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PubMed1978

[Physicochemical studies of Pharmachem's tylosin].

Studied is the effect of high temperature, light, moisture, the type of the solvent and the reaction in the medium on the chemical stability and biological activity of the tylosine base, tylosine tartarate and tylosine phosphate, produced by the "PHARMACHIM" State Economic Corporation. The evaluation of the effect is carried out by using the spectrophotometric (in the UV-region) and microbiological methods (diffusion in agar with Sarcina lutea A. T. C. C. 7341 as a test microorganism). It is found that tylosine is stable thermally both as substance and as solution, yet it loses a large part of its activity when the solutions are exposed to ultraviolet or direct sun light. This calls the solutions of the antibiotics in the course of their preparation, storage and application to be protected from the direct effect of light and that they should be packed in light-proof material. Depending on the air moisture (72--98 per cent), the tylosine base absorbs water from 4 to 11 per cent, the tartarate--from 9 to 37.5 per cent, the phosphate--from 8 to 28.5 per cent, the tylosine tartarate (water-soluble form)--from 7 to 32 per cent, and the tylosine phosphate (granules)--from 12 to 39 per cent of their weights. This requires their storage to be limited to dry, airy premises or they should be hermetically packed. Water, ethanol, methanol, phosphate buffers with pH 6--10.0, dimethylformamide and dimethylsulphoxide do not affect the activity of tylosine, but the last two solvents inhibit the diffusion of the antibiotic in agar and are unsuitable for biological tests. The tylosine base, manufactured by the "Elanco" Company, manifests similar properties in relation to thermal stability, light sensitivity, hygroscopicity and diffusions in agar.

Anti-Bacterial Agents↗
PubMed1994

[Blood serum and milk serum levels of sodium benzylpenicillin after intravenous regional antibiosis in surgery of the claw area in cattle].

An intravenous regional antibiosis using 10 Mega I.U. Sodium-Benzylpenicillin was carried out during surgery in 14 dairy cows affected with spontaneous occurring digital diseases. Blood serum and milk serum levels were determined over a period of 48 hours by means of a micro agar diffusion method using Sarcina lutea Stamm BGA Berlin as a test germ. Even before opening of the rubber tourniquet, penicillin traces were detectable in the blood serum of 6 cows. Maximal concentrations ranging from 0.43 mcg/ml to 8.63 mcg/ml were determined after 45 minutes to 4 hours. 24 hours after intravenous regional antibiosis no levels above the limit of detectability were determined. Significant lower maximal concentrations were found in claw amputation cases as compared with claw preserving surgical interventions. Milk serum levels showed delayed and lower maximal concentrations, ranging between 2.09 and 0.09 mcg/ml. In 5 animals no positive levels were detected. After 48 hours, penicillin levels were below the limit of detectability in the milk of all examined animals.

Anesthesia, Conduction↗
PubMed1994

Evaluation of lung tissue and hilar lymph node concentrations of azithromycin.

Since it is believed that most infections occur in the interstitial fluid, it has been suggested to measure the concentration of antimicrobial agents in pulmonary lymph that reflects the extracellular, extra-blood-vascular milieu in the lung. The aim of this study was to investigate the lung tissue and pulmonary lymph node penetration of azithromycin after 500 mg daily oral administration for three days in patients undergoing open thoracotomy. At the end of the treatment, each subject was assigned for 5 groups of 5 patients each according to thoracotomy time after the last dose (24, 48, 96, 120 and 144 h). Azithromycin was assayed by an agar diffusion method with Sarcina lutea Z114 (DRH) used as the test organism and the Antibiotic Assay Medium 1, pH 8.5 used as the medium. All patients had a detectable concentration of azithromycin in serum 24 h after the last dose (72 h after the first dose); the concentration fell below the detection limit (0.01 mg/l-1) after 96 h (168 h after the first dose). Peak concentrations in lung tissue and lymph nodes were found after 48 h (96 h after the first dose). Tissue and lymph node concentrations of azithromycin were much greater than serum concentrations and these tissue and lymph node concentrations persisted after serum concentrations declined. The concentrations in lung tissue of azithromycin were always higher than corresponding concentrations in hilar lymph nodes.(ABSTRACT TRUNCATED AT 250 WORDS)

Administration, Oral↗
PubMed1975

[Residues of antimicrobial substances in the meat and organs of slaughter calves].

