[Fluorometric determination of plasma niflumic acid by direct estimation of thin layer chromatograms].
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Biomedical subjects
Publications and source records attributed to H E Geissler.
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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.
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.
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.
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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%.
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.
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.
Different methods of in situ determination of drugs on TLC-plates are described and discussed. Suitable examples are given demonstrating the value for pharmacokinetics.
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%.
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.
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For the purpose of investigating drug interactions, a new selective method for determination of 5-dimethylamino-9-methyl-2-propyl-1H-pyrazolo[1,2-a] [1,2,4]benzotriazine-1,3(2H)-dione-dihydrate (azapropazone, Prolixan 300) was developed. The method is based upon the direct quantitation of the drug by thin-layer chromatography using remission measurement. The method is well suited for routine analysis of numerous samples, because of its simplicity and rapidity. The standar deviation of the method is about +/-4% at therapeutic plasma concentrations.