RESUMO
Background Probiotics are live microbial organisms that provide benefit to the host while co-habitating in the gastrointestinal tract. Probiotics are safe, available over the counter, and have clinical benefit by reducing the number of antibiotic-associated diarrhea days. Prescriptions from providers and direct consumer demand of probiotics appear to be on the rise. Several recent animal studies have demonstrated that probiotics may have significant effect on absorption of co-administered drugs. However, to date, most probiotic-drug interaction studies in animal models have been limited to bacterial probiotics and nonantibiotic drugs. Methods We performed a traditional pharmacokinetic mouse study examining the interactions between a common commercially available yeast probiotic, Saccharomyces boulardii CNCM I-745 (Florastor®) and an orally administered amoxicillin. Results We showed that there were no significant differences in pharmacokinetic parameters (half-life, area under the curve, peak concentrations, time to reach maximum concentration, elimination rate constant) of amoxicillin between the probiotic treated and untreated control groups. Conclusions Altogether, our findings suggest that coadministration or concurrent use of S. boulardii probiotic and amoxicillin would not likely alter the efficacy of amoxicillin therapy.
Assuntos
Amoxicilina/farmacocinética , Antibacterianos/farmacocinética , Probióticos/administração & dosagem , Saccharomyces boulardii/química , Administração Oral , Amoxicilina/administração & dosagem , Amoxicilina/análise , Animais , Antibacterianos/administração & dosagem , Antibacterianos/análise , Suplementos Nutricionais , Fígado/química , Fígado/metabolismo , Masculino , Camundongos , Camundongos Endogâmicos ICRRESUMO
The impact of electrolytes on the adsorption of emerging pollutants: pharmaceuticals onto layered materials: a raw clay mineral and its nonionic and cationic organoclay derivatives was studied. The selected pharmaceuticals: amoxicillin, norfloxacin, sulfamethoxazole, metoprolol, carbamazepine, and trimethoprim show different electric charges: zwitterionic, anionic, cationic and neutral and hydrophobic character (different LogP). Without any salts, the set of complementary data obtained by UV and infrared spectroscopies, X-ray diffraction points out the importance of the electric charge which represents a key parameter in both the spontaneity and feasibility of the adsorption. In contrast, the hydrophobicity of the analytes plays a minor role but determines the magnitude of the adsorbed amount of pharmaceuticals onto organoclays. With a dual hydrophilic and hydrophobic behavior, nonionic organoclay appears to be the most polyvalent material for the removal of the pharmaceuticals. In the presence of electrolytes (NaCl at a concentration of 1â¯×â¯10-2â¯molâ¯L-1), both nonionic and cationic organoclays show a decrease of their efficiencies, whereas the adsorption is particularly enhanced for Na-Mt except for the cationic species (trimethoprim and metoprolol). Thus, in realistic experimental conditions close to those of natural effluents, raw clay mineral appears as the most appropriate sorbent for the studied pharmaceuticals while it raises the question of the usefulness of organoclays in water remediation strategy.
Assuntos
Eletrólitos/química , Recuperação e Remediação Ambiental/métodos , Preparações Farmacêuticas/análise , Poluentes do Solo/análise , Solo/química , Poluentes Químicos da Água/análise , Adsorção , Amoxicilina/análise , Amoxicilina/química , Carbamazepina/análise , Carbamazepina/química , Cátions/análise , Interações Hidrofóbicas e Hidrofílicas , Metoprolol/análise , Metoprolol/química , Norfloxacino/análise , Norfloxacino/química , Preparações Farmacêuticas/química , Poluentes do Solo/química , Sulfametoxazol/análise , Sulfametoxazol/química , Trimetoprima/análise , Trimetoprima/química , Água/química , Poluentes Químicos da Água/química , Difração de Raios XRESUMO
While treatment of serious infectious diseases may require high-dose amoxicillin, continuous infusion may be limited by lack of knowledge regarding the chemical stability of the drug. Therefore, we have performed a comprehensive study so as to determine the chemical stability of high-dose amoxicillin solutions conducive to safe and effective continuous intravenous administration using portable elastomeric pumps. First, amoxicillin solubility in water was assessed within the range of 25 to 300 mg/mL. Then, amoxicillin solutions were prepared at different concentrations (25, 50, 125, 250 mg/mL) and stored in different conditions (5±2°C, 25±1°C, 30±1°C and 37±1°C) to investigate the influence of concentration and temperature on the chemical stability of amoxicillin. Finally, its stability was assessed under optimized conditions using a fully validated HPLC-UV stability-indicating method. Degradation products of amoxicillin were investigated by accurate mass determination using high-resolution mass spectrometry. Amoxicillin displayed limited water solubility requiring reconstitution at concentrations below or equal to 150 mg/mL. Amoxicillin degradation were time, temperature as well as concentration-dependent, resulting in short-term stability, in particular at high concentrations. Four degradation products of amoxicillin have been identified. Among them, amoxicilloic acid and diketopiperazine amoxicillin are at risk of allergic reaction and may accumulate in the patient. Optimized conditions allowing for continuous infusion of high-dose amoxicillin has been determined: amoxicillin should be reconstituted at 25 mg/mL and stored up to 12 hours at room temperature (22 ± 4°C) or up to 24 hours between 4 and 8°C.
