit
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  • 3
    Digitale Medien
    Digitale Medien
    Reactions of 1-Thia-3-azoniabutatriene Salts with Alcohols, Carbonyl Compounds, Diazoalkanes, Nitrile Oxides, Nitrones, Enamines, and Butadienes (1991)
    Weinheim : Wiley-Blackwell
    Berichte der deutschen chemischen Gesellschaft 124 (1991), S. 2537-2544 
    Details
    ISSN: 0009-2940
    Schlagwort(e): 1-Thia-3-azoniabutatriene salts ; 2-Azoniaallene salts ; 1,3-Dipolar cycloadditions ; Chemistry ; Inorganic Chemistry
    Quelle: Wiley InterScience Backfile Collection 1832-2000
    Thema: Chemie und Pharmazie
    Notizen: 1-Thia-3-azoniabutatriene salts 1 react with alcohols, carbonyl compounds, diazo alkanes, nitrile oxides, nitrones, enamines, and 1,3-butadienes in all cases at the C=S double bond to yield new types of 2-azoniaallene salts (3, 9a, b, 13a, b, 18, 22) and other imines (2, 20). An X-ray diffraction analysis for 9b, the reaction product of 1b with 9-diazofluorene, confirms the proposed constitution.
    Zusätzliches Material: 1 Ill.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1002/cber.19911241124
    Standort Signatur Erwartet Verfügbarkeit
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