Showing papers by "Novartis published in 1975"

Comparison of fixed interval and visual analogue scales for rating chronic pain

Abstract: A visual analogue scale (VAS) and a 4-point scale (FPS) have been compared in patients suffering from prolonged constant pain due to chronic inflammatory or degenerative arthropathy. Each patient was treated with a constant low or high dose of paracetamol or dihydrocodeine throughout a four week period. The VAS was accurate, as reliable and more sensitive than the FPS in registering the intensity of chronic pain. Separate records of each estimate, sealed immediately on completion by the patient, resulted in omission of significantly more pain recordings on the FPS, whereas retention by the patients of their previous records did not systematically influence subsequent judgments. In this study, the VAS appeared to be more satisfactory than the FPS for patient self-rating of pain intensity.

Aqueous wetting and film forming compositions

Abstract: The disclosure relates to aqueous compositions which comprise water soluble fluorinated surfactant, fluorinated synergist, ionic non-fluorochemical surfactant, nonionic non-fluorochemical surfactant, electrolyte, and solvent. This composition is a concentrate which when diluted with water spreads on fuel surfaces suppressing vaporization. Because of this property the aqueous solutions of the above compositions are effective as agents for fire fighting.

Light protection agents

Abstract: New 2-(2'-hydroxyphenyl)-benzotriazoles are used for protecting light-sensitive organic materials. They are prepared by diazotization of a 2-nitroaniline, coupling of the resulting diazo compound with a phenol and reduction of the resulting 2-nitroazo compound.

«Template»‐Reaktionen I. Herstellung von tricyclischen und tetracyclischen Metallkomplexen aus aromatischen 1,2‐Diaminen und 1,3‐Dicarbonylverbindungen

Abstract: The condensation of 1,2-phenylenediamine 1 and 1,3-dicarbonyl compounds 2 in the presence of a divalent metal ion such as Ni2+, Cu2+, Co2+, yields the tricyclic 4 or tetracyclic complexes 5. The yields of these one step template reactions is very high in a large number of examples with differently substituted diamines 1 and 1,3-dicarbonyls 2.

Lipopolysaccharide induces C-type virus in short term cultures of BALB/c spleen cells.

Abstract: IN certain strains of mice, such as AKR, C-type viruses occur throughout life and can readily be detected by infectivity assays1,2. In other seemingly virus-free strains, C-type viruses can be activated in vivo by X irradiation3,4, chemical carcinogens5, graft-versus-host reactions6 and in vitro by long term cultivation7, by X rays8, halogenated pyrimidine analogues9,10 and mixed lymphocyte reactions6. We report here that lipopolysaccharide, a B-cell mitogen18, induces C-type virus in short term cultures of BALB/c spleen cells.

Pharmacokinetic Data of Carbamazepine and Its Major Metabolites in Man

Abstract: Carbamazepine which is the active substance of the anti-epileptic drug Tegretol® has the chemical structure of 5-carbamyl-5H-dibenzo[b, f]azepine. Recently several papers relating to the biotransformation of the drug have been published but our present knowledge still appears insufficient.

Process for the purification of industrial effluents

Abstract: A novel process for purifying industrial effluents which comprises bringing said effluents into contact with cellulosic absorbent which has been pretreated with precipitants.

Manufacture of tabular habit silver halide crystals for photographic emulsions

Abstract: A process for the manufacture of photographic silver halide emulsions wherein the silver halide crystals are of tabular habit bounded by (100) cubic faces and which have an aspect ratio of from 1.5:1 to 7:1 is provided. The size of the crystals is from 0.2μ to 3.0μ in edge length, and they are obtained by adding an aqueous solution of a water-soluble halide and an aqueous solution of silver nitrate to an aqueous colloid medium by a double jetting technique at a controlled pAg value of between 4.0 and 8.0 and at a controlled constant temperature within the range of 35° to 75° C to produce monodispersed untwinned seed crystals. The seed crystals are then increased in size by Ostwald ripening in the presence of sufficient ammonia and alkali halide to favor the cubic habit of the crystals at a temperature of between 30° to 70° C. The photographic silver halide emulsion exhibit a high contrast on exposure and development.

Plant growth regulating agent

Abstract: 2-chloro-2',6'-dimethyl-N-(1-methoxyprop-2-yl)-acetanilide is disclosed as plant growth regulating and herbicidal agent with improved stability in the soil.

Biotransformation and pharmacokinetics of sulfinpyrazone (Anturan) in man.