Using a modified Gartside diffusion method (1960) the incidence of the residues of antimicrobial substances was followed in two categories of calves commercially slaughtered at the Brno Slaughter House. For testing the following three collection strains were used: B. subtilis (ATCC 6633), B cereus, var. mycoides (ATCC 11778), Sarcina lutea (ATCC 9341). In light weight calves samples of bile, liver, kidney, diaphragmatic and hind limb muscles, in heavy calves, due to technical reasons, only bile, liver and diaphragmatic muscle samples were examined. Residues were demonstrated in 26.2% of 103 light (suckling) calves; the most frequent finding was in the bile (22.2%) and kidney (15.5%). Identical residue findings in the diaphragmatic muscles and in the skeletal muscles of the hind extremities in light calves correspond to the formerly described results in calves from emergency slaughter (Malíková et al. 1974). In heavy calves the residues were demonstrated in 41.7% of 156 examined; the most frequent finding was in the liver (42.3%) and in the diphragmatic muscles (34%). Under the present operation conditions of calf fattening using milk replacer Biosan 20 not even an interval of 17-20 hours between the last feeding and the slaughter proved sufficient for elimination of the antimicrobial substances from the bodies of the slaughter animals.

Abattoirs↗
PubMedDate not supplied

Detection of beta-lactamase production and enzyme profiles in Enterobacteriaceae isolated in Moldova.

In our study, out of 449 Enterobacteriaceae strains isolated between 1985 and 1990, 16 strains (3 Proteus, 6 nontyphoidal Salmonella, 7 Escherichia coli) were resistant both to Ampicillin- Sulbactam and Amoxycillin-Clavulanic acid associations. The activity profiles of the beta-lactamases produced by these resistant strains are described. Sarcina lutea ATCC 9341 was used as test strain. The effect of the enzymatic filtrate against beta-lactam antibiotics: Ampicillin, Cloxacillin, Cefadroxil, Cefuroxime, Cefotaxime, Ceftriaxone, was followed up. The enzyme types were established according to the ability of inactivating the tested antibiotics. Penicillins and cephalosporins were inactivated by these enzymes, except for Carbenicillin and Oxacillin. These beta-lactamases were resistant to Sulbactam and Clavulanic acid. In the studied Salmonella strains they are plasmidic codified, demonstrating that they belong to a new beta-lactamase class.

Anti-Bacterial Agents↗
PubMed1976

[Persistance of penicillin residues in the calf organism after parenteral therapeutical administration of the preparation penicillin G, procaine inj ad usum vet].

By means of two biological diffusion methods a penicillin content in various calf tissues was determined. For the injections PROKAIN Penicillin G Spofa, inj. adusum vet., was used in a single dose of 25 000 i. u. kg-1 body mass. For the tests three collection strains -- B. subtilis (ATCC 6633), Sarcina lutea (ATCC 9341), and Micrococcus flavus (ATCC 10240) were used. A quantitative determination of penicillin in the samples was accomplished by reading from the standard curves. Sensitivities of the two methods were approximately the same; Micrococcus flavus proved most suitable of the microorganisms employed. At 2, 3, 5 and 20 post-treatment days both test animals were positive; at 10 days three out of four calves examined were positive, whereas at 15 days two out of three calves examined were positive. The residues were most frequently found in the liver, kidney and at the injection sites. Maximum detectable concentrations were at the injections sites, minimum ones in the bone marrow. In the musculature (noninjection site) a small quantity of penicillin was found up to 20 days after the application. Current culinary and technological treatment of positive meat and liver samples did not always suffice for complete inactivation of the penicillin residues. For the tested preparation, a preslaughter withdrawal time of 30 days is recommended.

