Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 20 de 22
Filtrar
1.
Sci Rep ; 12(1): 7729, 2022 05 11.
Artigo em Inglês | MEDLINE | ID: mdl-35545693

RESUMO

A simple, fast, and accurate capillary zone electrophoresis method has been developed for the determination of ciprofloxacin and ofloxacin. This method uses liquid-liquid extraction. Therefore, it is characterized by a very simple procedure of sample preparation but at the same time satisfactory precision and accuracy. The extraction process of the same urine sample was repeated three times. The extraction protocol was performed each time for 15 min with 1 mL of dichloromethane and chloroform mixture in a 3:1 volume ratio. A 0.1 mol/L phosphate-borate buffer (pH 8.40) was selected as the background electrolyte. UV detection was performed at 288 nm. The separation was carried out at a voltage of 16 kV, at a temperature of 25 °C. Experimentally evaluated LOQ values for ciprofloxacin and ofloxacin were 0.2 nmol/mL urine and 0.05 nmol/mL urine, respectively. For both analytes the calibration curves exhibited linearity over the entire tested concentration range of 1-6 nmol/mL urine. The precision of the method did not exceed 15%, and the recovery was in the range of 85-115%. The developed and validated procedure was applied to analyze human urine for the content of ciprofloxacin and ofloxacin.


Assuntos
Ciprofloxacina , Ofloxacino , Boratos/análise , Ciprofloxacina/análise , Eletroforese Capilar/métodos , Humanos , Extração Líquido-Líquido , Ofloxacino/análise , Reprodutibilidade dos Testes
2.
Braz. J. Pharm. Sci. (Online) ; 55: e17105, 2019. tab, graf, ilus
Artigo em Inglês | LILACS | ID: biblio-1019532

RESUMO

The efficacy of conventional ocular formulations is limited by poor corneal retention and permeation, resulting in low ocular bioavailability. Mucoadhesive chitosan (CS)/ tripolyphosphatesodium (TPP) and chitosan (CS)/ tripolyphosphatesodium (TPP)-alginate (ALG) nanoparticles were investigated for the prolonged topical ophthalmic delivery of ofloxacin. A modified ionotropic gelation method was used to produce ofloxacin-loaded nanoreservoir systems. The ofloxacin-loaded CS/TPP and CS/TPP-ALG nanoparticles were characterized for particle size, morphology, zeta potential, encapsulation efficiency, subsequent release and corneal penetration study. The designed nanoparticles have a particle size from 113.8 nm to 509 nm and zeta potential from 16.2 mV to 40.3 mV and encapsulation efficiency values ranging from 19.7% to 33.1%. Nanoparticles revealed a release during the first hours, followed by a more gradual drug release. The ofloxacin-loading CS/TPP or CS/TPP-ALG NPs developed are pronounced penetration enhancing effect as compared to OFX solution (5-6.5 times). Thus, these nanoparticles have a strong potential for ocular drug delivery.


Assuntos
Ofloxacino/análise , Quitosana/análise , Nanopartículas/análise , Administração Oftálmica , Fenômenos Fisiológicos Oculares , Infecções Oculares/classificação , Cromatografia Líquida de Alta Pressão/métodos , Córnea
3.
Environ Sci Pollut Res Int ; 24(33): 25977-25985, 2017 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-28940003

RESUMO

The interaction of oil shale, as a widespread sedimentary rock, with common antibiotics ofloxacine, oxytetracycline, and ciprofloxacine was studied. The selected Moroccan deposit and its thermally treated forms were fully characterized from a chemical and structural point of view, indicating the prevalence of quartz as a mineral component together with aluminum- and iron-rich phase that are converted into Al-doped iron oxide phases upon heating. The presence of 4 wt% organics was also detected, which was removed at 550 °C without significant loss of specific surface area. The pseudo-second-order kinetic model and Langmuir equation were found the most adequate to reproduce the kinetics and isothermal sorption experiments. These analyses enlighten the contribution of the organic matter on antibiotic retention as well as the key role of hydrophobic interactions on the molecule-mineral surface interactions. Our results emphasize the possible contribution of raw oil shale in the accumulation of antibiotics in soils and suggest that thermally treated oil shell powders can constitute cheap mineral sorbents for environmental cleaning.


