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Biomedical subjects

H Noguchi

Publications and source records attributed to H Noguchi.

At least 433 records · Page 24Linked to original sources
PubMed1980

Metabolic fate of [14C]-ceftizoxime, a parenteral cephalosporin antibiotic, in rats and dogs.

The metabolic fate of (6R,7R)-7-[(Z)-2-(2-amino-4-thiazoyl)-2-methoxyiminoacetamido]-8-oxo-5-thia-1-a zabicyclo[4,2,0]oct-2-ene-2-carboxylic acid (ceftizoxime), a new cephalosporin antibiotic for injection, was investigated in rats and dogs after i.v. dosing. Ceftizoxime was rapidly and widely distributed in the whole body of rats except the brain. The concentrations were high in the serum as well as in the kidneys, liver, lungs, trachea and skin. A small amount of radioactivity passed the placenta. Serum levels of ceftizoxime declined with a half-life of 0.22 h in rats and 0.98 h in dogs. Most of the serum radioactivity was present as unchanged ceftizoxime in dogs. Urinary excretion was rapid and this elimination route was predominant in the two species. Small amounts of metabolites of ceftizoxime were found in the rat urine and bile, however, a major portion of the given dose was excreted in unchanged form. In dogs, ceftizoxime was resistant to metabolic degradation in the body.

Animals↗
PubMed1980

[Application to dental casting machine of the rapid heating infrared image furnace (author's transl)].

The authors tried to manufacture a casting machine in dentistry by application of the infrared image furnace with a high heating speed and an easy control of a heating temperature. This machine melts an alloy in a carbon crucible set in the furnace, held in the horizontal position. Then, the furnace is turned to the vertical position to drop a melted alloy on the casting mold, and the alloy is cast in the mold by the pressure of Argon gas. The functions of trial casting machine were follows. 1. The trial casting machine was capable of heating to 1250 degrees C within one minute under 4 kW electric power. 2. The castability of the 20% Au-Pd-Ag commercial alloy cast in all casting conditions by the trial casting machine was higher than that of Thermotrol D-2 automatic centrifugal casting machine. 3. Castings of the trial casting machine showed higher tensile strength and elongation than those of the centrifugal casting machine, and the deviation of values got by the trial casting machine was small. In particular, some casting of the trial casting machine showed three times or over elongation values as compared with those of the centrifugal casting machine. 4. When casting conditions (casting temperature, casting pressure) of the trial casting machine changed, the physical properties of castings did not change so much. However, when the mold was not prevented from heating by the furnace in casting, the elongation of castings increased.

Dental Casting Technique↗
PubMed1980

Disposition and enterohepatic circulation of diclofenac in dogs.

Following i.v. administration of 14C-labelled 2-(2',6'-dichloroanilino) phenylacetic acid (14C-diclofenac) (25 mg/kg) to dogs, 65% of the dose of total radioactivity was excreted in the bile in the first 6 h. A trace of unchanged diclofenac and three metabolites were demonstrated in the bile by 2-dimensional TLC. Two of these metabolites were identified as diclofenac acyl-glucuronide (80% of total radioactivity in the bile) and taurine conjugate (10%); the third was an unknown metabolite (2%). Diclofenac acyl-glucuronide was hydrolyzed by weak alkaline and beta-glucuronidase. Intraduodenally administered diclofenac acyl-glucuronide was absorbed, and then excreted in the bile again. This suggests that diclofenac acyl-glucuronide is hydrolyzed in the intestine, and undergoes enterohepatic circulation. The plasma half-life of diclofenac was 1.3 h in dogs.

Animals↗
PubMed1980

A study on radiosensitivity and prognostic factors of cervical adenocarcinoma.

Investigations were made, with the patient having uterine cervical adenocarcinoma of differentiated type, on the histological damage of tumor cells caused by irradiation, on the time course of the of the diminution of adenocarcinoma cells and on the reason why the prognosis of patients with adenocarcinoma is usually poorer than those with squamous cell carcinoma. The results obtained are as follows: 1. As to the histological picture of good irradiation effect, the damage of the nucleus, desquamation of adenocarcinoma cells from their bases and the decrease of the number of adenocarcinoma cells due to irradiation was markedly slower than that of squamous cell carcinoma. 3. As important factors affecting the prognosis of patients with adenocarcinoma, the method of treatments, clinical stage, the size of cervical tumor and the degree of histological invasion may be implicated. In particular, regardless to the method of treatments good prognosis may not be expected to the case which is at advanced clinical stage, has hypertrophy of the cervix cervix greater than 4.5 cm in diameter or deep ulcer formation or shows histological picture of severe infiltration.

Adenocarcinoma↗
PubMed1979

Comparative studies of penicillin-binding proteins in Pseudomonas aeruginosa and Escherichia coli.

Penicillin-binding proteins in Pseudomonas aeruginosa were compared with those of Escherichia coli. These in P. aeruginosa were found exclusively in the cytoplasmic membrane fraction (fraction soluble in sodium N-lauroyl sarcosinate). Sodium dodecyl sulfate/acrylamide gel electrophoresis of the proteins bound to [14C]penicillin G resulted in the separation of six major bands and several minor bands. The proteins in these bands are referred to as proteins 1A, 1B, 2, 3, 4 and 5 in order of increasing electrophoretical mobility. The electrophoretic mobilities and other properties of penicillin-binding proteins in P. aeruginosa and E. coli were compared and correlated. Fundamentally they seem to be very similar in the two bacteria, but proteins 1A and 1B in P. aeruginosa seem to correspond respectively to proteins 1B and 1A in E. coli, and protein 6 seems to be missing or present in only small amount in P. aeruginosa. In addition, the affinities of currently developed beta-lactam antibiotics to each protein of P. aeruginosa and E. coli were examined in relation to the morphological changes of the cells induced by these antibiotics and their antibacterial potencies. Mecillinam showed high affinity to only protein 2 in both P. aeruginosa and E. coli. At a minimal inhibitory concentration, it converted cells of both P. aeruginosa and E. coli from rods to spherical cells, although its minimal inhibitory concentration was much higher for P. aeruginosa than for E. coli.