Abattoirs↗
PubMed1993

New heterocyclic structures. thiazolo[3,2-a][1,2,5] thiadiazolo[3,4-d]pyrimidine and [1,2,5]thiadiazolo[3',4':4,5] pyrimido[2,1-b][1,3]thiazine. biological assays.

6,7-Dihydro-9H-thiazolo[3,2-a][1,2,5]thiadiazolo [3,4-d]pyrimidin-9-one, 7,8-dihydro-6H,10H-[1,2,5]thiadiazolo[3',4':4,5]pyrimido [2,1-b][1,3]thiazin-10-one and its 3-methyl derivative were prepared by reacting 6,7-diamino-2,3-dihydro-5H-thiazolo[3,2-a]pyrimidin-5-one, 7,8-diamino-3,4-dihydro-2H,6H-pyrimido[2,1-b][1,3]thiazin-6-one or its 3-methyl derivative with N-thionylaniline. A reaction mechanism is proposed. The compounds and the sodium salts of (7-amino-2,3-dihydro-5H-thiazolo[3,2-a]pyrimidin-5-on-6-yl)sulfamic acid, (8-amino-3,4-dihydro-2H,6H-pyrimido[2,1-b][1,3]thiazin-6-on-7-yl) sulfamic acid and its 3-methyl derivative were tested for antimicrobial and antimycotic activity on a number of strains, namely: E. Coli, Proteus mirabilis, P. vulgaris, Pseudomonas aeruginosa, Salmonella spp, Staphylococcus spp, Streptococcus faecalis, Bacillus subtilis, Sarcina lutea, Candida albicans, and for antiviral activity on Herpes simplex virus type 1 and Vescicular stomatitis virus. None of the compounds showed antiviral activity or exhibited biological activity against gram-negative, gram-positive bacteria or against mycetes.

Animals↗
PubMed1995

Laboratory and clinical stain removal evaluations of two tartar control dentifrices.

The purpose of this research was to evaluate Colgate original Tartar Control dentifrice (TC) and new Colgate Micro Cleansing Tartar Control (MCTC) dentifrice in a laboratory and clinical study for their ability to remove induced stain. In the laboratory study, polished and etched bovine enamel specimens were stained for 4 days with a coffee, tea, and mucin, Sarcina lutea tartox culture in trypticase soy broth. Sixteen specimens were then brushed for 200 strokes with a sodium carboxymethyl cellulose solution to remove loose stain, and then brushed for 300 strokes with a 1:1 toothpaste slurry. Tooth color was measured by reflectance with the CLE L*a*b* scale. The calculated stain removal, 37% for MCTC and 24% for TC, was significantly different (p<0.01) favoring the MCTC dentifrice. In the clinical study, eight-six subjects were given Peridex (0.12% chlorhexidine gluconate) mouthrinse, a low abrasive dentifrice and a soft toothbrush to use twice a day for 8 weeks. Stain was monitored on the buccal and lingual surfaces of the anterior teeth using the Lobene index. The seventy-seven subjects with sufficient total stain were stratified into two balanced groups, given a new soft toothbrush and were randomly assigned to use one of the dentifrices tested, twice a day for 8 weeks. At 4, 6 and 8 weeks in the study, the MCTC dentifrice product had consistent, significantly (p<0.05-0.001) lower total stain scores than the TC dentifrice. In the laboratory and clinical studies conducted, even though stain induction and evaluation procedures differed, the new Colgate Micro Cleansing Tartar Control dentifrice was significantly more effective at removing stain than the Colgate original Tartar Control dentifrice formula.

Adolescent↗
PubMed1996

Influence of fowl uropygial gland and its secretory lipid components on growth of skin surface bacteria of fowl.