Assuntos
Antibacterianos/química , Recuperação e Remediação Ambiental/métodos , Minerais/química , Poluentes do Solo/química , Adsorção , Antibacterianos/análise , Ciprofloxacina/análise , Ciprofloxacina/química , Interações Hidrofóbicas e Hidrofílicas , Minerais/análise , Marrocos , Ofloxacino/análise , Ofloxacino/química , Oxitetraciclina/análise , Oxitetraciclina/química , Pós/análise , Pós/química , Poluentes do Solo/análise
4.
Anal Chim Acta ; 934: 239-51, 2016 Aug 31.
Artigo em Inglês | MEDLINE | ID: mdl-27506366

RESUMO

In order to assess the true impact of each single enantiomer of pharmacologically active compounds (PACs) in the environment, highly efficient, fast and sensitive analytical methods are needed. For the first time this paper focuses on the use of ultrahigh performance supercritical fluid based chromatography coupled to a triple quadrupole mass spectrometer to develop multi-residue enantioselective methods for chiral PACs in environmental matrices. This technique exploits the advantages of supercritical fluid chromatography, ultrahigh performance liquid chromatography and mass spectrometry. Two coated modified 2.5 µm-polysaccharide-based chiral stationary phases were investigated: an amylose tris-3,5-dimethylphenylcarbamate column and a cellulose tris-3-chloro-4-methylphenylcarbamate column. The effect of different chromatographic variables on chiral recognition is highlighted. This novel approach resulted in the baseline resolution of 13 enantiomers PACs (aminorex, carprofen, chloramphenicol, 3-N-dechloroethylifosfamide, flurbiprofen, 2-hydroxyibuprofen, ifosfamide, imazalil, naproxen, ofloxacin, omeprazole, praziquantel and tetramisole) and partial resolution of 2 enantiomers PACs (ibuprofen and indoprofen) under fast-gradient conditions (<10 min analysis time). The overall performance of the methods was satisfactory. The applicability of the methods was tested on influent and effluent wastewater samples. To the best of our knowledge, this is the first feasibility study on the simultaneous separation of chemically diverse chiral PACs in environmental matrices using ultrahigh performance supercritical fluid based chromatography coupled with tandem mass spectrometry.


Assuntos
Cromatografia com Fluido Supercrítico , Poluentes Químicos da Água/análise , Aminorex/análise , Carbazóis/análise , Cloranfenicol/análise , Cromatografia Líquida de Alta Pressão , Flurbiprofeno/análise , Humanos , Ibuprofeno/análise , Ifosfamida/análise , Imidazóis/análise , Indoprofen/análise , Estrutura Molecular , Naproxeno/análise , Ofloxacino/análise , Omeprazol/análise , Praziquantel/análise , Extração em Fase Sólida , Estereoisomerismo , Espectrometria de Massas em Tandem , Tetramizol/análise
5.
Environ Technol ; 37(16): 2003-15, 2016 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-26752017

RESUMO

A new catalytic wet peroxide oxidation of ofloxacin antibiotic is presented in this work. The removal was achieved using a biodegradable sodium alginate-iron material. Several parameters were studied such as iron content, drying duration of the catalytic support, temperature, solid amount and initial drug concentration. The process showed a strong oxidative ability; at optimum conditions, a nearly complete removal of the drug (around 98%) has been reached after three h of treatment. A relatively low decrease of support activity (around 10%) has been observed after three successive oxidation runs and a low iron leaching has been detected (1.2% of the incorporated quantity). The removal of the substrate has been also examined in the absence of hydrogen peroxide in order to discriminate between the contributions of simple adsorption and oxidation processes in the drug disappearance. We also discussed the influence of the studied experimental parameters on the removal kinetic.


Assuntos
Alginatos/química , Peróxido de Hidrogênio/química , Ferro/química , Ofloxacino/química , Poluentes Químicos da Água/química , Ácido Glucurônico/química , Ácidos Hexurônicos/química , Ofloxacino/análise , Oxirredução , Poluentes Químicos da Água/análise
6.
Anal Chim Acta ; 853: 668-675, 2015 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-25467516

RESUMO

A kind of new temperature sensitive molecularly imprinted polymer (MIP) with ofloxacin (OFL) as template was prepared for the coating of solid phase microextraction (SPME). Dopamine was self-polymerized on stainless steel fiber (SSF) as the SPME support followed by silanization. Then MIP was synthesized as SPME coating on the modified SSF in a capillary, with N-isopropyl acrylamide as temperature sensitive monomer and methacrylic acid as functional monomer. The synthesis could be well repeated with multiple capillaries putting in the same reaction solution. The obtained MIP fiber was evaluated in detail with different techniques and various adsorption experiments. At last the MIP fiber was used to extract the OFL in milk. Satisfied recoveries between 89.7 and 103.4% were obtained with the limit of quantification (LOQLC) of 0.04 µg mL(-1) by the method of SPME coupled with high performance of liquid chromatography (HPLC).