Assuntos
Amoxicilina/química , Antibacterianos/química , Estabilidade de Medicamentos , Elastômeros , Bombas de Infusão , Amoxicilina/administração & dosagem , Amoxicilina/efeitos adversos , Amoxicilina/análise , Antibacterianos/administração & dosagem , Antibacterianos/efeitos adversos , Antibacterianos/análise , Infecções Bacterianas/tratamento farmacológico , Química Farmacêutica , Relação Dose-Resposta a Droga , Humanos , Infusões Intravenosas/instrumentação , Solubilidade , Temperatura , Fatores de TempoRESUMO
In the present work, we synthesized the carbon quantum dots (CQDs) by one step hydrothermal method using the dried beet powder as the carbon source without additional chemical reagents and functionalization. The as-prepared CQDs are quasi-spherical carbon nanoparticles with diameters of 4-8 nm as well as surface functional groups such as carboxyl and hydroxyl groups, and exhibit good water-solubility, biocompatibility, and strong fluorescence. It is confirmed that amoxicillin (AMO) could enhance the fluorescent intensity of CQDs, the I/I0 showed a linear correlation between the intensity of fluorescence and the concentration of AMO in a broad range. These superior properties render a potential application of the CQDs in biomedical.
Assuntos
Amoxicilina/análise , Beta vulgaris/química , Carbono/química , Pontos Quânticos/química , Fluorescência , Nanopartículas/química , Tamanho da PartículaRESUMO
The project studied the occurrence, fate, and seasonal variation of 14 antibiotics, from five wastewater treatment plants (WWTPs) in Shanghai. The results indicated that ofloxacin, sulfamethoxazole, and oxytetracycline were the predominant antibiotics, with maximum concentrations of 1208.20, 959.13, and 564.30 ng/L in influents, while 916.88, 106.60, and 337.81 ng/L in effluents, respectively. The level of antibiotics in WWTPs obviously varied with seasonal changes, and higher detectable frequencies and concentrations were found in winter. The daily mass loads per capita of amoxicillin, enrofloxacin, and oxytetracycline in the study were all higher than those in other regions/countries, such as Hong Kong, Australia, and Italy. The elimination of antibiotics through these WWTPs was incomplete, and a wide range of removal efficiencies during the different treatment process and seasons were observed (-500.56 to 100 % in winter and -124.24 to 94.21 % in summer). Sulfonamides were relatively easy to be removed in WWTPs and the ultraviolet (UV) process can effectively improve the removal efficiency. Risk assessment of antibiotics in effluents was estimated. Only AMOX's hazard quotient (HQ) was higher than 0.01. Even though the environmental risks in the study were estimated to be low, the potential negative effects on aquatic ecosystems should call our attention as continually discharge in the long term.
Assuntos
Antibacterianos/análise , Águas Residuárias/química , Poluentes Químicos da Água/análise , Purificação da Água/estatística & dados numéricos , Amoxicilina/análise , China , Enrofloxacina , Monitoramento Ambiental , Fluoroquinolonas/análise , Ofloxacino/análise , Medição de Risco , Estações do Ano , Eliminação de Resíduos LíquidosRESUMO
Microcystis aeruginosa was cultured with 0.05-5 mg L(-1) of phosphorus and exposed to 200-500 ng L(-1) of amoxicillin for seven days. Amoxicillin presented no significant effect (p>0.05) on the growth of M. aeruginosa at phosphorus levels of 0.05 and 0.2 mg L(-1), but stimulated algal growth as a hormesis effect at phosphorus levels of 1 and 5 mg L(-1). Phosphorus and amoxicillin affected the contents of chlorophyll-a, adenosine triphosphate (ATP) and malondialdehyde, the expression of psbA and rbcL, as well as the activities of adenosinetriphosphatase and glutathione S-transferase in similar manners, but regulated the production and release of microcystins and the activities of superoxide dismutase and peroxidase in different ways. Increased photosynthesis activity was related with the ATP consumption for the stress response to amoxicillin, and the stress response was enhanced as the phosphorus concentration increased. The biodegradation of amoxicillin by M. aeruginosa increased from 11.5% to 28.2% as the phosphorus concentration increased. Coexisting amoxicillin aggravated M. aeruginosa pollution by increasing cell density and concentration of microcystins, while M. aeruginosa alleviated amoxicillin pollution via biodegradation. The interactions between M. aeruginosa and amoxicillin were significantly regulated by phosphorus (p<0.05) and led to a complicated situation of combined pollution.
