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Results for “ETHYL BISCOUMACETATE”

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At least 19 recordsLinked to original sources
PubMed1994

Pharmacokinetics of ethyl biscoumacetate and its metabolite 7-hydroxy ethyl biscoumacetate in healthy volunteers.

Disposition kinetics of ethyl biscoumacetate and its metabolite 7-hydroxy ethyl biscoumacetate were evaluated in ten healthy volunteers, after a single 300 mg oral dose of ethyl biscoumacetate. Serum concentrations of parent compound and its metabolite were measured by HPLC. The maximum serum ethyl biscoumacetate concentrations were reached 1.0-4.0 hours after drug dosing. From 3 hours after drug administration the concentration of the metabolite was always higher than the concentration of the parent compound. Geometric mean of elimination half-life was 0.66 hours for ethyl biscoumacetate and 2.03 hours for the 7-hydroxy ethyl metabolite.

Administration, Oral↗
PubMedDate not supplied

[Effect of dimethicone on pharmacokinetics and pharmacodynamics of ethyl biscoumacetate].

The influence of dimeticone (Gel de Polysilane Midy) on the pharmacokinetics and pharmacodynamics of oral ethyl biscoumacetate was studied in 6 healthy volunteers in a randomised single dose, two-way cross-over study. Each volunteer received at one week interval a single dose (300 mg) of ethyl biscoumacetate, either alone or with dimeticone. Ethyl biscoumacetate levels were measured in plasma for 24 hours. Pharmacodynamic parameters were measured for 96 hours. Ethyl biscoumacetate peak concentration was significantly higher when administered with dimeticone (40.3 +/- 25.3 mg/l vs 31.0 +/- 25.7 mg/l; p = 0.031), without significant change in the area under curve. Other pharmacokinetic and pharmacodynamic parameters did not differ significantly. The slight increase of the ethyl biscoumacetate bioavailability with dimeticone in repeated dosing might have pharmacodynamic consequence; a clinical trial should address this question.

Adult↗
PubMed1992

Determination of ethyl biscoumacetate and its metabolite 7-hydroxyethyl biscoumacetate in human serum by high-performance liquid chromatography and mass spectrometry.

An efficient reversed-phase high-performance liquid chromatographic method has been developed for the determination of ethyl biscoumacetate (EBA) and its metabolite in human serum, using the mu Bondapak C18 column and methanol-water-phosphoric acid (56:46.8:0.2, v/v/v) as the mobile phase. This method permitted the determination of both EBA and a metabolite in human serum. The latter has been mentioned by other authors only in urine samples, where significant concentrations were found. Identification of the metabolite as 7-hydroxyethyl biscoumacetate was based on its chromatographic separation, followed by isolation from the eluate and direct mass spectrometric identification. It has been found that the higher EBA concentrations in human serum described by Brodie et al. [J. Pharmacol. Exp. Ther., 106 (1952) 453] were caused by the insufficient resolving power of the spectrophotometric method used, leading to overlapping of the UV spectra of the parent drug and its metabolite.

Chromatography, High Pressure Liquid↗
PubMed1977

The effects of menadione, ethyl biscoumacetate, and sodium salicylate on the metabolism of mucopolysaccharides in the aortic wall and liver of rats.

In rats with hyper- and hypovitaminosis the contents were determined of acid mucopolysaccharides (MPS) on the basis of contents of hexuronic acids; the total contents of biopolymers containing hexosamines (acid MPS, glycoproteins), on the basis of contents of hexosamines in the aortic wall and in the liver; and the activity of glutamine-fructose-6-phosphate aminotransferase (GPAT; EC 2.6.1.16) in the liver. Menadione-induced K hypervitaminosis was accompanied by moderate elevations of indicators of MPS metabolism. Protracted administration of ethyl biscoumacetate or sodium salicylate lowered the contents of acid MPS and of biopolymers containing hexosamines in the aortic wall and in the liver. Simultaneously, the GPAT activity in the liver markedly decreased.

Animals↗