Assuntos
Cromatografia Líquida de Alta Pressão , Impressão Molecular , Ofloxacino/análise , Polímeros/química , Aço Inoxidável/química , Adsorção , Animais , Leite/química , Ofloxacino/isolamento & purificação , Microextração em Fase Sólida , Temperatura
7.
J Environ Manage ; 127: 114-24, 2013 Sep 30.
Artigo em Inglês | MEDLINE | ID: mdl-23685272

RESUMO

Aqueous solutions of four pharmaceutical compounds, belonging to the group of emergent contaminants of water: atenolol (ATL), hydrochlorothiazide (HCT), ofloxacin (OFX) and trimethoprim (TMP), have been treated with different oxidation systems, mainly, photocatalytic oxidation, ozonation and photocatalytic ozonation. TiO2 has been used as semiconductor for photocatalytic reactions both in the presence of air, oxygen or ozone-oxygen gas mixtures. Black light lamps mainly emitting at 365 nm were the source of radiation. In all cases, the influence of some variables (concentrations of semiconductor, ozone gas and pharmaceuticals and pH) on the removal of pharmaceuticals, total polyphenol content (TPC) and total organic carbon (TOC) was investigated. A discussion on the possible routes of pharmaceutical and intermediates (as TPC and TOC) elimination has been developed. Thus, OFX TiO2/UVA degradation mechanism seems to develop through the participation of non-hydroxyl free radical species. Furthermore, the presence of OFX inhibits the formation of hydroxyl radicals in the photocatalytic process. The most effective processes were those involving ozone that lead to complete disappearance of parent compounds in less than 30 min for initial pharmaceutical concentrations lower than 2.5 mg L(-1). In the ozonation systems, regardless of the pH and the presence of TiO2, pharmaceuticals are degraded through their direct reaction with ozone. Photocatalytic ozonation was the most efficient process for TPC and TOC removals (≥ 80% and ≥60% elimination after 2 h of treatment, respectively) as well as in terms of the ozone consumption efficiency (1, 5.5 and 4 mol of ozone consumed per mol of TOC mineralized, at pH 4, 7 and 9, respectively). Weakly acid conditions (pH 4) resulted to be the most convenient ones for TPC and TOC removal by photocatalytic ozonation. This was likely due to formation of hydroxyl radicals through the ozonide generated at these conditions.


Assuntos
Atenolol/química , Hidroclorotiazida/química , Ofloxacino/química , Ozônio/química , Trimetoprima/química , Poluentes Químicos da Água/química , Adsorção , Atenolol/análise , Recuperação e Remediação Ambiental/métodos , Hidroclorotiazida/análise , Concentração de Íons de Hidrogênio , Ofloxacino/análise , Oxirredução , Oxigênio/química , Processos Fotoquímicos , Semicondutores , Titânio/química , Trimetoprima/análise , Raios Ultravioleta , Poluentes Químicos da Água/análise
8.
Bioelectrochemistry ; 89: 42-9, 2013 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-23044173

RESUMO

A novel cysteic acid modified carbon paste electrode (cysteic acid/CPE) based on electrochemical oxidation of L-cysteine was developed to simultaneously determine ofloxacin and gatifloxacin in the presence of sodium dodecyl benzene sulfonate (SDBS). Fourier transform infrared spectra (FTIR) indicated that L-cysteine was oxidated to cysteic acid. Electrochemical impedance spectroscopy (EIS) and cyclic voltammograms (CV) indicated that cysteic acid was successfully modified on electrode. The large peak separation (116 mV) between ofloxacin and gatifloxacin was obtained on cysteic acid/CPE while only one oxidation peak was found on bare electrode. And the peak currents increased 5 times compared to bare electrode. Moreover, the current could be further enhanced in the presence of an anionic surfactant, sodium dodecyl benzene sulfonate. The differential pulse voltammograms (DPV) exhibited that the oxidation peak currents were linearly proportional to their concentrations in the range of 0.06-10 µM for ofloxacin and 0.02-200 µM for gatifloxacin, and the detection limits of ofloxacin and gatifloxacin were 0.02 µM and 0.01 µM (S/N=3), respectively. This proposed method was successfully applied to determine ofloxacin and gatifloxacin in pharmaceutical formulations and human serum samples.


