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1.
Huan Jing Ke Xue ; 45(9): 5244-5253, 2024 Sep 08.
Artigo em Chinês | MEDLINE | ID: mdl-39323143

RESUMO

Taking Liangshui River, the reclaimed water-receiving river in Beijing, as the research area, the types, detection frequencies, and concentrations of 16 antibiotics in water and sediment were analyzed, and their temporal-spatial variation and occurrence characteristics were discussed. The results showed that nine and 13 target antibiotics were detected in the water and sediment of Liangshui River, with the antibiotic concentration ranges of ND-116.68 ng·L-1 and ND-235.42 ng·g-1, respectively. The main antibiotics in water were ofloxacin and clarithromycin, and the main antibiotic in sediment was ofloxacin. The total concentration of antibiotics in water and sediment showed a gradual decrease from the upstream to the downstream in the Liangshui River mainstream, and the concentration of antibiotics in tributaries was higher than that in the mainstream. The inflow of tributaries had an obvious impact on the antibiotic concentration in water for the Liangshui River but had little impact on its sediment. The total concentration of antibiotics in water and sediment during the dry season was generally higher than that during the wet season. The detected antibiotics with the highest concentration were quinolones in water during the wet season and macrolides in the dry season. Quinolones had the highest concentration in sediment in both seasons. The ecological risk assessment results showed that clarithromycin had a low risk in water in the dry season and sediment in both seasons, whereas the other antibiotics had no risk. The combined ecological risk and the most sensitive trophic level ecological risk assessment showed that all sampling sites had low risk or no risk, and the risk of the dry season was generally greater than that of the wet season. The risk values of some sampling points were close to the medium risk threshold during the dry season, which requires further attention.


Assuntos
Antibacterianos , Monitoramento Ambiental , Sedimentos Geológicos , Rios , Poluentes Químicos da Água , Rios/química , Poluentes Químicos da Água/análise , Antibacterianos/análise , Medição de Risco , Pequim , Sedimentos Geológicos/química , Ofloxacino/análise , China , Eliminação de Resíduos Líquidos/métodos , Claritromicina/análise
2.
Microbiol Spectr ; 9(3): e0192821, 2021 12 22.
Artigo em Inglês | MEDLINE | ID: mdl-34878300

RESUMO

The clinical importance of Mycobacterium abscessus (MABS) pulmonary disease has been increasing. However, there is still a lack of information about MIC distribution patterns and changes in clinical practice settings. The MIC results of rapidly growing mycobacteria isolated from 92 patients with nontuberculous mycobacterial pulmonary disease diagnosed from May 2019 to March 2021 were retrospectively analyzed. Most of the patients (86 patients; 93.5%) were infected with MABS; 46 with Mycobacterium abscessus subsp. abscessus (Mab), and 40 with Mycobacterium abscessus subsp. massiliense (Mma). Significant differences in susceptibility to clarithromycin (15.2% versus 80.0%, P < 0.001) and azithromycin (8.7% versus 62.5%, P < 0.001) were observed between Mab and Mma. Most isolates were susceptible to amikacin (80; 93.0%), and over half were susceptible to linezolid (48; 55.8%). Only one-quarter of isolates (22, 25.6%) were susceptible to imipenem, while more than half (56; 65.1%) had intermediate susceptibility. Fifty-one isolates (59.3%) had MIC values of less than 1 µg/mL for sitafloxacin, which were significantly higher than isolates for moxifloxacin (5; 5.8%), especially in Mab. Sixty-five (75.6%) isolates had MICs of less than 0.5 µg/mL to clofazimine. Two patients showed obvious MIC result changes: from susceptible to resistant to clarithromycin and from resistant to susceptible to amikacin and imipenem. In conclusion, MABS isolates were relatively susceptible to amikacin and linezolid, and clarithromycin and azithromycin were especially effective against Mma. In addition, sitafloxacin and clofazimine had low MICs and might be effective treatment agents. IMPORTANCE The MICs of isolates from 86 patients with Mycobacterium abscessus (MABS); 46 with Mycobacterium abscessus subsp. abscessus (Mab), and 40 with Mycobacterium abscessus subsp. massiliense (Mma) were retrospectively analyzed. The main findings are as follows: (i) Mma were significantly more susceptible to clarithromycin and azithromycin than Mab, and both subspecies tended to be more susceptible to clarithromycin than azithromycin. (ii) Most isolates were susceptible to amikacin (93.0%), and over half to linezolid (55.8%). (iii) Fifty-one isolates (59.3%) had MIC values of less than 1 µg/mL for sitafloxacin, and 65 (75.6%) had less than 0.5 µg/mL for clofazimine, which seems worth clinical investigating. (iv) Among nine cases analyzed chronological changes, only two patients showed obvious MIC result changes even after the long-term multidrug treatment. The present study revealed MICs of MABS clinical isolates before and after treatment in clinical settings, which could help develop future MABS treatments strategies.