Binding, Competitive↗
PubMed1979

Pharmacokinetics and metabolism of 2-chloro-11-(2-dimethylaminoethoxy)-dibenzo[b,f]thiepine (zotepine) in rat, mouse, dog and man.

The absorption, distribution, metabolism and excretion of 2-chloro-11-(2-dimethylaminoethoxy)dibenzo [b,f]thiepine (zotepine), a new neuroleptic agent, were investigated in rat, mouse, dog and man. Zotepine was absorbed rapidly and almost completely from the gastrointestinal tract in all species after oral dosing. The serum level of the unchanged drug in man was comparatively higher than in animals. The serum half-lives of zotepine after i.v. dosing were approximately 3.2 h in rats, 1.5 h in mice and 3.0 h in dogs. The drug and radioactive metabolites were rapidly distributed to the tissues of rats and mice, and the brain levels of the unchanged drug were about 20 to 30 times higher than the serum levels. Only small amounts of the unchanged drug were excreted in the urine in all species; faecal excretion through the bile was the main route of elimination of the drug and metabolites. Extensive biliary excretion and enterohepatic circulation of the radioactive compound were observed in rats. Zotepine was well metabolized in the body. Besides N-demethylation and oxygenation of the N and/or S atoms, hydroxylation of the aromatic ring and consecutive conjugation were important metabolic pathways of zotepine.

Adult↗
PubMed1978

Antibacterial activity of apalcillin (PC-904) against gram-negative bacilli, especially ampicillin-, carbenicillin-, and gentamicin-resistant clinical isolates.

Apalcillin (PC-904) is active against carbenicillin- and ampicillin-resistant strains of gram-negative bacilli. Among Pseudomonas aeruginosa strains highly resistant to carbenicillin (>/=3,200 mug/ml), half of them were susceptible to PC-904 at a concentration of 50 to 1,600 mug/ml. The minimal inhibitory concentration of PC-904 against P. aeruginosa strains resistant to carbenicillin (400 to 1,600 mug/ml) ranged from 3.1 to 25 mug/ml. Ampicillin- and carbenicillin-resistant Enterobacteriaceae strains were similarly susceptible to PC-904. However, drug resistance to PC-904 was already apparent among some strains of P. aeruginosa, Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, P. vulgaris, and P. morganii, recently isolated in Japan; i.e., 4, 35, 32, 4, 6, and 14% of strains isolated were resistant. PC-904 was more active, on the other hand, than ampicillin and carbenicillin against antibiotic-susceptible Enterobacteriaceae and also showed high activity against most species of Pseudomonadaceae, especially P. cepacia and P. aeruginosa. The minimum inhibitory concentrations of PC-904 were greatly affected by inoculum size when the organisms tested were strains producing large amounts of beta-lactamase.

Ampicillin↗
PubMed1978

New antipseudomonal penicillin, PC-904: affinity to penicillin-binding proteins and inhibition of the enzyme cross-linking peptidoglycan.

The mechanism of action of a new antipseudomonal penicillin, PC-904, was studied with respect to its binding affinities to penicillin-binding proteins (PBPs) and its inhibitory activities on cross-linking enzymes of peptidoglycan synthesis in vitro. PC-904 showed especially high affinity (compared with that of penicillin G) to Escherichia coli PBP-3. It also had high affinities to PBP-2 and -1Bs and low affinities to PBP-1A, -4, -5, and -6. Similar results were obtained with Pseudomonas aeruginosa, in which this antibiotic showed very high affinity (compared with that of penicillin G) to PBP-3, -1A (presumably corresponding to E. coli PBP-1Bs), and -2; there was especially high affinity to PBP-3 and much less affinity to PBP-1B (presumably corresponding to E. coli PBP-1A). These results are compatible with morphological observations that at concentrations near its minimal inhibitory concentration or less, this antibiotic induced the formation of filamentous cells of E. coli and P. aeruginosa. At higher concentrations or after prolonged incubation, it induced lysis of the cells. The remarkably high affinity of PC-904 to pseudomonal PBP-3, -1A, and -2 may partly explain the potent antipseudomonal activity of this antibiotic. In E. coli, the concentration of PC-904 required to inhibit the cross-linking reaction in enzymatic peptidoglycan synthesis, presumably carried out by PBP-1Bs, was as low as the inhibitory concentrations of penicillin G, ampicillin, and carbenicillin.

Ampicillin↗
PubMed1978

Computer-assisted system for a mycobacteria tuberculosis laboratory using MUMPS.

A Laboratory Information System (LIS) has been developed and the main part of LIS is an on-line system with auto analysers. In April 1976, the Biochemistry Laboratory was computerized in Osaka Prefectural Habikino Hospital. This LIS uses a PDP 11/40 minicomputer system using MUMPS language. At present a Mycobacteria Tuberculosis Laboratory (MTL) is computerized using the same computer and MUMPS. In this laboratory, there is no auto analyser, so this computerization aims at saving on labour in paper work and increasing the reliability of test results. This paper shows that the computerization of MTL with no auto analyser can be effectively achieved using MUMPS.

Computers↗