Assuntos
Benzenossulfonatos/química , Ácido Cisteico/química , Eletroquímica/métodos , Fluoroquinolonas/análise , Fluoroquinolonas/química , Ofloxacino/análise , Ofloxacino/química , Carbono/química , Química Farmacêutica , Eletroquímica/instrumentação , Eletrodos , Fluoroquinolonas/sangue , Gatifloxacina , Humanos , Ofloxacino/sangue , Oxirredução , Propriedades de Superfície , Fatores de Tempo
9.
Environ Sci Pollut Res Int ; 19(5): 1392-404, 2012 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-22743989

RESUMO

BACKGROUND AND PURPOSE: Estrogenic compounds and antibiotic residues in environment are receiving significant attention because of their potential adverse effects on ecosystems and human health. The objectives of this study were to determine the occurrence and seasonal variability of eight kinds of estrogenic compounds and 14 antibiotics. The study developed an occurrence database of the estrogenic compounds and antibiotics in spatial and temporal scale in Jiulongjiang River, South China, to provide useful information for environmental management of this region. METHODS: Eight estrogenic compounds and 14 antibiotic compounds were detected in Jiulongjiang River from 19 sampling sites during high-flow and low-flow season in surface water. The samples were preconcentrated by solid-phase extraction for analysis. Eight estrogenic compounds were analyzed by gas chromatography mass spectrometry (Agilent 7890A-5975C), and antibiotics were determined by liquid chromatography-tandem mass spectrometry (LC-MS/MS) system (ABI 3200 Q TRAP). RESULTS: All target compounds could be detected, except 17α-ethynylestradiol, sulfamerazine, and ofloxacin. The median concentrations for seven estrogenic compounds ranged from 6.00 to 610.72 ng/L, with the detection frequency range of 16.00-100%. However, the detection frequencies of 13 antibiotics detected varied from 50% to 100%, with the median concentrations ranged from 0.89 to 117.97 ng/L. Seasonal variations were obvious for most estrogenic compounds in Jiulongjiang River, except for octylphenol and estriol. There were significant (P < 0.001) differences for three tetracyclines, sulfadiazine, and sulfamethoxazole between in low-flow season and in high-flow season. Besides, spatially considerable variations in the concentrations were observed for antibiotics, nonylphenol, octylphenol, and bisphenol A. CONCLUSION: The Jiulongjiang River water was more seriously contaminated by diethylstilbestrol, estrone, sulfamethazine, and tetracyclines. Higher overall concentration levels of estrogenic compounds and antibiotics were detected in low-flow water than those in high-flow water. The pollution of estrogenic compounds and antibiotics in Jiulongjiang River mainly came from municipal sewage and livestock breeding activities.


Assuntos
Antibacterianos/análise , Estrogênios/análise , Rios/química , Poluentes Químicos da Água/análise , Compostos Benzidrílicos , China , Água Doce/análise , Cromatografia Gasosa-Espectrometria de Massas , Ofloxacino/análise , Fenóis/análise , Estações do Ano , Esgotos , Extração em Fase Sólida , Sulfamerazina/análise , Tetraciclinas/análise , Qualidade da Água
10.
Toxicol Mech Methods ; 22(3): 225-30, 2012 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-22087570

RESUMO

Impurities in drug substances and drug products generally do not have beneficial effects and may impose a risk without associated benefit. Levofloxacin n-oxide is an impurity isolated from levofloxacin. However there is insufficient toxic information about levofloxacin n-oxide. This study investigates the genotoxicity of this impurity by in silico and in vitro methods. We used Derek, a commercial structure-activity relationship software package as an in silico tool. The results showed that there was a structural alert (quinolone-3-carboxylic acid or naphthyridine analogue) in this impurity. Then the mouse lymphoma assay (MLA) and chromosome aberration assay in Chinese hamster lung (CHL) cells were conducted in vitro. Both assays were conducted in the presence or absence of S-9 mix. The test impurity was not mutagenic in the test of MLA. While there was a statistically significant increase in the number of metaphase CHL cells with structural aberrations at the concentration of 1 mg/mL with S-9 mix, and the aberrations rate is 6.5%. It did not significantly increase the number of structural aberration in CHL cells in the presence (at other two doses) or absence of S-9 mix. Based on these assays, levofloxacin n-oxide could be controlled as a non-genotoxic impurity despite the DEREK alert for quinolone-3-carboxylic acid or naphthyridine analogue.