Abstract: The absorption, biotransformation and elimination of sulfinpyrazone, 1,2-diphenyl-3,5-dioxo-4-(2′-phenylsufinylethyl)-pyrazolidine, have been studied by administration of single 200 mg oral doses of a14C-labelled preparation to two male volunteers. Absorption from the gastro-intestinal tract was rapid and complete and the plasma concentration of unchanged drug reached maximum values of 22.67 and 13.04 µg/ml, respectively, after 1 – 2 hours. The elimination half-life in the two subjects, calculated from the decline between 3 and 8 hours, was 2.7 and 2.2 hours. The integrated concentration of unchanged sulfinpyrazone in plasma, estimated from the area under the concentration curves (AUC), was almost as high as that of total14C-substances, so the proportion of metabolized drug in plasma was low. In no case did the AUC of the three specifically determined metabolites, i.e. the sulphone G 31 442, the “para-hydroxy”-compound G 32 642 and the “4-hydroxy”-compound GP 52 097, exceed 4% of the sulfinpyrazone value. More than 95% of whole blood radioactivity was confined to plasma. The oral dose was rapidly and completely excreted, since within 4 days more than 95% was recovered, 85% from urine and 10% from faeces. A large proportion of the dose was excreted as unchanged drug in the two volunteers: 51 and 54% of total urinary radioactivity was present as sulfinpyrazone; 8.2 and 8.8% was present as “para-hydroxy”-metabolite, 2.7 and 3.0% as sulphone-metabolite, and 0.6 and 0.8% as “4-hydroxy”-metabolite. About 30% of urinary radioactivity consisted of highly polar metabolites. Spectroscopy of them showed that they were the C-β-glucuronides of sulfinpyrazone (28%) and the corresponding sulfone (2%). In these metabolites the C(4) of the pyrazolidine ring was directly attached to glucuronic acid, and thus they represent a new type of biosynthetic conjugate.

Single dose air pressure operated dispenser

Abstract: An air pressure-operated dispenser for spraying a single dose of a fluent material of liquid or powder form. The dispenser has a single dose container having a compressed air inlet opening and a closable discharge orifice and means for closing the discharge orifice in a non-dispensing position of the dispenser. An air-compressing piston pump having a compressed air outlet from a compression space thereof is provided on the dispenser at the junction of the inlet opening and the compressed air outlet. The inlet opening of the single dose container is joined to the compressed air outlet of the compression space and valve means is provided on the piston pump for releasing a flow of compressed air after build up of a determined excess pressure.

Process for coating inorganic substrates with carbides, nitrides and/or carbonitrides

Abstract: A process for coating inorganic substrates, especially metallic or metalloid substrates, sintered metal carbides and carbon materials with carbides, nitrides and/or carbonitrides, using certain nitriles as sources of carbon and nitrogen, is described. High deposition rates and smooth coatings of good to very good adhesion are achievable by this process.

Inhibition of prostaglandin synthetase by psychotropic drugs.

Abstract: Psychopharmaka mit neuroleptischer, antidepressiver und/oder tranquillisierender Wirkung, die eine trizyklische Struktur besitzen, hemmen in vitro dosisabhangig die Prostaglandin-Synthetase, welche aus Ochsensamenblase isoliert wurde. Hingegen weist das Neuroleptikum Haloperidol, das sich strukturell von den anderen untersuchten Praparaten wesentlich unterscheidet, kaum einen solchen Effekt auf. Die pharmakologische Bedeutung dieser Befunde wird diskutiert.

Transfer printing process for hydrophilic fibrous material or blends of hydrophilic and synthetic fibrous material, with reactive disperse dyes

Abstract: A transfer printing process for dyeing or optically brightening hydrophilic fibrous material and blends of hydrophilic and synthetic fibrous material with sublimable reactive disperse dyes or fluorescent brighteners, which process comprises the use of inert carriers that are treated with at least one reactive disperse dye or fluorescent brightener, which, during the heat treatment of the transfer printing process, has a vapor pressure higher than 10 -5 Torr at temperatures above 160° C., and treating the material to be printed with at least two compounds, one of which has a boiling point higher than 120° C. and a solubility or dispersibility in water of at least 25 g/l at 25° C., direct or with the aid of an auxiliary solvent or dispersant, and under the transfer conditions of the dyes or fluorescent brighteners is sparingly volatile, and the other is an acid acceptor, or with at least one compound that combines both functions simultaneously.

