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Differences in endogenous esterification and retention in the rat trachea between budesonide and ciclesonide active metabolite.
Drug Metab Dispos
October 2007
AstraZeneca Research and Development Lund, Lund, Sweden.
The airway retention of inhaled glucocorticosteroids (GCs) depends largely on their lipophilicity. Inhaled budesonide (BUD) becomes highly lipophilic reversibly by the formation of esters acting as a reservoir of active BUD. Ciclesonide (CIC) was also reported to form esters after hydrolysis to active metabolite (CIC-AM).
View Article and Find Full Text PDFInhibition of purified pig and human liver retinyl ester hydrolase by pharmacologic agents.
Lipids
May 2001
Department of Human Nutrition and Food Science, Christian-Albrechts-Universität zu Kiel, Germany.
Identification of inhibitors of retinyl ester hydrolase (REH) would help to elucidate its role in vitamin A metabolism in vivo. By using standard incubation conditions, the effects of 215 drugs as potential inhibitors of purified pig and human liver REH when acting on micellar substrate retinyl palmitate were evaluated at 16.7, 167, and 1670 microM.
View Article and Find Full Text PDFIn an open randomized cross-over study 800 mg cyclandelate (Natil, CAS 456-59-7) was applicated to 24 young, male volunteers. Before and during 24 h after application of a single dose a 17-channel, quantitative topographical pharmaco-EEG was recorded. A significant increase of the spectral power density was observed in the alpha 2, beta 1 and beta 2 frequency bands starting 2 h after application until 4.
View Article and Find Full Text PDFEffect of food on the bioavailability of cyclandelate from commercial capsules.
Clin Pharmacol Ther
June 1991
Division of Drugs, National Institute of Hygienic Sciences, Tokyo, Japan.
The bioavailability of five capsules of cyclandelate that are commercially available in Japan was determined in ten healthy volunteers by measuring mandelic acid (a main metabolite of cyclandelate) excreted in the urine. Bioinequivalence among the five capsules was demonstrated. The relative cumulative excretion of mandelic acid of the most poorly bioavailable capsule was 38% of the most highly bioavailable capsule.
View Article and Find Full Text PDFIn vivo pharmacokinetics of aldose reductase inhibitors: 3-fluoro-3-deoxy-D-glucose NMR studies in rat brains.
NMR Biomed
June 1989
Neurochemistry Research Laboratory, Veterans Administration Medical Center, Martinez, California 94553.
Direct quantification of the inhibitory effects of orally administered drugs (sorbinil, cyclandelate and sulindac) on aldose reductase activities in rat brains was performed non-invasively using the 3-fluoro-3-deoxy-D-glucose (3-FDG) 19F NMR spectroscopic technique. Quantitative data obtained directly from the target organ (brain) allowed for unprecedentedly accurate analysis of drug effects in the brain in vivo. Sorbinil, a potent aldose reductase inhibitor, exhibited a classic monophasic organ response, whereas cyclandelate and sulindac showed biphasic suppression patterns.
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