Assuntos
Antibacterianos/uso terapêutico , Pneumopatias/tratamento farmacológico , Infecções por Mycobacterium não Tuberculosas/tratamento farmacológico , Mycobacterium abscessus/efeitos dos fármacos , Idoso , Antibacterianos/análise , Azitromicina/análise , Azitromicina/uso terapêutico , Claritromicina/análise , Claritromicina/uso terapêutico , Feminino , Humanos , Pneumopatias/microbiologia , Masculino , Testes de Sensibilidade Microbiana , Pessoa de Meia-Idade , Infecções por Mycobacterium não Tuberculosas/microbiologia , Mycobacterium abscessus/genética , Mycobacterium abscessus/isolamento & purificação , Mycobacterium abscessus/fisiologia , Estudos Retrospectivos
3.
J Pharm Biomed Anal ; 189: 113450, 2020 Sep 10.
Artigo em Inglês | MEDLINE | ID: mdl-32693204

RESUMO

A lateral flow immunoassay (LFIA) using latex particles labeled with antibody to BSA-clarithromycin (CLA) was developed for the rapid simultaneous group determination of six macrolide antibiotics. Optimization of antigen spotting on the membrane and latex probe loading allowed improving visual detectability (vLOD) 100 times, which was 1, 1, 10, 10, 50, and 1000 ng/mL for CLA, roxithromycin, erythromycin, dirithromycin, azithromycin, and oleandomycin in buffer, respectively. The calculated limits of instrumental detection (cLOD) were respectively 0.12, 0.15, 1.4, 2.1, 2.4, and 3.3 ng/mL. To avoid a strong influence of breast milk of a very diverse and variable composition, a sample pretreatment is proposed. The six macrolides mentioned can be visually detected in breast milk after 20 min pretreatment at concentrations of 10-1000 ng/mL or instrumentally with cLOD of 4.0, 2.5, 30, 42, 42 and 180 ng/mL. The recovery rate from the spiked samples carried out using a strip scanner device ranged from 71 % to 110 %, and precision expressed as relative standard deviation was between 3-14 %. The described rapid on-site diagnostic assay format can be useful for monitoring the content of antibiotics in breast milk during macrolide treatment to ensure safe breastfeeding of infants.


Assuntos
Macrolídeos , Leite Humano , Antibacterianos/análise , Claritromicina/análise , Humanos , Imunoensaio , Microesferas , Leite Humano/química
4.
Molecules ; 25(6)2020 Mar 24.
Artigo em Inglês | MEDLINE | ID: mdl-32213976

RESUMO

In this study, a screening of 26 selected antimicrobials using liquid chromatography coupled to a tandem mass spectrometry method in two Polish wastewater treatment plants and their receiving surface waters was provided. The highest average concentrations of metronidazole (7400 ng/L), ciprofloxacin (4300 ng/L), vancomycin (3200 ng/L), and sulfamethoxazole (3000 ng/L) were observed in influent of WWTP2. Ciprofloxacin and sulfamethoxazole were the most dominant antimicrobials in influent and effluent of both WWTPs. In the sludge samples the highest mean concentrations were found for ciprofloxacin (up to 28 µg/g) and norfloxacin (up to 5.3 µg/g). The removal efficiency of tested antimicrobials was found to be more than 50% for both WWTPs. However, the presence of antimicrobials influenced their concentrations in the receiving waters. The highest antimicrobial resistance risk was estimated in influent of WWTPs for azithromycin, ciprofloxacin, clarithromycin, metronidazole, and trimethoprim and in the sludge samples for the following antimicrobials: azithromycin, ciprofloxacin, clarithromycin, norfloxacin, trimethoprim, ofloxacin, and tetracycline. The high environmental risk for exposure to azithromycin, clarithromycin, and sulfamethoxazole to both cyanobacteria and eukaryotic species in effluents and/or receiving water was noted. Following the obtained results, we suggest extending the watch list of the Water Framework Directive for Union-wide monitoring with sulfamethoxazole.


