[Improvement of the absorption of the active substance 2'-hydroxy-5'-methyllaurophenoxamine (FLM 5011) with prodrugs and preparations].
Methods to improve the absorption of problem drugs are presented for the strongly lipophilic, poorly water-soluble, potential lipoxygenase inhibitor FLM 5011 (1). The water-solubility is improved by using prodrugs or by solubilizing. The characterization of solubility has been characterized with an suitable in vitro model system. The bioavailability of 1 in rabbits after oral administration is markedly increased using 1-prodrugs studied. The good correlation between the ABC measured in vitro and the AUC estimated in vivo demonstrates that it is possible to predict the bioavailability at the rabbit of highly lipophilic drugs such as 1 using the flow through model system.
Tscheuschner
C
C
Fachbereich Pharmazie, Martin-Luther-Universität Halle.
Neubert
R
R
Fürst
W
W
Lücke
L
L
Fries
G
G
D000818:Animals; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical; D007408:Intestinal Absorption; D007850:Lauric Acids; D016859:Lipoxygenase Inhibitors / Q000097:blood / Q000493:pharmacokinetics*; D010091:Oximes; D011355:Prodrugs; D011817:Rabbits; D012995:Solubility
D007850:Lauric Acids; D016859:Lipoxygenase Inhibitors; D010091:Oximes; D011355:Prodrugs; C059535:FLM 5011
Verbesserung der Absorption des Wirkstoffes 2'-Hydroxy-5'-methyllaurophenonoxim (FLM 5011) durch Herstellung von Prodrugs und Zubereitungen.