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G Zanolo

Publications and source records attributed to G Zanolo.

At least 37 records · Page 2Linked to original sources
PubMed1983

Pharmacokinetics of a slow-release preparation of ketoprofen lysine in man.

The lysine salt of 2-(3-benzoylphenyl)propionic acid (ketoprofen lysine) was administered at the dose of 160 mg either in two conventional capsules (Artrosilene) or in one slow-release capsule in a randomized sequence to 8 volunteers. Serum and urine concentrations of ketoprofen were determined by HPLC. The slow-release preparation had a bioavailability greater than 90% as compared with the conventional capsule and produced lower and longer lasting ketoprofen serum levels. These results suggest that two daily administrations of the new formulation should be suitable for therapeutic use.

Adult↗
PubMed1982

On the absorption, distribution and excretion of sorbinicate in the rat and the monkey.

Absorption, distribution and excretion of 14C-D-glucitol hexanicotinate (sorbinicate, SN) were studied after oral dosing in the rat against 14C-nicotinic acid (NA). SN is absorbed in large quantities from the gastro-intestinal tract, even if to a lesser extent than NA. The serum 14C-radioactivity after SN presents a distinctly different trend from that after NA administration: peak at 8 h (against 15 min for NA), slow excretion, very low and constant levels (peak 1/10 of that induced by NA). The superior performance of SN is explained partly by the different absorption of the two drugs and partly by a strong tropism for the tissues, especially for the liver, of which SN gave proof in the distribution tests. The excretion of 14C after SN in the urine is about half of that after NA whereas excretion in the feces is several times greater. Some results obtained in the monkey substantially confirm the findings in the rat.

Animals↗
PubMed1981

Serum and urinary levels of fentiazac after a single oral and epicutaneous administration in human subjects.

An acute pharmacokinetic investigation was carried out on 6 healthy subjects with 200 mg of epicutaneous 2-phenyl-4-p-chlorophenyl-thiazol-5-ylacetic acid (fentiazac) (5% cream) versus and equivalent dose of oral drug (coated tablets). The two pharmaceutical dosage forms were given to same subjects at a one-week interval according to a cross-over design. The gas chromatographic analysis of the blood and urinary samples allowed to demonstrate that fentiazac is absorbed through the skin. The bioavailability resulting from the epicutaneous administration is markedly lower than that provided by the oral administration. Actually, the coated tablet/cream ratio between the areas under mean serum concentration-time curves amounts to 30:1 approximately. The distribution into the systemic circulation is slow but constant and prolonged; the blood levels remain practically unchanged from 0.5-8 h when a peak begins to be observed; the urinary excretion increases in the course of time and reaches its maximum in the interval between the 12th and 24th h. Vice versa, the renal excretion proves higher in the first 6 h.

Acetates↗
PubMed1981

Pharmacokinetics of fentiazac in rats and monkeys.

Pharmacokinetic investigations were carried out on 2-phenyl-4-p-chlorophenyl-thiazol-5-ylacetic acid (fentiazac) in the rat and in the monkey. The drug, rapidly absorbed by the gastrointestinal system, shows a long maintenance in the body, with a long half-life in both animal species. The rate of biotransformation and the times of presence in the blood circulation of both unchanged drug and of its metabolites are indicated by the serum levels of cold fentiazac and labelled fentiazac. Urinary and fecal excretion attain levels amounting to 24 and 70%, respectively, of the dose administered.

Acetates↗
PubMed1981

Absorption, distribution and excretion of DL-gamma-amino-beta-hydroxybutyric acid-1-14C (GABOB-1-14C) in the rat.

1. Serum levels of DL-gamma-amino-beta-hydroxybutyric acid-1-14C (DL-GABOB-1-14C) in the rat (50 mg/kg) were quite similar after single i.v. and p.o. doses. Also the disappearance from the serum was similar with both administration routes. Within 6 days after p.o. treatment with the same single dose, about 26.5% and 1.6% of the dose were excreted in the urine and the faeces, respectively, and after i.v. administration excretion was 10.15% in urine and 1.75% in faeces. The results show that the compound is well absorbed and retained by the organism. After repeated oral doses (200 mg/kg three times daily for 4 days) the serum levels tended to become constant. 2. Urinary excretion after repeated administration increased progressively every day. Investigations on bile-cannulated rats showed that about 0.4% of the p.o. dose was excreted in 24 h. 3. After single (50 mg/kg) or multiple p.o. doses (200 mg/kg) of GABOB-1-14C, there was no unusual localisation of radioactivity in the organs the highest concentrations being present in the liver and the kidneys. Brain radioactivity was not related to serum levels or to administration route. Radioactivity concentration in other organs, for example the liver, was a function of serum levels. 4. Investigations performed to identify the radioactive products in the brain showed that the radioactivity was mainly ascribable to the unchanged DL-GABOB-1-14C.

Administration, Oral↗
PubMed1980

Metabolism of fentiazac.

The main metabolite of 2-phenyl-4-p-chlorophenylthiazol-5-ylacetic acid (fentiazac) is represented by a p-hydroxylated compound which is formed rapidly and that, still 72 later, can be detected in the general circulation. The p-hydroxylated metabolite is much less toxic than the original molecule from which it derives, being still active from an anti-inflammatory standpoint (its activity being equal to 70--75% of that of fentiazac). The metabolite, which possesses a therapeutic index much higher than that of fentiazac, represents quite an important step in the detoxication processes of the drug and enhances the therapeutic activity of the drug itself.

Acetates↗