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  • 1
    Electronic Resource
    Electronic Resource
    Epimerization Kinetics of Moxalactam in Frozen Urine and Plasma Samples (1990)
    Springer
    Pharmaceutical research 7 (1990), S. 364-369 
    Details
    ISSN: 1573-904X
    Keywords: moxalactam ; epimerization ; frozen plasma ; frozen urine ; electrolyte ; protein binding
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The epimerization of moxalactam (LMOX) in frozen urine and plasma samples was studied during long-term storage. The R/S ratio at equilibrium [(R/S)eq] at −10°C was similar in urine and in rat and human plasma ultrafiltrate but differed from that in water. The (R/S)eq values in human plasma and its ultrafiltrate differed slightly, while they were the same in rat plasma and in its ultrafiltrate. The difference for the human plasma and ultrafiltrate may result from differences in plasma protein binding between R- and S-epimers in the liquid region of the frozen plasma. The change of R/S ratio in frozen human plasma continued below the collapse temperature of LMOX aqueous solution, where the liquid region appeared still to exist as determined by NMR measurement. Consequently, the biological LMOX samples should be preserved at or below −70°C to prevent changes in the R/S ratio.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1015815321570
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    Paper (German National Licenses)
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  • 2
    Electronic Resource
    Electronic Resource
    Factors Determining the Intrinsic Lymphatic Partition Rate of Epitiostanol and Mepitiostane (1992)
    Springer
    Pharmaceutical research 9 (1992), S. 1617-1621 
    Details
    ISSN: 1573-904X
    Keywords: mepitiostane ; epitiostanol ; intrinsic lymphatic partition rate ; lipophilicity ; chylomicron
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Substitution of the steroid epitiostanol (EP) at position 17 with methoxycyclopentane yields the extremely lipophilic mepitiostane (MP) with preferential partitioning into the lymph. Most of the MP in the lymph was associated with the core lipids of chylomicrons and very low-density lipoproteins (VLDL), as was also the case for EP. However, the dialysis velocity of EP and MP from lymph to plasma differed greatly; EP, but not MP, was transferred from the lymph to the plasma. This difference was attributed to differences in their unbound fraction in the lymph. Lymphatic transfer and the logP value of several tested steroids correlated well. Therefore, the oral EP prodrug, MP, partitioned into the lymph because of its superlipophilicity and resultant retention in the core lipids of chylomicrons and VLDL.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1015824710957
    Library Location Call Number Volume/Issue/Year Availability
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    Paper (German National Licenses)
    Fulltext
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