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.
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Lipoxygenase inhibitor FLM 5011, an effective protectant of myocardial microvessels against ischemia-reperfusion injury? An ultrastructural-morphometric study.
Exp Toxicol Pathol
March 2000
Institute of Anatomy, University of Leipzig, Germany.
The lipoxygenase inhibitor FLM 5011 was used for protection of the coronary microcirculation against ischemia/ reperfusion injury after ligation of the left coronary artery in dogs. Epimyocardial biopsies from ischemic and non-ischemic areas of protected and unprotected areas taken before and after ischemia of 90 min duration and after 180 min reperfusion were analysed by means of electron microscopic morphometry. The ischemic injury consisted in endothelial swelling, luminal blebbing, and formation of irregular protrusions, partly occurrence of pericapillary edema and cellular debris.
View Article and Find Full Text PDFThe protective effect of lipoxygenase inhibitor FLM 5011 on mitochondria ultrastructure of ischemic and reperfused cardiomyocytes.
Exp Toxicol Pathol
May 1999
Institute of Anatomy, University of Leipzig, Germany.
Lipoxygenase inhibitor FLM 5011 was used in experimental ischemia and reperfusion with dogs to investigate its ultrastructure-preserving effects on the mitochondria of myocardium. Ischemic and non-ischemic areas of the heart were ultrastructural-morphometric analysed, which revealed that FLM 5011 was able to diminish ischemic damage especially of mitochondria. The protective effects on mitochondria consisted mainly in reduction of defective intramitochondrial areas and in excellent protection of the structural integrity of cristae and matrix.
View Article and Find Full Text PDFBiotransformation and toxicity of the lipoxygenase inhibitor 2-hydroxy-5-methyllaurophenone oxime (FLM 5011) on Hep G2 cells.
Arch Pharm (Weinheim)
October 1998
Institut für Pharmazie, Humboldt Universität zu Berlin, Germany.
2-Hydroxy-5-methyllaurophenone oxime (FLM 5011) is an inhibitor of lipoxygenase with antiinflammatory and antiallergic actions. We incubated FLM 5011 on the human immortal cell line Hep G2 and found a similar metabolite spectrum as in rat urine and faeces. We also measured the cytotoxicity of FLM 5011 on Hep G2 monolayers by the amido black assay and found that the influence of cell proliferation is partly due to apoptotic activities.
View Article and Find Full Text PDF[Biotransformation of the lipoxygenase inhibitor 2-hydroxy-5-methyl-laurophenone-oxime (FLM 5011)].
Pharmazie
June 1996
Institut für Pharmazie, Humboldt-Universität zu Berlin, Germany.
2-Hydroxy-5-methyl-laurophenone-oxime (FLM 5011, 1) is an inhibitor of the lipoxygenase with antiinflammatory and antiallergic actions. The studies on the biotransformation using in vivo investigations and in vitro test systems resulted in finding of at least eight metabolites. Four of these compounds have been detected and identified in urine and faeces after p.
View Article and Find Full Text PDF[Improvement of the absorption of the active substance 2'-hydroxy-5'-methyllaurophenoxamine (FLM 5011) with prodrugs and preparations].
Pharmazie
September 1993
Fachbereich Pharmazie, Martin-Luther-Universität Halle.
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.
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