Assuntos
Águas Residuárias/análise , Poluentes Químicos da Água/análise , Anti-Infecciosos/análise , Azitromicina/análise , Cromatografia Líquida , Ciprofloxacina/análise , Claritromicina/análise , Esgotos/química , Sulfametoxazol/análise , Espectrometria de Massas em Tandem , Eliminação de Resíduos Líquidos/métodos
5.
Environ Pollut ; 255(Pt 1): 113161, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31541808

RESUMO

In this study a target analysis approach with method detection limits down to 0.01 ng L-1 was developed in order to determine ultra-trace pharmaceuticals in seawater of the German coast and their estuaries. The selection of target analytes based on a prioritisation commissioned by the German Environmental Agency considering occurrence in German surface waters, production volumes and ecotoxicological data. Using ultra-high pressure liquid chromatography coupled to a triple quadrupole mass spectrometer equipped with an electrospray ionisation source 21 prioritised pharmaceuticals out of seven therapeutical classes (antibiotics, iodinated X-ray contrast media (ICM), analgesics, lipid reducers, antiepileptics, anticonvulsants, beta-blockers) have been detected in the low to medium ng L-1-range. The most frequently measured substance groups in the German Baltic Sea and German Bight are the ICM, represented by the non-ionic ICM iomeprol (German Bightmax: 207 ng L-1; Baltic Seamax: 34.5 ng L-1) and the ionic ICM amidotrizoic acid (German Bight: 86.9 ng L-1), respectively. The same pattern of substance distribution could be detected in the German Bight, the German Baltic Sea and their inflows with lower concentrations in the offshore region that are partly a result of dilution with marine water. Pharmaceuticals entering the estuaries and coastal regions are an environmental issue since data on the ecotoxicological effects on aquatic marine organisms is limited. Especially the antibiotics clarithromycin and sulfamethoxazole could be ecotoxicologically/environmentally critical.


Assuntos
Monitoramento Ambiental/métodos , Preparações Farmacêuticas/análise , Água do Mar/química , Poluentes Químicos da Água/análise , Organismos Aquáticos/efeitos dos fármacos , Países Bálticos , Cromatografia Líquida de Alta Pressão , Claritromicina/análise , Ecotoxicologia , Estuários , Alemanha , Limite de Detecção , Medição de Risco , Sulfametoxazol/análise
6.
Ecotoxicol Environ Saf ; 181: 180-186, 2019 Oct 15.
Artigo em Inglês | MEDLINE | ID: mdl-31185432

RESUMO

This study examined the distribution of pharmaceuticals in Yeongsan River and at point sources (PSs) in the associated water system, and performed a risk assessment based on our findings. The samples included effluents collected from three sewage treatment plants (PS1, PS2, and PS3) and two industrial complexes (PS4 and PS5) as well as surface water collected from seven mainstreams and 11 tributaries of the river. The target pharmaceuticals were acetylsalicylic acid, carbamazepine, clarithromycin, naproxen, sulfamethazine, sulfamethoxazole, sulfathiazole, and trimethoprim, which were detected by liquid chromatography-tandem mass spectrometry. All pharmaceuticals except acetylsalicylic acid and sulfathiazole were found in PS1, PS2, and PS3 samples, whereas acetylsalicylic acid, carbamazepine, sulfamethazine, and sulfamethoxazole were found in PS4, most of the pharmaceuticals were not present in PS5. The rank order of pharmaceutical concentration in surface water was carbamazepine (97.2%, 0.2067 µg/L) > sulfamethoxazole (88.9%, 0.1132 µg/L) > naproxen (51.4%, 0.0516 µg/L) > clarithromycin (43.1%, 0.0427 µg/L). The distribution of pharmaceuticals in the Yeongsan River at PSs and non-PSs differed, and higher concentrations of human pharmaceuticals were detected in upstream and midstream areas whereas higher concentrations of animal pharmaceuticals were found downstream. Hazard quotients (HQs) evaluated at each sites based on mean concentration and 95% upper confidence limits (95% UCLs) were all less than one, indicating a low risk of toxicity. The findings of this study are expected to be useful for risk assessment of aquatic ecosystems.


