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At least 1,171 records · Page 65Linked to original sources
PubMed1987

Effects of sodium taurodihydrofusidate on nasal absorption of insulin in sheep.

To investigate the utility of a novel adjuvant, sodium taurodihydrofusidate (STDHF), as an enhancer of mucosal permeation of drugs, experiments involving intranasal insulin:STDHF administration in sheep were performed. Rabbit erythrocyte lysis assays were employed to assess the relative membrane lytic activity of STDHF, as well as that of its glycine-conjugated analogue, compared with a nonionic detergent and a common bile salt. Equivalent weight concentrations of the fusidates were found to be 5- to 10-fold less lytic than the bile salt and at least 100-fold less lytic than the nonionic detergent laureth-9. Provided the concentration of STDHF was greater than its critical micellar concentration, formulations of insulin with STDHF greatly enhanced intranasal insulin absorption. Optimal nasal insulin absorption was attained at a molar ratio of STDHF to insulin of 5:1. In addition, intranasal absorption was linearly related to insulin dose. Compared with intravenous administration, the mean bioavailability of intranasal insulin was 16.4%. Interovine variability was low, with a coefficient of variation of 14% for 12 animals. It was found that intranasal absorption of sodium insulin was not significantly different from that of zinc insulin. However, formulations of both crystalline insulin preparations were absorbed more efficiently than a formulation prepared using commercially available solutions of U-500 insulin. The results taken together indicate that STDHF is an excellent enhancer of insulin absorption from the nasal mucosa.

Absorption↗
PubMed1991

Intranasal bioavailability of insulin powder formulations: effect of permeation enhancer-to-protein ratio.

The intranasal administration of powder formulations containing insulin and the permeation enhancer sodium tauro-24,25-dihydrofusidate (STDHF) were investigated in the sheep model. Both the hypoglycemic response and the serum insulin levels increased as the mole ratio of STDHF to insulin was increased from 0 to 16.8. In vitro dissolution rates of the powders and the rapid tmax (approximately 5 min) observed after intranasal administration suggest that the absorption of insulin is not dissolution limited. The bioavailabilities (F) of the powder formulations ranged from 2.9 to 37.8%. In comparison, the F values for a solution formulation with a STDHF:insulin ratio of 8.4 administered as either drops or spray were 15.7 and 37.4%, respectively. The permeation enhancer STDHF increases mucosal permeability and reduces the average molecular weight of the insulin species.

Absorption↗
PubMed1994

Aggregation behavior of sodium fusidate in aqueous solution.

We analyzed the freezing point depression and pNa measurements for aqueous solutions of sodium fusidate. At concentrations lower than 0.011 mol kg(-1), sodium fusidate behaves as a strong 1:1 electrolyte. At higher concentrations, sodium fusidate self-aggregates. To analyze the results two hypotheses on the monomer concentration are presented and discussed. The first one accepts that the monomer concentration, C(A), is constant and equal to 0.023 mol kg(-1). This concentration corresponds to a break point in the plot of the freezing point depression vs total sodium fusidate concentration, C(A)t. The second hypothesis accepts that C(A) increases with C(A)t following a leveling-off curve. Measurements of hydrodynamic radii and comparison with similar systems, such as sodium taurocholate, strongly support the second hypothesis. The results indicate that at concentrations lower than 0.08 mol kg(-1) the aggregation number increases from 2 to 3. Above this concentration, both the aggregation number and the fraction of bound counterions remain constant, with average values of 3.13 +/- 0.10 and 0.31 +/- 0.05, respectively. Such results indicate that for trimers only one Na+ counterion is involved per aggregate. We propose that this counterion shields the repulsion between the two nearest carboxylate groups which, according to a disklike model in which the monomers are packed with that group alternatively oriented up and down, should hold together. Values for the formation equilibrium constant of aggregates are also calculated. Its dependence with the aggregation number allows the determination of the reversible transfer of a free surfactant ion together with the associated counterions from the bulk solution to the aggregate, the resulting value being w(0) = -4.2k(B)T.

Anti-Bacterial Agents↗
PubMed1994

In vivo and in vitro EPR oximetry with fusinite: a new coal-derived, particulate EPR probe.

The peak-to-peak line width (LW) of the first derivative electron spin resonance (EPR) spectrum of the coal maceral fusinite is reversibly broadened by O2. The extent of broadening per unit of partial pressure of oxygen (pO2) is unusually large, exceeding that of nitroxides by almost two orders of magnitude. This paramagnetic property of fusinite, combined with its very stable physicochemical properties and low toxicity, is shown to be of utility in the measurement of pO2 in vitro and in vivo. Fusinite particles are endocytosed by chinese hamster ovary (CHO) cells in vitro; this is useful for intracellular O2 measurements with commercially available EPR spectrometers operating at 9.1-9.3 GHz. For measurement of oxygen in vivo using low frequency EPR (1.1-1.3 GHz), fusinite provides a sensitive and persistent means to measure pO2 in tissues. Particles implanted into the gastrocnemius muscle of A/J mice remained interstitially in the same position for months with undiminished sensitivity to pO2 and no specific toxic effects.

Adsorption↗
PubMed1999

Evidence that MRas1 and MRas3 proteins are associated with distinct cellular functions during growth and morphogenesis in the fungus Mucor racemosus.

