摘要:

Pharmacokinetics of phenoxymethylpenicillin was studied in 12 healthy volunteers. They received four different single oral dose sizes. At all dose levels (0.4, 1, 2 and 3 g) phenoxymethylpenicillin was rapidly absorbed, usually with serum peaks within 0.75 h. The mean maximal serum peaks ( ± SD) were 6.1 ± 2.0, 15.0 ± 4.3, 26.3 ± 10.0 and 35.5 ± 10.8 mg/l after 0.4, 1, 2 and 3 g, respectively. The relationship between the mean peak serum concentrations and the doses was nonlinear (p < 0.001). The mean areas under the serum concentrations vs. time curve (AUC) increased almost linearly with increasing doses, and the deviation from linearity was not significant (p < 0.05). Very low penicillin concentrations were obtained in saliva. The urinary excretion during 10 h was 37–43% of the doses given. The pharmacokinetic results indicated that phenoxymethyl penicillin in the present formulation is rapidly and well absorbed up to as high doses as 3 g. The tablet formulations used were better absorbed than previous ones. The percent of absorption was relatively lower with the highest doses, but this probably has only minor therapeutic conseq

ISSN:0009-3157    

DOI:10.1159/000238084

出版商:S. Karger AG    

年代:1982

数据来源: Karger

摘要:

A modified high-performance liquid chromatographic (HPLC) method for sensitive and rapid determination of trimethoprim, sulfamethoxazole and its metabolite N4-acetylsulfamethoxazole has been compared with the bioassay for trimethoprim and a colorimetric procedure for sulfonamides. The sensitivity of the (HPLC) method has been increased by ultrafiltration of the sample. Thus, the sample dilution was markedly reduced compared to the values obtained with precipitation procedures. The recovery was 102.7 ± 6.1% for trimethoprim, 93 ± 5.4% for sulfamethoxazole and 90.2 ± 7.9% for N4-acetylsulfamethoxazole. The between-day reproducibility was 5% (n = 5). The coefficients of correlation for HPLC and reference methods were 0.993 (bioassay) and 0.995 (colorimetic assa

ISSN:0009-3157    

DOI:10.1159/000238085

出版商:S. Karger AG    

年代:1982

数据来源: Karger

摘要:

The in vitro activities of three aminoglycosides [Schering 21420 (a 1N-HAPA derivative of gentamicin B), amikacin and gentamicin] plus carbenicillin or piperacillin were tested against 16 clinical isolates of Pseudomonas aeruginosa. Piperacillin, when combined with any of the three aminoglycosides, demonstrated synergy significantly more frequently than carbenicillin plus these same aminoglycosides.

ISSN:0009-3157    

DOI:10.1159/000238086

出版商:S. Karger AG    

年代:1982

数据来源: Karger

摘要:

The standardized Bauer-Kirby agar diffusion test served to examine 100 clinical isolates of Pseudomonas aeruginosa against various recently introduced broad-spectrum penicillins and cephalosporins. Neither cefotaxime nor lamoxactam displayed significant activity against this microorganism. Azlocillin, cefsulodin, and piperacillin were significantly more effective (p < 0.0001) than mezlocillin against the majority of isolates. When compared individually, azlocillin and piperacillin displayed comparable in vitro activity; the same was true for cefsulodin compared with piperacillin. On the other hand, cefsulodin was somewhat more active than azlocillin (p 0.01) against P. aeruginosa. These data should enable diagnostic laboratories to curtail the number of antimicrobial drugs routinely utilized to examine clinical isolates of P. aeruginosa for antibiotic susceptibility, i.e., piperacillin exclusively.

ISSN:0009-3157    

DOI:10.1159/000238087

出版商:S. Karger AG    

年代:1982

数据来源: Karger

摘要:

In vitro studies were performed to examine the potential usefulness of two new drugs, moxalactam and cefoperazone, for the treatment of infections caused by Streptococcus pneumoniae. 34 isolates of S. pneumoniae 1 μg/ml) were also resistant to moxalactam (MIC =128 μg/ ml) but were sensitive to cefoperazone (MIC = 2–4 μg/ml). All isolates relatively resistant to penicillin (MIC 0.25–0.5 μg/ml) were sensitive to cefoperazone (MIC 0.25–1 μg/ml) and had moxalactam MICs of 4–16 μg/ml for 10/12 isolates. The disk diffusion test was unreliable for detecting strains relatively resistant to moxalactam. These studies showed that cefoperazone is more active than moxalactam in vitro against 5. pneumoniae regardless of the penicillin susceptibility of t