Assuntos
Amoxicilina/farmacologia , Microcystis/efeitos dos fármacos , Fósforo/análise , Fotossíntese/efeitos dos fármacos , Poluentes Químicos da Água/farmacologia , Amoxicilina/análise , Clorofila/metabolismo , Clorofila A , Monitoramento Ambiental , Expressão Gênica/efeitos dos fármacos , Microcystis/crescimento & desenvolvimento , Microcystis/metabolismo , Fotossíntese/genética , Microbiologia da Água , Poluentes Químicos da Água/análiseRESUMO
The kinetics and mechanism ofamoxicillin (AMO) degradation using a 1 x 1 molecular sieve-structured manganese oxide (MnO2) was studied. The presence of the buffer solution (i.e., NaHCO3, NaH2PO4 and KH2PO4) diminished AMO binding to MnO2, thus reducing AMO degradation in the pretest; therefore, all other experiments in this study were conducted without the addition of a buffer. Third-order rate constants, second-order on AMO and first-order on MnO2 increased with elevating pH level (2.81-7.23) from 0.54 to 9.17 M(-2) s(-1), and it decreased to 4.27 M(-2) s(-1) at pH 8.53 beyond the pk(a2) of AMO (7.3). The dissolution of the MnO2 suspension with and without AMO exhibited a similar trend; that is, Mn2+ concentration increased with decreasing pH. However, the dissolution of MnO2 with AMO was greater than that without AMO, except for the reaction occurring at pH 8.53, partially indicating that MnO2 acts as an oxidant in AMO degradation. The preliminary chromatogram data display different products with varying pH reaction s, implying that AMO elimination using this 1 x 1 molecular sieve-structured MnO2 is by adsorption as well as oxidative degradation. A complementary experiment indicates that the amount of oxidatively degraded AMO increases substantially from 65.5% at 4 h to 95% at 48 h, whereas the AMO adsorbed onto MnO2 decreases slightly from 4.5% at4 h to 2.4% at 48 h. The oxidative degradation accounted for more AMO removal than adsorption over the whole reaction course, indicating that the oxidative reaction of AMO on MnO2 dominated the AMO removal.
Assuntos
Amoxicilina/metabolismo , Antibacterianos/metabolismo , Compostos de Manganês/química , Óxidos/química , Poluentes Químicos da Água/metabolismo , Purificação da Água/métodos , Adsorção , Amoxicilina/análise , Antibacterianos/análise , Concentração de Íons de Hidrogênio , Cinética , Oxirredução , Poluentes Químicos da Água/análiseRESUMO
An outbreak-causing strain of Salmonella enterica serovar Typhimurium was exposed to groundwater with residual antibiotics for up to four weeks. Representative concentrations (0.05, 1, and 100 µg L(-1)) of amoxicillin, tetracycline, and a mixture of several other antibiotics (1 µg L(-1) each) were spiked into artificially prepared groundwater (AGW). Antibiotic susceptibility analysis and the virulence response of stressed Salmonella were determined on a weekly basis by using human epithelial cells (HEp2) and soil nematodes (C. elegans). Results have shown that Salmonella typhimurium remains viable for long periods of exposure to antibiotic-supplemented groundwater; however, they failed to cultivate as an indication of a viable but nonculturable state. Prolonged antibiotics exposure did not induce any changes in the antibiotic susceptibility profile of the S. typhimurium strain used in this study. S. typhimurium exposed to 0.05 and 1 µg L(-1) amoxicillin, and 1 µg L(-1) tetracycline showed hyper-virulent profiles in both in vitro and in vivo virulence assays with the HEp2 cells and C. elegans respectively, most evident following 2nd and 3rd weeks of exposure.