Assuntos
Preparações Farmacêuticas/análise , Rios/química , Poluentes Químicos da Água/análise , Carbamazepina/análise , Cromatografia Líquida , Claritromicina/análise , Ecossistema , Monitoramento Ambiental , Naproxeno/análise , República da Coreia , Medição de Risco , Sulfametoxazol/análise , Espectrometria de Massas em Tandem , Águas Residuárias/química
7.
J Sep Sci ; 40(17): 3535-3544, 2017 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-28683179

RESUMO

A capillary electrophoresis with capacitively coupled contactless conductivity detection based method for the assay of azithromycin, clarithromycin and clindamycin was optimized and validated in this study. A buffer solution of 20 mM 2-(N-morpholino) ethane sulfonic acid, 40 mM l-histidine and 0.6 mM cetyltrimethylammonium bromide (pH 6.39) was used for the electrophoresis. An uncoated, bare-fused silica capillary (total length 60 cm, effective length 32 cm, 75 µm id) was used at 25°C. The sample was injected hydrodynamically at 0.5 psi for 5 s. The electrophoresis was conducted at 30 kV in reverse polarity for 6 min with 3 and 2 min of in-between sodium hydroxide (0.1 M) and background electrolyte rinsing, respectively. Ammonium acetate was used as internal standard. This simple and robust method showed reasonable limit of detection and limit of quantitation for azithromycin (0.0125/0.03 mg/mL), clarithromycin (0.017/0.03 mg/mL), and clindamycin (0.038/0.06 mg/mL), with good selectivity, precision both intraday (relative standard deviation ≤ 1.0%) and interday (relative standard deviation < 3.7%), linearity (R2  > 0.999) and recovery (99 - 101.7%). The method was successfully applied for the determination of azithromycin, clarithromycin and clindamycin in formulations.


Assuntos
Azitromicina/análise , Claritromicina/análise , Clindamicina/análise , Condutividade Elétrica , Eletroforese Capilar
8.
J Chromatogr Sci ; 55(8): 798-804, 2017 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-28449104

RESUMO

Two multivariate calibration-prediction techniques, principal component regression (PCR) and partial least-squares regression (PLSR) were applied to the chromatographic multicomponent analysis of the drug containing lansoprazole (LAN), clarithromycin (CLA) and amoxicillin (AMO). Optimum chromatographic separation of LAN, CLA and AMO with atorvastatin as the internal standard (IS) was obtained by using Xterra® RP18 column 5 µm 4.6 × 250 mm2, and 25 mM ammonium chloride buffer prepared ammonium chloride, acetonitrile and bidistilled water (45:45:10 v/v) as the mobile phase at flow rate 1.0 mL/min. The high pressure liquid chromatography data sets consisting of the ratios of analyte peak areas to the IS peak area were obtained by using diode array detector detection at five wavelengths (205, 210, 215, 220 and 225 nm). LC-chemometric calibration for LAN, CLA and AMO were separately constructed by using the relationship between the peak-area ratio and training sets for each analyte. A series of synthetic solutions containing different concentrations of LAN, CLA and AMO were used to check the prediction ability of the PCR and PLS. Both of the two-chemometric methods in this study can be satisfactorily used for the quantitative analysis and for dissolutions tests of multicomponent commercial drug.


