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Biomedical subjects

E Moro

Publications and source records attributed to E Moro.

At least 127 records · Page 7Linked to original sources
PubMed1981

Bioavailability and pharmacokinetics in man of acipimox, a new antilipolytic and hypolipemic agent.

Two separate studies were performed: in the first study for healthy male volunteers received three single oral doses (150, 250 and 400 mg) of 5-methylpyrazine carboxylic acid 4-oxide (acipimox) according to a randomized sequence. Plasma levels of the drug were determined by RIA and urinary excretion by HPLC. In the second trial the effect of food on the drug bioavailability and pharmacokinetics during repeated administration was investigated in six volunteers. The RIA method was adopted to measure plasma and urine levels. Acipimox was rapidly and almost completely absorbed after the three single doses. About 90% of the administered dose was recovered as unchanges drug in urine collected up to 24 h. Peak plasma levels, area under plasma levels curves and urinary excretion were linearly related to the administered dose. The presence of food in the gastro-intestinal tract did not adversely affect the bioavailability of the drug. No significant changes were noted in the rate of elimination after 6 days of treatment with 250 mg t.i.d. Plasma levels determined after the 19th dose were in good agreement with those predicted on the assumption of linear pharmacokinetics and a one-compartment open model, with a half-life of about 2 h.

Administration, Oral↗
PubMed1980

Plasma and synovial fluid pharmacokinetics and prostaglandin inhibitory effect of indoprofen in patients with rheumatoid arthritis.

Indoprofen was given intravenously (bolus followed by infusion) and orally to 7 patients suffering from active rheumatoid arthritis with knee joint effusion. Indoprofen readily penetrated into synovial fluid in amounts which were directly correlated with areas under curves of plasma drug levels. Synovial fluid acted as a compartment distinct from the central (plasma) compartment. Indoprofen caused a substantial decrease in E2 and F2 alpha prostaglandin concentration in synovial fluid.

Adult↗
PubMed1980

[Emergency surgical treatment in complications of Crohn disease].

The Authors refer to four cases of complications in patients suffering from Crohn's disease. Three patients were already subjected to surgery for the same illness. The Authors value the opportunity of an urgency surgery on the complications of this disease.

Adult↗
PubMed1980

Pharmacokinetics and metabolism of indoprofen in the hamster.

2-[p-(1-Oxo-2-isoindolinyl)phenyl]propionic acid (indoprofen) is rapidly absorbed after oral administration (2 mg/kg) to male and female hamsters. Peak plasma levels of about 12-13 microgram/ml are reached within 1 h of dosing. Plasma concentrations in males and females are similar until 4 h but different at subsequent observation times. The half-life of indoprofen in plasma is approximately 7 h for males and 16 h for females. In experiments with 14C-labelled compound, radioactivity is mainly excreted in the urine: 94% of the dose in 6 days for males and 73% in 5 days for females. The females also excrete a significant amount of the drug (22%) in the faeces, probably via the bile. Residual radioactivity in female carcasses on the 5th day represents 1% of the dose. The main excretory product is the unchanged drug as such (about 35% and 21%, respectively, in 0-24 hour urine for males and females) and as glucuronic acid conjugate (29% and 12%). Small amounts of 5- and 6-hydroxy-isoindolinyl derivatives, and of two metabolites whose structures have not been identified, are also found in the urine of the animals of both sexes.

Animals↗
PubMed1979

Pharmacokinetic, bioavailability and pharmacodynamic study of indobufen (K 3920), an inhibitor of platelet aggregation, after a single dose in man.

Six healthy volunteers received single iv and oral doses of 2-[p-(1-oxo-2-isoindolinyl)phenyl] butyric acid 100 mg (indobufen; K 3920), an inhibitor of platelet aggregation. Plasma levels and urinary excretion of the drug were determined by GLC. Collagen-induced platelet aggregation was assessed turbidimetrically at various intervals after administration. The plasma half-life of the drug was 7--8 h and more than 70% of the administered dose was recovered within 48 h in urine, as unchanged drug and as the glucuronide of indobufen. After oral administration of tablets of two different formulations, the drug was completely absorbed, but one formulation showed faster absorption. The maximal inhibitory effect on platelet aggregation was observed 1 to 4 h after iv administration, and it had decreased by 8h. After tablets, peak effect and the time of the peak were similar, but activity was significantly prolonged, in accordance with the higher plasma levels found at 8 h. The data suggest that the effect of indobufen on platelets is reversible, and that for this drug platelets behave as a compartment that slowly equilibrates with plasma.

Administration, Oral↗
PubMed1979

Indobufen (K 3920), a new inhibitor of platelet aggregation: effect of food on bioavailability, pharmacokinetic and pharmacodynamic study during repeated oral administration to man.

The effect of food on bioavailability of indobufen tablets was investigated in 6 healthy volunteers. Subsequently, the same subjects took 100 mg b.i.d. for 7 days. Plasma levels and urinary excretion of indobufen were determined by GLC. Platelet aggregation induced by several concentrations of adrenaline was determined turbidimetrically at various times after the first and last doses. The absorption of indobufen tablets was not substantially impaired by the presence of food in the GI tract, although peak plasma levels and AUCs were slightly reduced after food. Pharmacokinetic analysis of plasma and urinary levels of indobufen did not indicate any change in drug disposition after repeated dosing. Adrenaline-induced platelet aggregation was markedly inhibited for up to 12 h after the first dose and the intensity and duration of this effect did not change after repeated administration. A twice-daily dosing appears suitable for clinical trials.

Adult↗
PubMed1977

Na+ dependence of phenacetin absorption.

Phenacetin in solution at different concentrations of Na+ was orally administered to dogs. Phenacetin absorption is increased by the Na+: a positive correlation was noted between the Na+ concentration in the medium and the plasma levels of phenacetin. Ouabain antagonizes the effect of Na+ on phenacetin absorption.

Administration, Oral↗
PubMed1977

Effect of food on absorption of indoprofen administered orally to man in two dosage forms.

The influence of food on the bioavailability of two oral dosage forms (100-mg capsules and 200-mg tablets) of indoprofen, a new propionic acid derivative with marked anti-inflammatory and analgesic properties, has been investigated. Plasma levels and urinary excretion of indoprofen were determined both in the fasting state and after a standard meal in healthy volunteers after administration of two 100-mg capsules (4 subjects) and of one 200-mg tablet (6 subjects). Indoprofen in biological fluids was determined by gas-liquid chromatography. The extent of absorption from tablets was not affected by food as indicated from the values of the total area under plasma level curves and urinary excretion of the drug. The rate of absorption was faster after meal than in the fasting state. The opposite was found for capsules, which showed a slightly delayed absorption after food. The results suggest that food may differently influence the absorption pattern of different pharmaceutical forms of the same drug.

Administration, Oral↗
PubMed1977

Pharmacokinetic studies of indoprofen in healthy volunteers and in patients.

The pharmacokinetics of indoprofen in healthy subjects after single oral and i.v. administrations is reviewed. During repeated administration of indoprofen to 6 normal subjects (200-mg tablet every 8 hours for 6 days) no variations in the disposition of the drug were found in comparison with single dose administration. In 6 inpatients, with rheumatoid arthritis, the pharmacokinetics of indoprofen was studied after single oral (tablet) and i.m. administration. As for oral doses, no difference in main kinetic parameters was detected between the patients and normal subjects except for a higher volume of distribution in the former population. The bioavailability of the drug given by i.m. injection was not significantly different from that observed after oral administration.

Administration, Oral↗