Search results for "Canrenone"
showing 6 items of 6 documents
High-performance liquid chromatographic determination of spironolactone and its major metabolite canrenone in urine using ultraviolet detection and c…
1994
A rapid and simple column liquid chromatographic method involving a column-switching system for the determination of spironolactone and its main metabolite canrenone in urine is described. Purification and concentration was performed using an Hypersil ODS-C18, 30 microns (20 x 2.1 mm I.D.) pre-column. The most polar urinary compounds were removed by washing the pre-column with water, and the analytes were subsequently switched to a LiChrospher RP C18, 5 microns (125 x 4 mm I.D.) analytical column and separated by means of an acetonitrile-water mobile-phase. Under the proposed conditions, the extraction efficiency was approximately 100% over the 0.5-10.0 micrograms/ml concentration range. Th…
Nanosuspension Formulations for Low-Soluble Drugs: Pharmacokinetic Evaluation Using Spironolactone as Model Compound
2005
Various particle sizes of spironolactone as a model low solubility drug were formulated to yield micro-and nanosuspensions of the type solid lipid nanoparticles and DissoCubes. Seven oral and one i.v. formulations were tested in an in vivo pharmacokinetic study in rats with the aim of characterizing the bioavailability of spironolactone on the basis of its metabolites canrenone and 7-alpha-thiomethylspirolactone. In addition, a dose escalation study was carried out using nonmicronized spironolactone suspension as well as a nanosuspension type DissoCubes. On the basis of AUC as well as Cmax ratios, three groups of formulations were distinguished. The biggest improvement was seen with a solid…
The effects of canrenone on left ventricle diastolic function, left atrial compliance and on atrial natriuretic hormones in some subjects with “chall…
2010
STUDY PROPOSAL: Proposal to evaluate the response of left ventricular function of 30 patients with challenge hypertension to 50 or 100 mg of canrenone. Evaluation will be performed by repeated control of echocardiographic parameters, left atrial function and NT-proBNP. We also will use Tissue Doppler Imaging to identify and follow early left ventricular dysfunction. Careful monitoring of serum creatinine and electrolyte levels will be carried out. At the end of the study we will be able to identify the best dose of aldosterone we can recommend to control hypertension and left ventricular diastolic dysfunction. In possible successive evaluations other end points such as mortality, morbility,…
Zur Acetylierung von Spironolacton, Canrenon und 2-Methylencanrenon
1995
Bei der Umsetzung der Titelverbindungen mit Acetanhydrid und Acetylchlorid werden das 3,5-Dien-3-yl-acetat 2, die isomeren 2,4,6- und 3,5,7-Trien-3-yl-acetate 3 und 4 sowie das 2,4,6,8(14)-Tetraen-3-yl-acetat 7 erhalten. Hydrolyse von 7 liefert das 2α-Methl-8,14-didehydro-canrenon (9). 7 und 9 wurden auf ihre Bindungsfahigkeit gegenuber Hormon-Rezeptoren sowie den Serumproteinen SHBG und CBG gepruft: Die Substanzen erwiesen sich als inaktiv. Acetylation of Spironolactone, Canrenone, and 2-Methylene Canrenone Reaction of the title compounds with acetic anhydride and acetyl chloride yields the 3,5-dien-3-yl acetate 2 the isomeric 2,4,6- and 3,5,7-trien-3-yl acetates 3 and 4 as well as the 2,4…
Heterocyclisch anellierte Steroide aus 2-Hydroxymethylen-canrenon
1995
A-ring annulated heterocycles, the isoxazole 6, the pyrazoles 8 and the pyrimidines 9 are prepared starting from 2-hydroxymethylene canrenone 1. Binding studies were carried out with the compounds 1 and 6-8 using estrogen, progesterone, androgen, gluco- and mineralocorticoid receptors as well as the serum proteins SHBG and CBG: the substances were inactive on the receptor level. 1, 7 and 8a show weak binding affinity to CBG.
Darstellung und Reaktionen von 2-Methylen-canrenon
1995
Ausgehend vom Mannich-Salz 1 des Aldosteronantagonisten Canrenon oder von 2-Methylen-canrenon (2) wurden die am A-Ring anellierten Hetero- und Carbocyclen 5, 6, 8–13 dargestellt. Mit den Verbindungen 2, 3, 4b, 5, 6b, 8 und 12 wurden Bindungsstudien am Estradiol-, Progesteron-, Androgen-, Glucocorticoid- und Mineralocorticoid-Rezeptor sowie an den Serumproteinen Sexualhormonbindendes Globulin (SHBG) und Corticosteroidbindendes Globulin (CBG) durchgefuhrt. Die relativen Bindungsaffinitaten lagen bei CBG unter 1%, in allen anderen Fallen niedriger als 0.01%. Synthesis and Reactions of 2-Methylene-canrenone Starting from the Mannich salt 1 of the aldosterone antagonist canrenone or from 2-methy…