Assuntos
Amoxicilina/análise , Cromatografia Líquida de Alta Pressão/métodos , Claritromicina/análise , Lansoprazol/análise , Modelos Lineares , Análise Multivariada , Reprodutibilidade dos Testes , Comprimidos
9.
J Pharm Biomed Anal ; 136: 162-169, 2017 Mar 20.
Artigo em Inglês | MEDLINE | ID: mdl-28024686

RESUMO

Hydrophobic subtraction model (HSM) is widely applied to select columns of equivalent or different selectivity compared with a reference column, but its application in identifying optimal columns for specific separations of real samples is rare. In this work, a column selection method was proposed by firstly directly correlating separation selectivity of different pairs of solutes to column parameters based on the quantitative relationship of HSM and then selecting the optimal columns according to the predicted selectivity in consideration of the total separation of all critical pairs of solutes. Three critical pairs of solutes in clarithromycin impurity analysis were evaluated as examples. Starting with the analysis of clarithromycin impurities on 15 columns with different selectivities, ten optimal columns were finally identified for clarithromycin impurity analysis from the HSM column characterization database containing nearly 600 columns and two of them were validated with satisfactory separations for all critical peak pairs. The proposed methodology was also compared to the traditional column selection procedure based on calculations of scalar measures of the Euclidean distance between chromatographic columns. Results showed that our method provides an effective way to find the desired columns that may be overlooked by the traditional column selection due to selection of an inappropriate reference column or overestimation of column similarity, such as Fs introduced in HSM.


Assuntos
Antibacterianos/análise , Cromatografia de Fase Reversa/métodos , Claritromicina/análise , Contaminação de Medicamentos , Modelos Químicos , Interações Hidrofóbicas e Hidrofílicas , Reprodutibilidade dos Testes , Sensibilidade e Especificidade
10.
Sci Total Environ ; 562: 136-144, 2016 08 15.
Artigo em Inglês | MEDLINE | ID: mdl-27096634

RESUMO

The macrolide antibiotics erythromycin, clarithromycin and azithromycin are very important in human and animal medicine, and can be entrained onto agricultural ground through application of sewage sludge or manures. In the present study, a series of replicated field plots were left untreated or received up to five annual spring applications of a mixture of three drugs to achieve a nominal concentration for each of 10 or 0.1mgkg(-1) soil; the latter an environmentally relevant concentration. Soil samples were incubated in the laboratory, and supplemented with antibiotics to establish the dissipation kinetics of erythromycin and clarithromycin using radioisotope methods, and azithromycin using HPLC-MS/MS. All three drugs were dissipated significantly more rapidly in soils with a history of field exposure to 10mgkg(-1) macrolides, and erythromycin and clarithromycin were also degraded more rapidly in field soil exposed to 0.1mgkg(-1) macrolides. Rapid mineralization of (14)C-labelled erythromycin and clarithromycin are consistent with biodegradation. Analysis of field soils revealed no carryover of parent compound from year to year. Azithromycin transformation products were detected consistent with removal of the desosamine and cladinose moieties. Overall, these results have revealed that following several years of exposure to macrolide antibiotics these are amenable to accelerated degradation. The potential accelerated degradation of these drugs in soils amended with manure and sewage sludge should be investigated as this phenomenon would attenuate environmental exposure and selection pressure for clinically relevant resistance.


Assuntos
Antibacterianos/análise , Monitoramento Ambiental , Macrolídeos/análise , Poluentes do Solo/análise , Agricultura/estatística & dados numéricos , Azitromicina/análise , Claritromicina/análise , Poluição Ambiental/estatística & dados numéricos , Eritromicina/análise , Solo , Eliminação de Resíduos Líquidos
11.
Chem Pharm Bull (Tokyo) ; 63(9): 663-8, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-26329859

RESUMO

The aim of this study was to evaluate pharmaceuticals using a near-infrared chemical imaging (NIR-CI) technique for visualizing the distribution of ingredients in solid dosage forms of commercially available clarithromycin tablets. The cross section of a tablet was measured using the NIR-CI system for evaluating the distribution of ingredients in the tablet. The chemical images were generated by performing multivariate analysis methods: principal component analysis (PCA) and partial least squares (PLS) with normalized near-infrared (NIR) spectral data. We gained spectral and distributional information related to clarithromycin, cornstarch, and magnesium stearate by using PCA analysis. On the basis of this information, the distribution images of these ingredients were generated using PLS analysis. The results of PCA analysis enabled us to analyze individual components by using PLS even if sufficient information on the products was not available. However, some ingredients such as binder could not be detected using NIR-CI, because their particle sizes were smaller than the pixel size (approximately 25×25×50 µm) and they were present in low concentrations. The combined analysis using both PCA and PLS with NIR-CI was useful to analyze the distribution of ingredients in a commercially available pharmaceutical even when sufficient information on the product is not available.


