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  • 1
    Electronic Resource
    Electronic Resource
    Prodrugs of Gestodene for Matrix-Type Transdermal Drug Delivery Systems (1998)
    Springer
    Pharmaceutical research 15 (1998), S. 1419-1424 
    Details
    ISSN: 1573-904X
    Keywords: drug design ; gestodene caproate ; prodrug ; progestin ; transdermal drug delivery system
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. The aim of this study was to enhance the transdermal absorption of the highly active progestin gestodene from matrix type transdermal delivery systems (TDDS) by formation of prodrugs with improved matrix solubility. Methods. Gestodene esters were synthesized via acylation of the drug with the respective carboxylic anhydrides. Subsequently TDDS were produced using the solvent cast method. Selected formulations were examined with in vitro diffusion experiments using skin of nude mice. Results. One prodrug, gestodene caproate proved to be an oil at ambient temperature and showed a very high solubilty of over 10.5% in the TDDS matrix. Within in vitro penetration studies using those systems the prodrug exhibited a significantly higher transdermal penetration rate than gestodene from reference systems. Furthermore, the prodrug was hydrolyzed to the parent drug to a high extent during the passage of the skin. Conclusions. Designing prodrugs to the requirements of matrix TDDS is an efficient way of enhancing the transdermal drug flux rate.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1011957822961
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  • 2
    Electronic Resource
    Electronic Resource
    Radikalinduzierte Reduktion von α,β-ungesättigten Steroidketonen mit Tributylzinnhydrid (1983)
    Weinheim : Wiley-Blackwell
    Liebigs Annalen 1983 (1983), S. 1996-1999 
    Details
    ISSN: 0170-2041
    Keywords: Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Radical-induced Reduction of α,β-Unsaturated Steroid Ketones with Tributyltin HydrideConjugated steroid ketones are reduced stereoselectively with tributyltin hydride in the presence of azobisisobutyronitrile as radical initiator to give the corresponding saturated ketones in high yields.
    Notes: Konjugierte Steroidketone werden mit Tributylzinnhydrid in Gegenwart des Radikalbildners Azobisisobutyronitril stereoselektiv und in hohen Ausbeuten zu den gesättigten Ketonen reduziert.
    Additional Material: 1 Tab.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/jlac.198319831114
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