Assuntos
Aberrações Cromossômicas/induzido quimicamente , Simulação por Computador , Contaminação de Medicamentos , Levofloxacino , Linfoma/genética , Testes de Mutagenicidade , Mutação , Ofloxacino/toxicidade , Óxidos/toxicidade , Animais , Linhagem Celular Tumoral , Distribuição de Qui-Quadrado , Cricetinae , Camundongos , Estrutura Molecular , Ofloxacino/análise , Ofloxacino/química , Óxidos/análise , Óxidos/química , Medição de Risco , Software , Relação Estrutura-Atividade
11.
Braz. j. pharm. sci ; 48(2): 217-225, Apr.-June 2012. graf, tab
Artigo em Inglês | LILACS | ID: lil-643014

RESUMO

Bitter taste of ofloxacin, a broad spectrum bactericidal agent, is masked and orally disintegrating tablets were formulated. The bitter taste is masked by forming complex between drug and weak cation exchange resins, Tulsion 335 and Indion 204. Effect of pH and drug:resin ratio on the drug loading was studied. Maximum drug loading was observed at pH 6. Ratio of 1:2 of drug:resin masked almost complete bitterness of ofloxacin. Formation of complexes was confirmed by IR spectroscopy. Physical characterization of taste masked complexes was carried out. Present work envisages the taste masking of ofloxacin and development of orally disintegrating tablets. The effect of pH and resin quantities on drug loading were studied to find the optimum conditions of drug loading for complete taste masking. Effect of superdisintegrants like sodium starch glycolate, croscarmellose sodium and polyplasdone XL at varying level on physical parameters of compressed tablets was also assessed. The formulations containing 5 % w/w polyplasdone XL showed about 90 % of drug release within 5 minutes. No significant differences were observed in the physical parameters of resinates as well as tablets prepared from Tulsion 335 and Indion 204.


O gosto amargo de ofloxacina, agente bactericida de largo espectro, é mascarado e formularam-se comprimidos dispersíveis. O sabor amargo é mascarado pela formação de complexo entre o fármaco e resinas de troca catiônica fraca, Tulsion 335 e Indion 204. Efeito do pH e da proporção fármaco: resina sobre a carga de fármaco foi estudada. Carga de fármaco máxima foi observada em pH 6. Proporção 1:2 do fármaco: resina mascarou quase completamente o gosto amargo de ofloxacina. A formação de complexos foi confirmada por espectroscopia no IV. Caracterização física dos complexos de sabor mascarado foi realizada. O presente trabalho preconiza o mascaramento do gosto de ofloxacina e desenvolvimento decomprimidos por via oral, se desintegrando. O efeito do pH e da resina quantidades de carga de fármaco foram estudadas paraencontrar as condições óptimas de carga de fármaco para dissimulação do saborcompleto. Efeito da superdisintegrants como amido glicolato de sódio, croscarmelose sódica e Polyplasdone XL em diferentes níveis de parâmetros físicos de comprimidos também avaliados foi avaliada. As formulações contendo 5 %w/w Polyplasdone XL mostraram cerca de 90% de libertação do fármaco no prazo de 5 minutos. Não foram observadas diferenças significativas nos parâmetros físicos de resinatosbem como comprimidos preparados a partir de Tulsion 335 e Indion 204.


Assuntos
Comprimidos/farmacocinética , Ofloxacino/análise , Resinas de Troca Iônica/farmacocinética , Fator de Crescimento de Hepatócito/classificação
12.
J Ocul Pharmacol Ther ; 27(3): 247-50, 2011 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-21548793

RESUMO

PURPOSE: We investigated whether an optimized combination of oral and topical levofloxacin would lead to higher levofloxacin concentrations in aqueous humor. METHODS: Fifteen patients with cataracts in both eyes began topical treatment at 1 week before the first surgery and oral treatment at 1 day before the first surgery. On the day of surgery, they received oral and topical levofloxacin at 4 h and 1 h before surgery, respectively. Two days after the first operation, we performed cataract surgery on the second eye with the same drug administration protocol. RESULTS: Postsurgery concentrations of levofloxacin in the aqueous humor of the first and second eyes were 2.87±0.89 µg/mL (mean±standard deviation, n=15) and 3.76±1.32 µg/mL, respectively; the levofloxacin level in the second eye was significantly higher than that in the first eye (P=0.0085). CONCLUSIONS: Our protocol to achieve high aqueous humor concentrations of levofloxacin may be favorable in preventing endophthalmitis after eye surgery.


Assuntos
Antibacterianos/administração & dosagem , Levofloxacino , Ofloxacino/administração & dosagem , Corpo Vítreo/química , Administração Oral , Idoso , Idoso de 80 Anos ou mais , Antibacterianos/análise , Antibacterianos/farmacocinética , Extração de Catarata , Cromatografia Líquida de Alta Pressão , Endoftalmite/prevenção & controle , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Ofloxacino/análise , Ofloxacino/farmacocinética , Soluções Oftálmicas , Complicações Pós-Operatórias/prevenção & controle , Reprodutibilidade dos Testes , Distribuição Tecidual
13.
Environ Sci Technol ; 44(13): 4924-9, 2010 Jul 01.
Artigo em Inglês | MEDLINE | ID: mdl-20521844