Selektive Abspaltung säurelabiler Aminoschutzgruppen von Peptiden in Trifluoräthanol

Abstract: In building up large polypeptides, it has become the established practice to use acide-labile protecting groups of the t-butyl type. Up to now, only one step of selectivity under acidic conditions has been used, consisting in the cleavage of Trt, Bpoc or Ppoc from N(α) without attacking the t-butyl protecting groups. We have found that the use of 90% trifluoroethanol as solvent permits the selective cleavage of Trt in the presence of Bpoc or Ppoc under controlled acidolytic conditions. This additional selectivity-step may be utilized when two-chained polypeptides are to be constructed. The procedure consists in acidolytic cleavage with hydrochloric acid at a constant potential as measured by the glass electrode (pH-stat). The automatic protonation of the freshly deprotected amino groups permits the evaluation of kinetic and quantitative data of the cleavage reaction. The selectivity ratios and cleavage conditions of Trt, Bpoc and Ppoc in N(α) are demonstrated here by reference to a series of model dipeptides. The successful application of this technique in the total synthesis of human insulin, a polypeptide with two peptida chains, has recently been described [8].

Apparatus for producing a laminar flow

Abstract: A laminar flow producing means is described having a blower which passes air to a distributor having a buffer zone with a ratio between its volume and cross-sectional area A being smaller than 1/2√A and two mesh screens spaced about 0.2 to 5 cm apart and each having mesh openings measuring about 0.001 to 1mm so that the air from the blower is passed through the screen meshes seriatim to produce a clean, dust-free laminar flow of air.

Methods of forming a fiber reinforced pipe on an inflatable mandrel

Abstract: A method and apparatus is provided for continuously making fiber reinforced plastic pipe in which a conveyor tube is formed on an axially fixed hollow rotatable mandrel. A plurality of bands of resin impregnated fiber elements are wound on the conveyor tube as it advances to provide the pipe assembly. The terminal end of the generated pipe assembly is sealed with a plug. A fluid under pressure is fed through the hollow mandrel and out the forward end of the mandrel into a chamber formed by the generated pipe assembly, the plug, and a fluid sealing means within the pipe assembly being generated, thereby causing the pipe assembly to advance.

Studies in the molecular weight distribution of epoxide resins. I. Gel permeation chromatography of epoxide resins

Abstract: The molecular weight distributions as measured by gel permeation chromatography of solid epoxide resins made by the direct addition of epichlorohydrin to bisphenol A (the “taffy” process) and by the reaction of low molecular weight liquid epoxide resins whose main constituent is the diglycidyl ether of bisphenol A with bisphenol A (the “advancement” process) have been compared with the theoretical distribution calculated by the application of Flory statistics. The model used for predicting the molecular weight distribution has been shown to be too simple to describe the real size distribution of these resins. For resins prepared by the “taffy” process, incompleteness of reaction, the presence of monofunctional epoxides, and the possibility of branching reactions through the epoxide–hydroxyl reaction lead to a distribution that more nearly resembles one calculated for a resin having a higher epoxide value than that actually measured. In the case of resins prepared by the “advancement” process, the presence of small amounts of the higher oligomeric diepoxides and monofunctional epoxides in the starting material used for the synthesis lead to complex molecular weight distributions that are not easy to deduce theoretically. The experimentally determined molecular weight distributions for the higher molecular weight epoxide resins (epoxide value <2 eq/kg) made by the “advancement” process resemble more nearly those calculated for resins having lower epoxide values than those actually measured.

Urethanes containing two perfluoroalkylthio groups

Abstract: Perfluoroalkylthio glycols and esters thereof can be prepared by the free-radical catalyzed addition of a perfluoroalkylthiol to an acetylenic alcohol or ester thereof. The compounds obtained are useful intermediates for the synthesis of fluorochemicals with low free surface energies having oil and water repellent properties. In one embodiment, a perfluoroalkylthio glycol can be reacted with a diisocyanate to obtain a polyurethane containing perfluoroalkylthio groups, which polyurethanes are useful as coatings to provide oil and water repellence to textiles and as additives to plastics to provide mold-release and other desirable properties.

Hindered piperidine carboxylic acids, metal salts thereof and stabilized compositions

Abstract: Compounds having the formula ##STR1## wherein R 1 and R 2 are lower alkyl or together lower alkylene, R 3 is hydrogen, alkyl, methoxyethyl, alkenyl, propargyl, benzyl, alkyl substituted benzyl, or acyl, R 4 is alkylene of 1 to 4 carbon atoms substituted with alkyl or alkenyl of 1 to 18 carbon atoms, alkenylene of 1 to 4 carbon atoms, cycloalkylene, cycloalkenylene, bicycloalkylene, bicycloalkenylene, or phenylene, M is hydrogen or a metal, and z has a value of from 1 to 4, and either (a) R 5 is alkyl of 1 to 6 carbon atoms, R 6 is alkyl of 1 to 6 carbon atoms, and R 7 and R 8 are independently hydrogen or alkyl of 1 to 5 carbon atoms, provided that R 7 and R 8 are not both hydrogen, or (b) R 5 and R 6 are together lower alkylene and R 7 and R 8 are independently hydrogen or alkyl of 1 to 5 carbon atoms, are good light stabilizers. The carboxylic acids are prepared for example, from 2,3,6-trimethyl-2,6-diethylpiperidin-4-ol and 1,2-cyclohexanedicarboxylic anhydride to give 2,3,6-trimethyl-2,6-diethyl-4-piperidyl hydrogen 1,2-cyclohexanedicarboxylate. The metal salts of the acids are readily prepared by reacting the acids or their salts with a reactive form of the metal or metal complex.