Bacterial species, which occur on the breast skin surface of adult (1 year old) white leghorn fowl with intact uropygial gland, were identified as : Staphylococcus epidermidis, Sarcina lutea, Streptomyces sp. and a facultative diphtheroid belonging to the genus Corynebacterium; S. epidermidis being the most predominant one. Two species of bacteria, namely, Staphylococcus aureus and Proteus sp. were shown to colonize the skin surface after 60 days of captivity. Extirpation of uropygial gland caused severe depletion of population of S. epidermidis, Streptomyces sp. and diphtheroid. The effect was more conspicuous after 60 days compared to that after 30 days of the gland removal. On the skin surface of glandless fowls the population of S. aureus increased significantly and a new form identified as anthracoid bacillus became the most predominant species after 60 days. Addition of total lipids from the free-flowing fowl uropygial secretion, as 0.2% suspension, to trypticase soya broth cultures of individual bacteria of fowl skin surface encouraged strongly the growth of S. epidermidis, Streptomyces sp. and Proteus sp. but suppressed the population of the anthracoid. When identical amount of diester wax or wax alcohol of the secretion was supplemented to the culture, more or less similar result was obtained. Wax alcohol also had a mild inhibitory effect on Streptomyces sp. Wax acids, added to the culture (0.2%) suppressed population of all the bacterial forms except Proteus sp., while the hydrocarbon fraction, which also contained some amount of squalene, produce an opposite effect.

Animals↗
PubMed1996

Biological studies on 1,2-benzisothiazole derivatives V. Antimicrobial properties of N-alkanoic, N-arylalkanoic and N-aryloxyalkanoic derivatives of 1,2-benzisothiazolin-3-one: QSAR study and genotoxicity evaluation.

N-alkanoic, N-arylalkanoic and N-aryloxyalkanoic acids of 1,2-benzisothiazolin-3-one, esters and amides of N-arylalkanoic and N-aryloxyalkanoic acids and 1,1-dioxide derivatives of N-arylalkanoic acids and esters were investigated in vitro antimicrobial activity. N-arylalkanoic and N-aryloxyalkanoic acids (compounds 4-12) and their esters and amides (compounds 13-26) exhibited a good antimicrobial activity against Gram positive bacteria, with several compounds showing potencies 10-20 times higher than 1,2-benzisothiazolin-3-one. None of the chemicals tested inhibited the growth of E. coli. Yeasts and moulds possess a considerable susceptibility to compounds 12-23. The logP (octanol-water) of esters and amides of N-arylalkanoic and N-aryloxyalkanoic acids were measured by the shake-flask technique and the potencies against Gram positive bacteria of the compounds tested was related to their lipophilicity. QSAR analysis showed a bilinear relation, with a logD0 around 3 for the activity on B. subtilis. The phenoxyacetic and phenoxybutyric acid derivatives are positive outliers, showing a potency higher than that predicted from their lipohilicity. The most active compounds were further tested against different Gram positive bacteria and moulds, including Bacilli, Sarcina lutea, Staphylococcus epidermidis, Candida spp. and dermatophytes. The antibacterial and antifungal activity was specific for 1,2-benzisothiazolin-3-ones, the corresponding 1,1-dioxide derivatives being inactive. The genotoxic properties of the compounds studied were evaluated by the Bacillus subtilis rec-assay and Salmonella-microsome test. None of the compounds showed DNA-damaging or mutagenic activity.

Animals↗
PubMed1997

Serum and cerebrospinal fluid concentrations of rifampicin at two dose levels in children with tuberculous meningitis.

Twenty patients of tuberculous meningitis (TBM) in age group of 6 months to 10 years included in the study were divided into two groups of 10 patients each. Rifampicin was administered in dosage of 10 mg and 7.5 mg/kg bw to each patient of groups I and II respectively. Drug concentrations in serum and CSF of these patients were measured by a microbiological tube dilution method using a strain of Sarcina lutea. In group I mean serum and CSF concentration was 3.84 micrograms/ml and 0.178 microgram/ml respectively, while in group II it was 2.16 micrograms/ml and 0.206 microgram/ml respectively. These concentrations were many times higher than the MIC against Mycobacterium tuberculosis. Mean percentage penetration of rifampicin in CSF was 5 and 10% in group I and II respectively. We recommend similar studies in large number of children before advocating the therapy with low dose of rifampicin in TBM.

Antibiotics, Antitubercular↗