ISSN:0009-3157    

DOI:10.1159/000238088

出版商:S. Karger AG    

年代:1982

数据来源: Karger

摘要:

N-Formimidoyl thienamycin (MK0787) was found to be active against 21 gram-negative isolates, selected for their β-lactamase production. None of the crude β-lactamases could hydrolyze MK0787 or cefoxitin, in contrast to cefotaxime which was moderately attacked by a number of enzymes. MK0787 behaved as a moderate inhibitor of most β-lactamases, whereas cefoxitin and cefotaxime were strong inhibitors of cephalo-sporinases but not of broad-spectrum enzymes. The new compound had good penetration characteristics in a strain of Enterobacter cloacae, in contrast to cefoxitin. Against a number of trained cefamandole- and cefoxitin-resistant variants, MK0787 was clearly the most active of the compounds test

ISSN:0009-3157    

DOI:10.1159/000238089

出版商:S. Karger AG    

年代:1982

数据来源: Karger

摘要:

The quinazoline analog of folic acid, 5,8-dideazaisofolic acid (IAHQ), was tested for its effects on the growth of human tumor cells in vitro and in vivo. Of 23 human tumor cell lines tested in vitro, 7 were inhibited by IAHQ (ED50, 5 × 10-6 to 5 × 10-7 M). For in vivo studies, human osteosarcoma (OS) cells from the IAHQ-sensitive line TE-85 were implanted intraperitoneally in newborn hamsters: in the group treated with IAHQ, only 30% of the animals developed OS, compared with 100% of those not treated with IAHQ. The effects of IAHQ injections on mitogenic responses and natural killer activity of lymphocytes from normal 3-month-old hamsters were also examine

ISSN:0009-3157    

DOI:10.1159/000238090

出版商:S. Karger AG    

年代:1982

数据来源: Karger

摘要:

The antitumour properties of the drug N-137 were assessed in vivo in two mu-rine T lymphoma models and two naturally metastatic hamster fibrosarcomas of Herpesvirus hominis aetiology. N-137 therapy caused a significant delay in the subcutaneous growth rate of both lymphomas (EL4 and TLX9) and in many cases completely prevented tumour appearance when administered at high doses. The antitumour effect observed in both systems was shown to be dose dependent. In contrast, N-137 therapy failed to influence the growth of two hamster fibrosarcomas (HSV-333–2-26 Met A and Met B lines), and drug administration prior to or following resection of Met B tumours failed to influence the development of natural metastases as measured by monitoring animal surviva

ISSN:0009-3157    

DOI:10.1159/000238091

出版商:S. Karger AG    

年代:1982

数据来源: Karger

摘要:

Anti-tumour activity of RC-18, a pure isolate from Rubia cordifolia was repeatedly tested in different sets of experiments on a spectrum of experimental murine tumours, viz. P388, L1210, L5178Y, B16 melanoma, Lewis lung carcinoma and sarcoma-180. RC-18 exhibited significant increase in life span of ascites leukaemia P388, L1210, L5178Y and a solid tumour B16 melanoma. However, it failed to show any inhibitory effect on solid tumours, Lewis lung carcinoma and sarcoma 180. Promising results against a spectrum of experimental tumours suggest that RC-18 may lead to the development of a potential anti-cancer agent.

ISSN:0009-3157    

DOI:10.1159/000238092

出版商:S. Karger AG    

年代:1982

数据来源: Karger

摘要:

The efficacy of six antistaphylococcal agents for the treatment of experimental methicillin-resistant Staphylococcus aureusinfections was studied. Mice were injected intravenously with ≈ 5 × 108 methicillin-resistant S. aureus and treated by intraperitoneal administration of antimicrobics. Vancomycin, trimethoprim-sulfamethoxazole and rifampin therapies resulted in increased survival when compared to untreated contro

ISSN:0009-3157    

DOI:10.1159/000238093

出版商:S. Karger AG    

年代:1982

数据来源: Karger