RESUMO

Chlorination of wastewater can form genotoxic, mutagenic, and/or carcinogenic disinfection byproduct (DBPs). In this study, the effect of bromide on genotoxicity in secondary effluent of a municipal wastewater treatment plant during chlorination was evaluated by the SOS/umu test. The presence of bromide notably decreased the genotoxicity in secondary effluent during chlorination, especially under conditions of high ammonia concentration. Bromide significantly decreased the concentration of ofloxacin, a genotoxic chemical in secondary effluent, during chlorination with high concentration of ammonia, while genotoxic DBPs formation of humic acid and aromatic amino acids associated with bromide limitedly contributed to the changes of genotoxicity in secondary effluent under the conditions of this study. By fractionating dissolved organic matter (DOM) in the secondary effluent into different fractions, the fractions containing hydrophilic substances (HIS) and hydrophobic acids (HOA) contributed to the decrease in genotoxicity induced by bromide. Chlorination of HOA without bromide increased genotoxicity, while the addition of bromide decreased genotoxicity.


Assuntos
Brometos/análise , Brometos/química , Monitoramento Ambiental/métodos , Poluentes Químicos da Água/análise , Purificação da Água/métodos , Cidades , Desinfetantes/análise , Relação Dose-Resposta a Droga , Halogenação , Mutagênicos , Ofloxacino/análise
14.
Anal Sci ; 25(1): 125-8, 2009 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-19139586

RESUMO

A simple and sensitive spectrophotometric method for the determination of quinolone antibiotics was established based on an association complex formation with aluminum(III) and erythrosin. In the determination of ofloxacin as a quinolone antibiotic, Beer's law is obeyed in the range of 0.1 - 3.2 microg ml(-1), with an effective molar absorptivity at 555 nm and the relative standard deviation being 1.2 x 10(5) L mol(-1) cm(-1) and 0.9% (n = 6). This method was successfully applied to the assay of quinolone antibiotics in pharmaceutical preparations.


Assuntos
Antibacterianos/análise , Quinolinas/análise , Alumínio/química , Eritrosina/química , Ofloxacino/análise , Análise Espectral
15.
Curr Med Res Opin ; 23(12): 2955-60, 2007 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-17939882

RESUMO

OBJECTIVE: To compare corneal tissue and aqueous humor concentrations of levofloxacin 1.5% and gatifloxacin 0.3% ophthalmic solutions after topical dosing. RESEARCH DESIGN AND METHODS: This was a randomized, observer-masked, parallel-group, multicenter study. Fifty-nine subjects undergoing planned penetrating keratoplasty were randomly assigned to receive either levofloxacin 1.5% or gatifloxacin 0.3% as follows: one drop 15 min prior to surgery and a second drop 10 min before surgery. Corneal button and aqueous humor samples were collected during surgery and immediately stored at -70 degrees C. Levofloxacin and gatifloxacin concentrations were determined by high-pressure liquid chromatography and mass spectrometry. MAIN OUTCOME MEASURES: Corneal tissue and aqueous humor concentrations of levofloxacin and gatifloxacin. RESULTS: Levofloxacin achieved statistically significantly higher concentrations in both corneal tissue and aqueous humor compared to gatifloxacin in patients undergoing penetrating keratoplasty. In corneal tissue the mean concentration of levofloxacin was 64.8 +/- 123.4 mug/g vs. 7.0 +/- 9.3 mug/g for gatifloxacin (p < 0.0001). Mean aqueous humor concentration of levofloxacin was 0.976 +/- 2.215 mug/mL vs. 0.0523 +/- 0.143 mug/mL for gatifloxacin (p = 0.0002). CONCLUSIONS: The high concentrations of levofloxacin achievable in corneal tissue with topical dosing suggest that levofloxacin 1.5% should be a useful agent in the treatment of ocular bacterial infections. However, the corneal concentrations achieved in this study may not be representative of concentrations in patients using less frequent dosing.


Assuntos
Anti-Infecciosos/farmacocinética , Córnea/metabolismo , Transplante de Córnea , Fluoroquinolonas/farmacocinética , Levofloxacino , Ofloxacino/farmacocinética , Adulto , Idoso , Idoso de 80 Anos ou mais , Anti-Infecciosos/administração & dosagem , Anti-Infecciosos/análise , Córnea/química , Feminino , Fluoroquinolonas/administração & dosagem , Fluoroquinolonas/análise , Gatifloxacina , Humanos , Masculino , Pessoa de Meia-Idade , Ofloxacino/administração & dosagem , Ofloxacino/análise , Soluções Oftálmicas
16.
J Biomed Mater Res B Appl Biomater ; 83(2): 589-95, 2007 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-17410574

