An interaction study between benoxaprofen and digoxin.

The influence of maintenance therapy with benoxaprofen, 600 mg daily, on digoxin steady-state plasma levels was studied in 12 patients with rheumatic disease. No difference could be shown during concomitant therapy or after withdrawal of benoxaprofen (p greater than 0.10 and p greater than 0.90, respectively). Toxic concentrations were not observed. There were no changes in renal function values.

[Comparison of bumadizone-, phenylbutazone- and oxyphenbutazone-plasma levels after a single oral dose of phenylbutazone and of bumadizone, respectively (author's transl)]. / Vergleichende Untersuchung der Bumadizon-, Phenylbutazon- und Oxyphenbutazon-Plasmaspiegel nach einmaliger Gabe von Phenylbutazon und von Bumadizon.

Bumadizone-calcium-semihydrate and phenylbutazone were given orally to two groups (I and II) consisting of 6 persons each; plasma levels of bumadizone, phenylbutazone and oxyphenbutazone were determined over a period of 384 h. For bumadizone a plasma half-life of 6.9 h was found, maximum plasma levels were reached after 1-6 h varying from 27 to 46 microgram/ml. Phenylbutazone- and oxyphenbutazone-AUC-values were compared between the two groups.

Plasma and urinary levels of triamterene and certain metabolites after oral administration to man.

The plasma and urinary levels of triamterene and two metabolites were measured using a specific method of analysis. Urinary excretion was completed after 48 h, which permitted a rough estimate of its half-life as longer than two hours. The areas under the curve were 672.5 +/- 160.3 and 1.311.3 +/- 399.1 micrograms/ml X h after the triamterene 150 mg and 300 mg p.o., respectively and correspondingly 4.2 +/- 1.4% and 3.7 +/- 0.6% of the dose were excreted as unchanged drug. The principal metabolite of triamterene found was the sulfate conjugate. The area under the curve of this metabolite amounted to 6.672 +/- 2.120 and 11.941 +/- 5.005 micrograms/ml X h after the of 150 mg and 300 mg triamterene doses, respectively. The urinary excretion of the metabolite varied between 25.0 +/- 4.0% and 17.5 +/- 3.5% of the dose after either dose. In healthy subjects an effect on sodium excretion was observed after a dose of 150 mg, whereas the potassium-retaining effect was observed only after the dose of 300 mg.

Pharmacokinetics of a fixed combination with propranolol, hydrochlorothiazide and triamterene.

The blood levels of propranolol, hydrochlorothiazide and triamterene, three components of a new antihypertensive combination, Dociteren, were studied in patients with mild hypertension after single dosage. The blood levels of propranolol in the combination did not differ from the blood levels obtained after a single dose of propranolol given alone.

[Determination and comparison of the plasma and urine concentrations in men given tranylcypromine stereoisomers]. / Bestimmung und Vergleich der Plasma- und Urinkonzentrationen nach Gabe von (+)- und (-)-Tranylcypromin.

The (+) and (-)isomers of DL-trans-2-phenylcyclopropylamine (tranylcypromine, Parnate, Jatrosom) were tested under cross-over conditions on 10 volunteers. (-)Tranylcypromine entered blood circulation more rapidly, reached significantly higher concentrations and was metabolized more slowly than (+)tranylcypromine. These results indicate a difference in the pharmacokinetics of the tranylcypromine isomers. In the urine collected over a period of 24 h the excretion of unmetabolized (4)tranylcypromine was lower probably resulting from the greater metabolization rate of this isomer. There is a conformity between the findings in plasma and urine.

[Fluorimetric determination of tranylcypromine in plasma as its 1-dimethylamino-naphthaline-5-sulfonic acid chloride by direct measurement of TLC-plates (author's transl)]. / Fluorimetrische Bestimmung von Tranylcypromin in plasma als 1-Dimethylamino-naphthalin-5-sulfonsäure-Derivat durch direkte quantitative Dünnschichtchromatographie.

A fluorimetric method for analysis of tranylcypromine from plasma is described. After extraction from plasma tranylcypromine reacts with 1-dimethylamino-naphthaline-5-sulfonic acid chloride (DANS-Cl) in order to form the highly fluorescent DANS-tranylcypromine. After chromatographic separation on silicagel plates quantitation is achieved by in situ fluorescence determination. The recovery of tranylcypromine from plasma is 64% with a coefficient of variance of about +/- 6%.