Connective tissue-degrading enzymes of human leukocytes

Abstract: Human leukocytes, when exposed to aggregated human gamma-globulin (AHGG) or immune complexes (isolated from RA synovial fluid) fixed to a cartilagenous surface, release neutral proteases that degrade the extracellular matrix of cartilage. The chondromucoprotein destruction by these proteases is suppressed by a variety of synovial fluids but is not susceptible to inhibition by trypsin, chymotrypsin, elastase inhibitors, or a combination of these agents. The inhibitory effect of synovial fluid can be reversed in the presence of increasing enzyme concentrations. Intact viable human polymorphonuclear leukocytes in the presence of AHGG also release a collagenase precursor that can be activated by limited proteolysis with trypsin or RA synovial fluids. Enzyme release (neutral proteases) by phagocytosing cells is inhibited by the antiinflammatory agents phenylbutazone and colchicine; these agents do not affect release of the collagenase precursor. However, the latent collagenase release is susceptible to inhibition when leukocytes are preincubated (prior to exposure to AHGG) with inhibitors of protein synthesis. Under these conditions, neutral protease release is unaffected.

The optimization test in the guinea-pig. A method for the predictive evaluation of the contact allergenicity of chemicals

Abstract: Guinea-pigs were sensitized with various substances (DNCB, penicillin G, PPL, ethylaminobenzoate, formalin) by the Draize method, the maximization method and the new optimization method (intracutaneous test employing adjuvant). The advantages of the optimization method favouring its adoption as a standard sensitization test are discussed in the light of the results obtained by this method and with the two established tests.

Hardenable epoxy resin compositions and process for making the same

Abstract: A curable composition comprising a mixture of an epoxy resin and a hardener can be prepared by dissolving the resin and curing agent in a low boiling solvent and flashing off the solvent at temperatures in excess of 400° F, the evaporating solvent cooling the composition and minimizing precure of the resin. Reinforced composites can be prepared by passing a supporting material such as a continuous web strand or roving through the resin solution and thereafter heating at temperatures above 400° F to remove the solvent without appreciably precuring the resin. The curable epoxy compositions can be used for molding, laminating and the like.

C-glucuronides, a novel type of drug metabolites.

Abstract: The structure elucidation of C-β-glucuronides of sulfinpyrazone (Anturan®) and phenylbutazone (Butazolidin®) by spectroscopic means is reported. These conjugates represent a novel type of drug metabolites.

Containing hindered phenolic norbornane-2,3-dicarboximides stabilized compositions

Abstract: Compounds having the formula ##SPC1## Wherein R 1 and R 2 are lower alkyl, X and Y are hydrogen or, when taken together, they form a bond or an ether linkage, m is 0 to 3, and n is 0 to 2, are good ultraviolet light stabilizers for synthetic polymers.

Relation between plasma concentrations and cardiovascular effects of oral oxprenolol in man

Abstract: Oxprenolol, 40, 80 and 160 mg, was administered orally to seven healthy volunteers. Over the following eight hours repeated measurements were made of the plasma concentrations and effects on heart rate, myocardial contractility (PEPC) and systolic and diastolic blood pressure in recumbency, in the upright position and during physical effort at a work load of 120 watts on a bicycle ergometer. The maximum plasma levels and the area beneath the plasma concentration curves increased roughly in proportion to the dosage increment. No evidence of first-pass inactivation in the liver was found. The half-life of the drug in plasma was approximately 80 minutes, irrespective of the dose administered. Oxprenolol slowed heart rate, prolonged PEPC and lowered systolic blood pressure, by comparison with values recorded after a placebo. The effects were generally least marked in the recumbent position and most marked during effort, when a clear-cut dose-response relation was found. The pharmacodynamic effects of oxprenolol were compared with its concentration in plasma. Marked beta-receptor blockade still persisted eight hours after dosing, although at this time, after doses of 40 and 80 mg, the drug could not be detected in plasma.