Assuntos
Claritromicina/análise , Análise dos Mínimos Quadrados , Análise de Componente Principal , Espectroscopia de Luz Próxima ao Infravermelho , Comprimidos/análise
12.
J Pharm Sci ; 104(8): 2641-4, 2015 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-26053058

RESUMO

The pharmaceutical properties of clarithromycin (CAM) tablets containing the metastable form I of crystalline CAM were investigated. Although the dissolution rate of form I was higher than that of stable form II, the release of CAM from form I tablet was delayed. Disintegration test and liquid penetration test showed that the disintegration of the tablet delayed because of the slow penetration of an external solution into form I tablet. Investigation by scanning electron microscopy revealed that the surface of form I tablet was covered with fine needle-shaped crystals following an exposure to the external solution. These crystals were identified as form IV crystals by powder X-ray diffraction. The phenomenon that CAM releases from tablet was inhibited by fine crystals spontaneously formed on the tablet surface could be applied to the design of sustained-release formulation systems with high CAM contents by minimizing the amount of functional excipients.


Assuntos
Antibacterianos/química , Claritromicina/química , Adsorção , Antibacterianos/análise , Celulose/análogos & derivados , Celulose/química , Claritromicina/análise , Preparações de Ação Retardada , Excipientes/química , Cinética , Microscopia Eletrônica de Varredura , Estrutura Molecular , Transição de Fase , Difração de Pó , Dióxido de Silício/química , Solubilidade , Propriedades de Superfície , Comprimidos , Água/análise
13.
Anal Biochem ; 468: 75-82, 2015 01 01.
Artigo em Inglês | MEDLINE | ID: mdl-25256165

RESUMO

Erythromycin (ERY), clarithromycin (CLA), roxithromycin (ROX), and azithromycin (AZI) are macrolide antibiotics widely used in livestock and human medicine. Therefore, they are frequently found as pollutants in environmental water. A method based on indirect competitive enzyme-linked immunosorbent assay (ELISA) for group determination of these macrolides in foodstuffs, human biofluids, and water was developed. Carboxymethyloxime of clarithromycin (CMO-CLA) was synthesized and conjugated to bovine serum albumin (BSA) and gelatin to prepare immunogen and coating antigen with advantageous presentation of target epitopes, l-cladinose and d-desosamine, common for these analytes. Antibodies generated in rabbits were capable of recognizing ERY, CLA, and ROX as a group (100-150%), and AZI (12%) and did not cross-react with ERY degradants, which lack antibiotic activity. Assay displayed sensitivity of determination of 14-membered macrolides (IC50=0.13-0.2ng/ml) and low limit of detection (LOD) that was achieved at 0.02 to 0.03ng/ml. It allowed performing analysis of milk, muscle, eggs, bovine serum, water, human serum and urine, and avoiding matrix effect without special pretreatment using simple dilution with assay buffer. For 15-membered macrolide AZI, the corresponding characteristics were IC50=1.6ng/ml and LOD=0.14ng/ml. The recoveries of veterinary and human medicine macrolides from corresponding matrices were validated and found to be satisfactory.


Assuntos
Antibacterianos/análise , Azitromicina/análise , Macrolídeos/análise , Animais , Antibacterianos/química , Antibacterianos/imunologia , Anticorpos , Azitromicina/química , Azitromicina/imunologia , Líquidos Corporais/química , Bovinos , Claritromicina/análise , Claritromicina/química , Claritromicina/imunologia , Reações Cruzadas , Ensaio de Imunoadsorção Enzimática/métodos , Epitopos/química , Eritromicina/análise , Eritromicina/química , Eritromicina/imunologia , Contaminação de Alimentos/análise , Humanos , Limite de Detecção , Macrolídeos/química , Macrolídeos/imunologia , Coelhos , Roxitromicina/análise , Roxitromicina/química , Roxitromicina/imunologia , Poluentes Químicos da Água/análise , Poluentes Químicos da Água/química , Poluentes Químicos da Água/imunologia
14.
Arch Pharm Res ; 38(5): 839-48, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-25213008