[Pharmacokinetics of triamterene and its active metabolites in renal insufficiency (author's transl)]. / Zur Pharmakokinetik zon Triamteren und seinen wirksamen Metaboliten bei eingeschränkter Nierenfunktion.

1. After one oral dose of 100 mg triamterene plasma levels of triamterene (TA) and its metabolites hydroxytriamterene (OH-TA) and hydroxytriamterene sulfuric acid ester (OH-TA-ester) were studied in patients with normal and impaired renal function and in patients submitted to hemodialysis. Triamterene and its metabolites were also determined in the urine and the dialysate, respectively. 2. Hydroxytriamterene sulfuric acid ester (OH-TA-ester) representing a phase-II-metabolite of triamterene was found to yield plasma concentrations which were always higher than those of native TA. 3. In decreased renal function the elimination half-lives (t 1/2) of TA and OH-TA-ester were increased yielding elevated plasma levels of TA and its metabolites. The data of t 1/2 for TA and OH-TA-ester correlated with the creatinine clearance in an almost hyperbolic fashion. 4. Dialysance values of about 2 to 4 ml/min were determined for TA and OH-TA-ester.

[Determination of azapropazone and 8-hydroxyazapropazone in urine by direct quantitative thin-layer chromatography (author's transl)]. / Die Bestimmung von Azapropazon und 8-Hydroxyazapropazon im Harn durch direkte quantitative Dünnschichtchromatographie.

A method for quantitative determination of 5-dimethyl amino-9-methyl-2-propyl-1H-pyrazolo[1,2-a] [1,2,4]benzotriazine-1,3-(2H)-dione (azapropazone) and 8-hydroxyazapropazone in urine has been described. The analysis is performed by quantitatively thin-layer chromatography. The method is selective with a standard deviation of about 5%. After daily oral administration of 3 x 300 mg azapropazone-dihydrate a mean excretion of azapropazone of 62% and a mean excretion of 8-hydroxyazapropazone of 14% was determined.

[Quantitative thin-layer chromatography and its use in clinical pharmacology (author's transl)]. / Quantitative Dünnschichtchromatographie und ihr Einsatz in der klinischen Pharmakologie.

Different methods of in situ determination of drugs on TLC-plates are described and discussed. Suitable examples are given demonstrating the value for pharmacokinetics.

[Fluorometric determination of hydrochlorothiazide in body fluids by direct measurement of thin-layer chromatographic plates (author's transl)]. / Fluorimetrische Bestimmung von Hydrochlorothiazid in Körperfluüssigkeiten durch direkte Auswertung von Dunnschichtchromatogrammen.

Two fluorometric methods for analysis of hydrochlorothiazide (HCT) are described utilizing direct measurement of thin-layer plates. The first method employs a modification of the Bratton-Marshall reaction and is therefore applicable to all aromatic primary amines. Following diazotation and azocoupling of the HCT hydrolysis product, a fluorescent group is added to the compound. For this purpose N-(1-naphthyl)ethylenediamine is first coupled with 4-chloro-7-nitrobenzo-2,1,3-oxadiazole. In the second method, the intrinsic fluorescence of underivatized HCT, following its extraction from plasma, urine or saliva, is used. It is shown that the sensitivity of this method is sufficient for estimating the kinetics following oral administration of 25 mg HCT.

[Fluorometric determination of propranolol and its metabolite n-desisopropylpropranolol in plasma and urine by direct meausrement of thin-layer chromatographic plates (author's transl]. / Fluorimetrische Bestimmung von Propranolol und seines Metaboliten N-Desisopropylpropranolol in Plasma und Urin durch direkte Auswertung von Dünnschichtchromatogrammen.

The quantitative analysis of propranolol and its metabolite N-desisopropylpropranolol in plasma and urine is described. The drugs are extracted into 2-pentanol-heptane, and the solvent is concentrated. The whole residue is chromatographed on silica gel plates. The compounds are determined directly on the thin-layer plates without derivatization. The recovery of propranolol from plasma is 70%, with a standard deviation of +/- 4%.