The bioavailability (BA) of phenylbutazone and clofezone preparations had been determined in patients suffering from rheumatic diseases. Clofezone is a compound preparation of phenylbutazone and clofexamide, with which the phenylbutazone portion amounts to 49%. In spite of an equivalent dosage (0.4 g phenylbutazone or 0.8 g clofezone, resp.) significant differences in the phenylbutazone-serum level profile had partly been stated after the application of different kinds of the preparation of both the drugs. The oral administrations (phenylbutazone dragées, Perclusone capsules) resulted in a prompt resorption; the plateau values of the phenylbutazone concentration in serum had already been completed after 2-3 h. The resorption from suppositories was decreased. The serum level maximum with phenylbutazone suppositories occurred after 6 h, with Perclusone suppositories after 24 h only. Compared to the phenylbutazone i.v. injection, the phenylbutazone dragées proved a complete substance uptake into the systemic circulation, whereas a relative BA of 65% has been determined for Perclusone capsules. The BA of the phenylbutazone suppositories amounted to 67%, those of the Perclusone suppositories to 41%.

01 Jan 1982·YAKUGAKU ZASSHIQ4 · MEDICINE

Determination of Clofexamide and Its Metabolites in Plasma by Gas Chromatography

Q4 · MEDICINE

Article

Author: Tanaka, Makoto ; Shimizu, Hiroaki ; Saito, Morihiro ; Kigasawa, Kazuo

A specific and sensitive gas chromatog. method was developed for the simultaneous determination of clofexamide (I) [1223-36-5] and its two N-dealkylated metabolites in plasma.The method involves a solvent extraction, trifluoroacetylation, and anal. by gas chromatog. on a 5% OV-17 column with flame thermionic detection.The N-(2-methylaminopropyl) analog of clofexamide was used as an internal standardThe plasma concentration of each substance can be measured at the levels down to 4 ng/mL.The method was applied to determine the plasma levels of intact clofexamide and the metabolites after i.v. and oral administration to rabbits.

01 Jan 1972·Chemical and Pharmaceutical Bulletin

Studies on Absorption, Biotransformation and Excretion of Drug.(1). Metabolites of Clofexamide in Rat

Article

Author: IRINO, OSAMU ; FUKAWA, KAZUNAGA ; TATEISHI, MITSURU

Following administration of clofexamide (I) [1223-36-5] to rats, 12 metabolites were identified in the feces and urine and a metabolic pathway for I was proposed.

100 Deals associated with Clofexamide

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