RESUMO

We developed a local drug-release system consisting of two biodegradable polymers, poly(sebacic anhydride) (PSA) and poly-D,L-lactide (PLA), for the treatment of chronic osteomyelitis. PSA and PLA were dissolved and blended at different ratios in tetrahydrofuran. Ofloxacin was loaded with an 8:1 weight ratio of the blend to the drug. The ofloxacin-containing beads of the PSA/PLA blend were made by preheating and compressing them in a mold. The in vitro drug release showed that changing the ratio between the two polymers caused the effective ofloxacin-release duration to vary from 6 to 68 days. The ofloxacin-containing beads with 10% PSA and 90% PLA produced an inhibition zone for the bacteria Staphylococcus aureus, Escherichia coli, and Pseudomonas aeruginosa within 89 days of the experiment. The in vivo drug release of the beads in rabbits demonstrated that the average ofloxacin concentration in the local bone was 20.1 +/- 10.3 microg/g, while that in the plasma was 35.6 +/- 18.8 ng/mL, within 8 weeks. Roentgenography, bacterial cultures, and histological examinations showed that the local release of ofloxacin by the beads could cure osteomyelitis in rabbits. Our findings suggested that using PSA/PLA blends with different ratios as carriers for antibiotics might be useful in the treatment of chronic osteomyelitis and in the prophylaxis of bone infection.


Assuntos
Antibacterianos/administração & dosagem , Ofloxacino/administração & dosagem , Osteomielite/tratamento farmacológico , Animais , Antibacterianos/análise , Preparações de Ação Retardada/química , Escherichia coli/efeitos dos fármacos , Ofloxacino/análise , Osteomielite/diagnóstico por imagem , Osteomielite/microbiologia , Polianidridos/química , Poliésteres/química , Pseudomonas aeruginosa/efeitos dos fármacos , Coelhos , Radiografia , Staphylococcus aureus/efeitos dos fármacos
17.
Int J Antimicrob Agents ; 29(1): 44-50, 2007 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-17189094

RESUMO

Recent observations indicate that pharmacokinetics of beta-lactam antibiotics in the lung can be predicted by the use of concentration versus time profiles in peripheral soft tissues. If this observation is transferred to other classes of antimicrobials, measurement of antimicrobial concentrations in peripheral tissues would enable prediction of the pharmacokinetics of antimicrobials at the site of the respiratory tract infection. We set out to test the hypothesis that concentrations of the fluoroquinolone levofloxacin in the respiratory tract can be predicted on the basis of knowledge of its pharmacokinetics in peripheral soft tissues. After administration of a single intravenous dose of 500mg of levofloxacin, microdialysis was used to describe the concentration versus time profiles of levofloxacin in the interstitial space fluid of lung tissue of patients (n=5) undergoing elective lung surgery. These data were compared with the concentration versus time courses in the interstitial space fluid of skeletal muscle and subcutaneous adipose tissue of healthy volunteers (n=7). The median AUC(0-infinity) of free levofloxacin in lung (2267mg x min/L, 1980-2355) was about 2-fold and 1.5-fold lower compared with skeletal muscle (4381mg x min/L, range 1720-8195) and adipose tissue (3492mg x min/L, range 1323-6420) of healthy controls, respectively. Concentrations in the interstitial space fluid of the lung were descriptively lower compared with corresponding concentrations in peripheral soft tissues. This is in contrast to previous observations made for the class of beta-lactam antibiotics, and indicates that pharmacokinetics of levofloxacin derived from soft tissues may not be used uncritically for prediction of levofloxacin concentrations in the interstitium of the lung.


Assuntos
Líquido Extracelular/química , Levofloxacino , Pulmão/metabolismo , Microdiálise , Ofloxacino/farmacocinética , Tecido Adiposo Branco/química , Tecido Adiposo Branco/metabolismo , Adulto , Idoso , Antibacterianos/administração & dosagem , Antibacterianos/farmacocinética , Área Sob a Curva , Feminino , Humanos , Infusões Intravenosas , Pulmão/química , Pulmão/cirurgia , Masculino , Pessoa de Meia-Idade , Músculo Esquelético/química , Músculo Esquelético/metabolismo , Ofloxacino/análise , Ofloxacino/sangue , Projetos Piloto , Distribuição Tecidual
18.
Anal Biochem ; 353(1): 30-6, 2006 Jun 01.
Artigo em Inglês | MEDLINE | ID: mdl-16620758