The filamentous fungus Mucor racemosus provides a simple and unique model system for defining the function of individual ras genes in a gene family which is closely related to mammalian ras genes. The current study was designed to investigate the role of Mras1 and Mras3 in different stages of fungal morphogenesis, including sporangiospore germination, sporulation, and dimorphic transitions. The overall patterns of Mras1 and Mras3 transcript and protein accumulation were markedly different but, in general, transcripts and proteins were present at low levels during spherical growth and their accumulated level increased severalfold during polar growth (germ tube emergence and elongation). In contrast to Mras1, relatively high levels of Mras3 transcript accumulated during sporulation and MRas3 protein accumulated in sporangiospores. Transformation of M. racemosus with an activated allele of Mras3 reduced growth rate during aerobic sporangiospore germination, while a dominant-negative allele of Mras3 caused a 40% decrease in viable asexual spores. An activated allele of Mras1 increased growth rate during sporangiospore germination but neither activated nor dominant-negative alleles of Mras1 affected total number of asexual spores. Expression of MRas3 and MRas1 proteins appear to be subject to different regulatory mechanisms: exogenous dibutyryl-cAMP and fusidienol caused a strong repression of the level of MRas3 protein (but not MRas1) concurrent with the inhibition of polar growth. Differential posttranslational modification and intracellular localization of MRas1 and MRas3 proteins were also observed. The data strongly suggest that Mras3 and Mras1 play different roles in regulation of cell growth and morphogenesis in Mucor.

Alkyl and Aryl Transferases↗
PubMed2000

Sodium fusidate ameliorates the course of diabetes induced in mice by multiple low doses of streptozotocin.

We studied the effects of the immunosuppressant sodium fusidate (fusidin) on murine immunoinflammatory diabetes mellitus (DM) induced by multiple low doses of streptozotocin (SZ). Fusidin was given by gavage to three strains of mice (C57KsJ, C57BL/6, CD1) at doses 10 or 100 mg/kg body weight every other day. The drug was administered as an early or late prophylactic regime starting either 1 day prior to the first or after the fifth and last injection of SZ. In both situations the largest dose of fusidin successfully reduced the clinical, chemical and histological signs of DM, the treated mice having significantly lower glycaemic values and milder (often absent) insulitis compared with sham-treated animals or controls given SZ alone. The antidiabetogenic effect was long-lasting as it was maintained up to 1 month after cessation of therapy. In contrast, fusidin prophylaxis failed to prevent development of hyperglycaemia acutely induced by one single and high (160 mg/kg) dose of SZ, which is a model of DM primarily due to the toxic action of SZ on the beta cells and does not involve immunopathogenetic mechanisms. On day 14 after SZ, fusidin markedly altered the circulating cytokine profile induced in vivo by ConA, reducing the levels of IFN-gamma, IL-2 and TNF-alpha and augmenting the level of IL-6. However, only the inhibitory effect of the drug on the synthesis/release of IFN-gamma seemed to be causally related to its capacity to counteract the SZ-induced DM. In fact, the disease was prevented by a neutralizing monoclonal antibody (mAb) against IFN-gamma, but not by anti-IL-2 receptor mAb, a soluble form of TNF-receptor type 1 or recombinant human IL-6. The prevention of disease by fusidin was also partly reversed by exogenously administered recombinant mouse IFN-gamma. The data provide further in-vivo evidence for the anti-diabetogenic and immunomodulatory properties of fusidin and indicate that this drug could have a role in prevention and treatment of human type 1 DM.

Animals↗
PubMed1995

Biodegradable implants for potential use in bone infection. An in vitro study of antibiotic-loaded calcium sulphate.

Local antibiotic therapy by diffusion from plaster of Paris beads has proved promising in bone surgery. Sustained local delivery depends on thermostability, so we tested the antibacterial activity of 11 antibiotic solutions after storage at 37 degrees C using a microbiological method. Cephalosporins and penicillins were unstable, but aminoglycosides remained fully stable with 100% activity after 2 weeks. About 60% of the initial bactericidal activity of quinolone, glycopeptides and sodium fusidate were still detectable after 2 weeks. Release of these antibiotics from plaster of Paris beads was evaluated in vitro. Even those in the same family differed in their release rate. Plaster beads with sodium fusidate were the most effective association. A therapeutic level of glycopeptides, aminoglycosides and amoxicillin was leached for about 3 weeks. Cephalosporins and sodium amoxicillin were released in 2 to 3 days, and quinolone beads were too brittle to be used. Plaster of Paris, which is cheap, biocompatible and biodegradable, is an excellent carrier for sodium fusidate, aminoglycosides and glycopeptides.

Aminoglycosides↗
PubMed1977

Mapping of the drug resistance genes carried by the r-determinant of the R100.1 plasmid.

We have cloned the EcoRI fragments of pLC1, a circular DNA element found in an Escherichia coli dnaAts strain integratively suppressed by R100.1 (Chandler et al., 1977a), using the plasmid vector pCR1. All the resistance genes known to be present on the r-determinant of R100.1 were found to be present on pLC1. The isolation of pCR1 derivatives carrying various EcoRI fragments of either pLC1 or R100.1 has allowed a more precise mapping of the position of the resistance genes on the R100.1 molecule.

Chloramphenicol↗
PubMed1997

Nosocomial outbreak of Clostridium difficile diarrhea in a pediatric service.

An outbreak of nosocomial diarrhea that occurred in a pediatric orthopedic service between 1 December 1993 and 15 April 1994 is reported. A total of 37 patients (mean age, 9.6 years; range, 2 months-19.3 years) were involved in the outbreak, including six patients with bacteriologically documented Clostridium difficile infection. A multivariate analysis identified lincomycin treatment for at least three days as the only significant risk factor. Stool samples from four asymptomatic patients were also positive for Clostridium difficile and its cytotoxins. Isolates from all patients belonged to serogroup C, were highly resistant to lincomycin, and exhibited the same restriction pattern by pulsed-field gel electrophoresis. The outbreak ended after treatment with lincomycin was discontinued and hygiene control measures were implemented.

Adolescent↗