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1.
Drug Deliv Transl Res ; 8(1): 291-302, 2018 02.
Artículo en Inglés | MEDLINE | ID: mdl-29235075

RESUMEN

Fibers of poly(L-lactic acid) (PLLA)/polyhydroxybutyrate (PHB) with different concentrations of the drug dipyridamole (DPD) were prepared using solvent-free melt electrospinning to obtain a polymeric drug delivery system. The electrospun fibers were morphologically, structurally, thermally, and dynamically characterized. Crazes that resemble lotus root crevices were interestingly observed in the 7:3 PLLA/PHB fibers with 1% DPD. The crystallinity of PLLA slightly decreased as PHB was incorporated, and the addition of DPD significantly reduced the melting temperature of the composite. The interactions between PLLA and PHB mainly occurred at a proportion of 7:3, and drug encapsulation in the fibers was verified. The kinetic profiles of drug release demonstrated the predominant multiple patterns involving a diffusional stage in the short-term mode of release and kinetic process related to the hydrolysis of the biopolymers. Furthermore, the dynamic behavior of the polymer molecules was evaluated based on the segmental mobility using probe electron spin resonance spectroscopy. The segmental mobility in the amorphous fraction of PLLA decreased with increasing PLLA content. The 9:1 PLLA/PHB system was more resistant to polymer hydrolysis than to the 7:3 system and the rate of diffusion transport was approximately two times higher for the 7:3 PLLA/PHB fibers than for the 9:1 PLLA/PHB fibers.


Asunto(s)
Dipiridamol/química , Fibrinolíticos/química , Hidroxibutiratos/química , Poliésteres/química , Rastreo Diferencial de Calorimetría , Preparaciones de Acción Retardada/química , Difusión , Composición de Medicamentos/métodos , Liberación de Fármacos , Espectroscopía de Resonancia por Spin del Electrón , Hidrólisis , Espectroscopía Infrarroja por Transformada de Fourier , Difracción de Rayos X
2.
Int J Antimicrob Agents ; 14(2): 151-6, 2000 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-10720806

RESUMEN

Pseudomonas aeruginosa is important in the field of infectious disease especially with respect to its role in nosocomial infections. Infections with P. aeruginosa may be a problem as the organism has intrinsic resistance to several antibiotics and a capability in acquiring resistance during antibiotic therapy. Fluoroquinolones are sometimes used during antibiotic therapy of P. aeruginosa infections even though resistance to fluoroquinolones may develop. Six strains of P. aeruginosa were studied in an attempt to elucidate the mechanisms of resistance to fluoroquinolones. These included the electrophoresis patterns of the outer membrane proteins (OMPs), random amplified polymorphic DNA (RAPD) and polymerase chain reaction (PCR) analyses. A method is described that improved the clarity of the OMP gels. Resistance in these P. aeruginosa strains could depend not only on DNA-gyrase modifications but also on membranes alterations and on the presence (qualitative and quantitative) of the efflux pump formed by three subunits.


Asunto(s)
Antiinfecciosos/farmacología , Pseudomonas aeruginosa/efectos de los fármacos , Secuencia de Bases , Cartilla de ADN , Farmacorresistencia Microbiana/genética , Electroforesis en Gel de Poliacrilamida , Fluoroquinolonas , Humanos , Pruebas de Sensibilidad Microbiana , Reacción en Cadena de la Polimerasa , Infecciones por Pseudomonas/tratamiento farmacológico , Infecciones por Pseudomonas/microbiología , Pseudomonas aeruginosa/genética
3.
J Chemother ; 8(3): 193-9, 1996 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-8808715

