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Phenytoin‐Lipid Conjugates as Potential Prodrugs of Phenytoin
Author(s) -
Scriba Gerhard K. E.
Publication year - 1993
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.19933260810
Subject(s) - phenytoin , chemistry , prodrug , conjugate , pancreatic lipase , lipase , biochemistry , enzyme , epilepsy , mathematical analysis , mathematics , neuroscience , biology
Phenytoin‐1‐triglycerides and phenytoin‐2‐triglycerides were synthesized as potential prodrugs of phenytoin by covalent binding of 3‐hydroxymethylphenytoin by succinic acid to the positions 1 and 2 of diglycerides, respectively. The corresponding 1‐ and 2‐monoglycerides were prepared. In addition, replacement of glycerol by 3‐hydroxy‐2‐hydroxymethylpropionic acid furnished lipids that allowed direct coupling of 3‐hydroxyme‐thylphenytoin. The lipid conjugates proved to be substrates for pancreatic lipase in vitro .