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Biomedical subjects

G Coppi

Publications and source records attributed to G Coppi.

At least 73 records · Page 4Linked to original sources

Mutagenicity studies on dihydroergocristine.

Dihydroergocristine (DHEC) is an ergot derivative used for the therapy of patients with cerebrovascular insufficiency. It was tested for mutagenicity by means of four tests. In the mutagenicity in vitro assay on Salmonella typhimurium, DHEC was checked at 10,000 micrograms/plate on TA98 and TA1538 strains and at 3000 micrograms/plate on TA1535, TA1537 and TA100 strains with and without metabolic activation. In a quantitative in vitro test for mutagenicity in V79 Chinese hamster cells, DHEC was studied at concentrations between 30 and 0.3 microgram/ml with and without metabolic activation. DHEC was tested for its ability to induce chromosomal damage in human lymphocyte cultures utilizing the concentrations of 10, 3 and 1 microgram/ml. In the in vivo mouse (Swiss strain) micronucleus assay, DHEC was orally administered at two dosages (50% and 16% of LD50) following the schedule of the test. Dihydroergocristine is a drug free of mutagenic activity on the basis of all the results obtained from the above in vitro and in vivo tests.

Animals↗

[Pharmacological and clinical profile of tiaprofenic acid].

Tiaprofenic acid is a new generation anti-inflammatory drug synthesized to be a valid alternative to both cortisone preparations and other NSADs since it is less toxic yet equally effective. Its anti-inflammatory, analgesic, antipyretic activity is due to a particular interference mechanism active in the early phases of the inflammatory process (PG synthesis inhibition, stabilization of lysosomal membranes). Thanks to its good trophism toward tissues in the otolaryngological area and its tolerability this drug would appear particularly suited for the treatment of inflammatory E.N.T. pathologies.

Animals↗

Effect of montmorillonite on drug release from polymeric matrices.

Drug release from matrices of polyvinyl alcohol was affected by molecular weight and solubility of the drugs (either sodium salicylate or papaverine hydrochloride), and by the matrix loading. - Montmorillonite addition to the matrix formulation modified only the release constant of papaverine hydrochloride owing to drug interaction with the clay by an ionic exchange process. The kinetics exponent was affected a little bit by interaction of the drug with montmorillonite, whereas the influence of the matrix loading was more remarkable.

Bentonite↗

Distribution of drugs in polymers loaded by swelling.

Ethylene:vinyl acetate pellets were loaded at 20 degrees C by swelling the polymer with 1 and 3% (w/v) chloroformic solutions of tolbutamide. The energy dispersive X-ray analysis showed different concentrations of the tolbutamide sulfur in the pellets sections according to the loading time. At the beginning of the loading process, the sulfur in the pellets showed two concentration peaks which later joined in the center of the section before reaching a homogeneous distribution. The concentration peaks might depend on a drug sieving process as the solution flow reaches a less swollen inner area. Therefore, the concentration distribution of the drug would be affected by the size of the polymer network, which is related to the volume of the solvent in the polymer. Another possible explanation of these concentration profiles is that they could be a result of the solvent evaporation process. The concentration distribution of the drug becomes homogeneous only after the complete swelling of all of the polymer.

Chemistry, Pharmaceutical↗

HPLC determination of tetroxoprim and sulphadiazine in pharmaceutical dosage forms and in biological fluids.

Two HPLC methods for determination of tetroxoprim and sulphadiazine in pharmaceutical dosage forms and in biological fluid are reported. Both methods show good linearity, precision, accuracy and reproducibility. The serum levels and urinary excretion of tetroxoprim and sulphadiazine in man, after oral administration of two different syrup formulations, are reported. Tetroxoprim embonate, an insoluble salt very useful for obtaining a suspension with good palatability, shows a bioavailability not statistically different from that of tetroxoprim base. Sulphadiazine shows the same bioavailability in the two syrups.

Anti-Infective Agents↗

[3-substituted 1,2-benzisoxazole and their neuroleptic activity].

The authors report the synthesis of two new derivatives of 3-substituted 1,2-benzisoxazole. The new molecules (P-1368, P-1370), evaluated in many pharmacological C.N.S. tests, show interesting neuroleptic activity but inferior to those of haloperidol and chlorpromazine.

Animals↗

New isosorbide 5-mononitrate derivative with hypotensive activity.

Synthesis and pharmacological properties of the 5-fluoro-nicotinic ester with isosorbide-5-mononitrate 3 are reported. The new compound shows an in vitro activity on rabbit aortic helical strips five times higher than isosorbide-5-mononitrate. The hypotensive activity in guinea-pigs of 3 is markedly superior to that of 5-ISMN. In the rat 3 shows a bioavailability and an acute toxicity inferior to those of 5-ISMN after oral administration.

Animals↗

Synthesis and hypolipidemic activity of some new esters of glycerol and 2-O-methyl-glycerol with nicotinic and 5-fluoro-nicotinic acids.

A series of new esters of glycerol and 2-O-methyl-glycerol with nicotinic and 5-fluoro-nicotinic acids were synthesized and their hypolipidemic activities were comparatively tested. The two most interesting compounds, 5 and 12, show a higher activity than both nicotinic and 5-fluoro-nicotinic acids in the following experimental models: Triton and olive oil hyperdyslipemia and tests on old rats.

Animals↗

A method for studying expectorant action in the mouse by measurement of tracheobronchial phenol red secretion.

The paper reports a method for studying mucosecretolytic drugs in the mouse. After i.p. application of phenol red, part of the dye is secreted in the tracheobronchial tract and collected by lung washings with saline. The concentration of secreted phenol red is measured photometrically at 546 nm. All the most important expectorant drugs increase the tracheobronchial secretion of phenol red in the mouse. The ED50 values, calculated as mg/kg, show practically the same activity for N-acetylcysteine, Tiopronine, SF-1284 and S-carboxymethylcysteine, and a lower activity for Ambroxol and Sobrerol. The method was validated for reproducibility utilizing Tiopronine in many experiments performed over twelve months.

Animals↗