RESUMO

Information on comparing the penetration of ofloxacin and moxifloxacin in the human eye is unavailable, although these two antibiotics are commonly used in ophthalmic surgery. There is a need for a rapid, reliable, and sensitive methodology for their determination in ocular fluids. We developed a robust HPLC procedure with fluorescence detection for simultaneous analysis of ofloxacin and moxifloxacin in human and rabbit aqueous and vitreous samples. The linearity of the method ranged from 10 ng/ml to 100 microg/ml with r(2) > 0.996. Most inter- and intrabatch imprecision was about 5% (range 1.6-7.6%), recoveries between 95 and 104%, and accuracies between 93 and 104% at 0.1 and 1 microg/ml. The detection limits of both compounds were 10 ng/ml (0.028 nmol/ml for ofloxacin and 0.023 nmol/ml for moxifloxacin). No sample treatment was necessary for aqueous humor and only acetonitrile precipitation was required for vitreous humor. The chromatographic time was short, 22 min. We applied this method to study penetrations of ofloxacin and moxifloxacin in aqueous and vitreous humors of human and rabbits. There was no significant difference of penetration between the two antibiotics into aqueous and vitreous but ofloxacin was found at significantly higher concentrations in aqueous than in vitreous. We also detected contralateral transfer of the antibiotics in rabbit eyes.


Assuntos
Antibacterianos/análise , Humor Aquoso/química , Compostos Aza/análise , Ofloxacino/análise , Quinolinas/análise , Corpo Vítreo/química , Animais , Cromatografia Líquida de Alta Pressão/métodos , Fluorescência , Fluoroquinolonas , Humanos , Moxifloxacina , Coelhos
19.
Am J Kidney Dis ; 47(1): e9-13, 2006 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-16377378

RESUMO

Autosomal dominant polycystic kidney disease (ADPKD) is a common inherited disorder often complicated by cyst infection. Treatment becomes particularly challenging when the culprit organism is resistant to antibiotics known to sufficiently penetrate cysts. We present the case of a patient with ADPKD and suspected cyst infection caused by group B streptococcus who was treated successfully with levofloxacin and ampicillin. Although data support excellent cyst penetration with ciprofloxacin, its gram-positive antimicrobial activity is marginal. The newer quinolones have added gram-positive activity, but little is known about cyst penetration by these antibiotics. We simultaneously measured cyst and serum levels of levofloxacin and ampicillin and found levofloxacin to penetrate cysts well. Therefore, levofloxacin may be useful in the management of renal cyst infection, particularly for the treatment of gram-positive organisms.


Assuntos
Antibacterianos/farmacocinética , Levofloxacino , Ofloxacino/farmacocinética , Rim Policístico Autossômico Dominante/complicações , Pielonefrite/tratamento farmacológico , Infecções Estreptocócicas/tratamento farmacológico , Streptococcus agalactiae , Adulto , Ampicilina/análise , Ampicilina/farmacocinética , Ampicilina/uso terapêutico , Antibacterianos/análise , Antibacterianos/uso terapêutico , Disponibilidade Biológica , Quimioterapia Combinada , Feminino , Humanos , Ofloxacino/análise , Ofloxacino/uso terapêutico , Pielonefrite/complicações , Infecções Estreptocócicas/complicações
20.
J Chromatogr B Biomed Sci Appl ; 700(1-2): 147-53, 1997 Oct 24.
Artigo em Inglês | MEDLINE | ID: mdl-9390724

RESUMO

Cefotaxime, given intravenously, is currently used as a broad-spectrum antibiotic for prophylaxis of intra- and postoperative infections in ocular lens surgery. A proposed therapeutic and economic alternative is the use of orally active fluoroquinolone ofloxacine as prophylactic agent. A HPLC method was developed for determination of both antibiotics in ocular aqueous humor and plasma in order to optimize dosage for safe surpassing minimal inhibitory concentration in the humor compartment. For plasma determinations a solid-phase extraction procedure was used with ciprofloxacine as internal standard. Detection limits for direct HPLC-analysis of ocular aqueous humor was 0.08 microg/ml for all compounds, whereas in plasma 0.31 microg/ml could be determined after solid-phase extraction.


Assuntos
Antibacterianos/sangue , Humor Aquoso/química , Cefotaxima/análogos & derivados , Cefotaxima/sangue , Ciprofloxacina/sangue , Ofloxacino/sangue , Antibacterianos/análise , Antibacterianos/uso terapêutico , Antibioticoprofilaxia , Cefotaxima/análise , Cefotaxima/uso terapêutico , Cromatografia Líquida de Alta Pressão , Ciprofloxacina/análise , Humanos , Cristalino/cirurgia , Ofloxacino/análise , Ofloxacino/uso terapêutico
SELEÇÃO DE REFERÊNCIAS
DETALHE DA PESQUISA