RESUMEN

The in vitro activity of cefdinir (CI-983, FK-482), an orally absorbed aminothiazolyl cephalosporin, was evaluated against all 287 strains of Haemophilus influenzae, Haemophilus parainfluenzae, Moraxella catarrhalis, Streptococcus pneumoniae and Streptococcus pyogenes in comparison with cefaclor, cefuroxime, amoxicillin, amoxicillin-clavulanic acid, erythromycin and cotrimoxazole. The bactericidal activity of cefdinir, cotrimoxazole, amoxicillin-clavulanic acid and erythromycin was determined against H. influenzae, M. catarrhalis and S. pneumoniae. With the exception of one beta-lactamase negative ampicillin-resistant strain of H. influenzae (resistant to all antibiotics tested), no resistance to cefdinir was observed (MIC < or = 1 mg/l). Cefdinir was active against H. influenzae, H. parainfluenzae and M. catarrhalis regardless of whether or not they produced beta-lactamase. In general, the inhibitory concentrations of cefdinir against H. influenzae, H. parainfluenzae and M. catarrhalis were similar to those of amoxicillin/clavulanic acid, one or two dilutions lower than those of cefuroxime and four dilutions lower than those of cefaclor and cotrimoxazole. Against S. pneumoniae and S. pyogenes cefdinir had the same activity as cefuroxime and amoxicillin but was more effective than the other antibiotics tested. Kinetic studies showed that cefdinir was rapidly bactericidal at concentrations 2 and 4 times the minimum inhibitory concentration (MIC): a reduction of 99.9% in CFU values was generally observed after 6-8 h.


Asunto(s)
Cefalosporinas/farmacología , Farmacorresistencia Microbiana , beta-Lactamasas/metabolismo , Administración Oral , Amoxicilina/farmacología , Antibacterianos/farmacología , Cefaclor/farmacología , Cefdinir , Cefuroxima/farmacología , Cefalosporinas/administración & dosificación , Ácido Clavulánico , Ácidos Clavulánicos/farmacología , Eritromicina/farmacología , Haemophilus influenzae/efectos de los fármacos , Haemophilus influenzae/enzimología , Haemophilus influenzae/aislamiento & purificación , Moraxella catarrhalis/efectos de los fármacos , Moraxella catarrhalis/enzimología , Moraxella catarrhalis/aislamiento & purificación , Penicilinas/farmacología , Sicilia , Streptococcus pneumoniae/efectos de los fármacos , Streptococcus pneumoniae/enzimología , Streptococcus pneumoniae/aislamiento & purificación , Streptococcus pyogenes/efectos de los fármacos , Streptococcus pyogenes/enzimología , Streptococcus pyogenes/aislamiento & purificación , Relación Estructura-Actividad
4.
J Chemother ; 7(6): 530-4, 1995 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-8667038

RESUMEN

We determined the bactericidal kinetics and postantibiotic effect (PAE) of sparfloxacin against Haemophilus influenzae, Moraxella (Branhamella) catarrhalis, Klebsiella pneumonia, Streptococcus pneumoniae, and Staphylococcus aureus. Time-kill studies were performed by using 1 x and 4 x the minimum inhibitory concentrations (MICs) of sparfloxacin, ciprofloxacin, co-trimoxazole, amoxicillin/clavulanic acid and erythromycin (inoculum 10(5) and 10(7) CFU/ml). The PAE was induced by exposing the strains to 1xMIC and 4xMIC of sparfloxacin and ciprofloxacin for 1 h. Sparfloxacin was the most bactericidal of all the antibiotics tested, being active against Gram-positive and Gram-negative isolates with a 99.9% reduction within 3 to 6 h of exposure, depending upon strain, inoculum and concentration. The PAE of sparfloxacin against all species tested ranged from 1.1 to 2.6 hours; the most notable PAE occurring with M. catarrhalis.


Asunto(s)
Antibacterianos/farmacología , Fluoroquinolonas , Bacterias Gramnegativas/efectos de los fármacos , Bacterias Grampositivas/efectos de los fármacos , Quinolonas/farmacología , Haemophilus influenzae/efectos de los fármacos , Humanos , Técnicas In Vitro , Klebsiella pneumoniae/efectos de los fármacos , Moraxella catarrhalis/efectos de los fármacos , Staphylococcus aureus/efectos de los fármacos , Streptococcus pneumoniae/efectos de los fármacos
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