Assuntos
Antibacterianos/toxicidade , Farmacorresistência Bacteriana/fisiologia , Água Subterrânea/química , Salmonella typhimurium/efeitos dos fármacos , Poluentes Químicos da Água/toxicidade , Amoxicilina/análise , Amoxicilina/toxicidade , Antibacterianos/análise , Farmacorresistência Bacteriana/efeitos dos fármacos , Salmonella typhimurium/patogenicidade , Salmonella typhimurium/fisiologia , Tetraciclina/análise , Tetraciclina/toxicidade , Poluentes Químicos da Água/análiseRESUMO
This article presents some experience obtained by applying capillary gas chromatography coupled with thermal conductivity detection (GC/TCD) to the determination of water in substances for pharmaceutical use. This technique represents a useful, orthogonal tool complementary to water determination methods based on volumetric or coulometric titration. It can also represent an alternative technique when such titrations are not applicable. This article presents the preliminary results obtained in a number of case studies where a GC/TCD procedure was applied in comparison with pharmacopoeial methods to substances with different water contents.
Assuntos
Preparações Farmacêuticas/análise , Água/análise , Amoxicilina/análise , Antibacterianos/análise , Cromatografia Gasosa/métodos , Ciprofloxacina/análogos & derivados , Ciprofloxacina/análise , União Europeia , Indicadores e Reagentes , Solventes , Espectinomicina/análise , Teofilina/análise , Condutividade TérmicaRESUMO
Degradation kinetics and mineralization of an urban wastewater treatment plant effluent contaminated with a mixture of pharmaceutical compounds composed of amoxicillin (10 mg L(-1)), carbamazepine (5 mg L(-1)) and diclofenac (2.5 mg L(-1)) by TiO(2) photocatalysis were investigated. The photocatalytic effect was investigated using both spiked distilled water and actual wastewater solutions. The process efficiency was evaluated through UV absorbance and TOC measurements. A set of bioassays (Daphnia magna, Pseudokirchneriella subcapitata and Lepidium sativum) was performed to evaluate the potential toxicity of the oxidation intermediates. A pseudo-first order kinetic model was found to fit well the experimental data. The mineralization rate (TOC) of the wastewater contaminated with the pharmaceuticals was found to be really slow (t(1/2)=86.6 min) compared to that of the same pharmaceuticals spiked in distilled water (t(1/2)=46.5 min). The results from the toxicity tests of single pharmaceuticals, their mixture and the wastewater matrix spiked with the pharmaceuticals displayed a general accordance between the responses of the freshwater aquatic species (P. subscapitata>D. magna). In general the photocatalytic treatment did not completely reduce the toxicity under the investigated conditions (maximum catalyst loading and irradiation time 0.8 g TiO(2) L(-1) and 120 min respectively).
Assuntos
Indústria Farmacêutica , Resíduos Industriais/análise , Preparações Farmacêuticas/análise , Fotólise , Eliminação de Resíduos Líquidos/métodos , Poluentes Químicos da Água/análise , Amoxicilina/análise , Amoxicilina/toxicidade , Animais , Carbamazepina/análise , Carbamazepina/toxicidade , Clorófitas/efeitos dos fármacos , Cidades , Daphnia/efeitos dos fármacos , Diclofenaco/análise , Diclofenaco/toxicidade , Cinética , Lepidium sativum/efeitos dos fármacos , Preparações Farmacêuticas/química , Testes de Toxicidade , Água/química , Poluentes Químicos da Água/química , Poluentes Químicos da Água/toxicidadeAssuntos
Amoxicilina/uso terapêutico , Ampicilina/análogos & derivados , Bronquite/tratamento farmacológico , Amoxicilina/análise , Ensaios Clínicos como Assunto , DNA/análise , Avaliação Pré-Clínica de Medicamentos , Fibrinogênio/análise , Humanos , L-Lactato Desidrogenase/análise , Contagem de Leucócitos , Assistência de Longa Duração , Testes de Função Respiratória , Escarro/citologia , Escarro/microbiologiaRESUMO
A study of 11 patients suffering from acute exacerbations of chronic bronchial infection, all with purulent (Mp+++) sputum, showed that good penetration of amoxycillin into such sputum occurs. The levels of amoxycillin in sputum doubled proportionally with the oral dose, at least up to dosages of 2 g. High dosages or oral amoxycillin may therefore, be advantageous in the treatment of chronic bronchial infection. In a study of 30 chronic bronchitic patients, whose sputum varied in purulence from mucoid to purulent (Mp+++) the concentration of amoxycillin in sputum containing approximately 50% pus (Mp++) was significantly higher than that in any other degree of purulence. These results indicate that amoxycillin penetrates best into sputum at an intermediate degree of purulence.