RESUMO

Clarithromycin (CAM) is known to be poorly water-soluble and acid-labile drug. Various alkalizers such as MgO, Na2CO3, Na2HPO4 and NaHCO3 were utilized to modulate the microenvironmental pH (pHM) and to improve the low stability and solubility of CAM in a crystalline-solid dispersion system (CSD). Polyvinylpyrrolidone (PVP K-30) and hydroxypropylmethylcellulose (HPMC) 4000-based CSDs containing alkalizers were prepared by cosolvent precipitation followed by evaporation process. The dried-CSDs mixed with microcrystalline cellulose, 2% croscarmellose sodium, and 1% magnesium stearate was then directly compressed into tablet. A dissolution test was carried out in 900 mL of pH 5.0 buffer solutions at 37 °C with a 50 rpm paddle speed. pHM, surface morphology, and structural behaviors were investigated. The dissolution rates of CAM in CSD containing alkalizers were improved. The drug in CSD remained crystalline as observed by differential scanning calorimetry and powder X-ray diffraction. Scanning electron microscopy revealed nearly identical images regardless of the sorts and amounts of carriers. PVP-based CSD tablet without alkalizer showed greater drug release, while HPMC-based CSD tablet without alkalizer retarded drug release due to its greater swelling capability. However, when the alkalizers were added in CSD tablet, the drug release was sharply increased. NaHCO3 induced the most rapid drug release while MgO retarded drug dissolution. Alkalizers in CSD also could maintain the pHM of the tablet above pH 5 under acidic conditions. The use of pH modifiers in CSDs could provide a useful method to improve the dissolution rate and stability of CAM via modulation of pHM without changing drug crystallinity.


Assuntos
Antiácidos/química , Antibacterianos/química , Claritromicina/química , Antiácidos/análise , Antibacterianos/análise , Claritromicina/análise , Cristalização , Estabilidade de Medicamentos , Concentração de Íons de Hidrogênio , Solubilidade , Difração de Raios X
15.
Environ Toxicol Pharmacol ; 38(1): 79-83, 2014 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-24929476

RESUMO

In this study, environmental risks of selected pharmaceuticals were investigated to assess potential hazards. Ciprofloxacin, Clarithromycin, Cefuroxime axetil, antibiotics, Benzalkoniuman antiseptic, Paracetamol, an analgesic, and Naproxen, an anti-inflammatory, were selected due to their high rate of usage in Turkey. Ciprofloxacin was found to have the highest risk due to its high PEC/PNEC ratio (28.636). Benzalkonium, Paracetamol and Clarithromycin have a potential to cause environmental hazards. The biodegradation and biological concentration factors (BCF) of the drugs were also determined using EPA/STWIN and EPA/BCFWIN programs. The results illustrated that these pharmaceuticals are nonbiodegradable in wastewater treatment plants. The BCFs of Benzalkonium and Clarithromycin were found to be very high, 70.790 L/kg and 56.490 L/kg, respectively. It was suggested that alternative treatment methods other than biological ones should be investigated for these pharmaceuticals because of their low biodegradability. Also, unnecessary use of antibiotics is supposed to be discouraged to reduce environmental hazards.


Assuntos
Preparações Farmacêuticas/análise , Esgotos/análise , Poluentes Químicos da Água/análise , 1-Octanol/química , Acetaminofen/análise , Acetaminofen/química , Adsorção , Antibacterianos/análise , Antibacterianos/química , Anti-Infecciosos Locais/análise , Anti-Infecciosos Locais/química , Anti-Inflamatórios não Esteroides/análise , Anti-Inflamatórios não Esteroides/química , Compostos de Benzalcônio/análise , Compostos de Benzalcônio/química , Cefuroxima/análogos & derivados , Cefuroxima/análise , Cefuroxima/química , Ciprofloxacina/análise , Ciprofloxacina/química , Claritromicina/análise , Claritromicina/química , Monitoramento Ambiental , Naproxeno/análise , Naproxeno/química , Preparações Farmacêuticas/química , Medição de Risco , Esgotos/química , Turquia , Água/química , Poluentes Químicos da Água/química
16.
Environ Sci Pollut Res Int ; 21(18): 10917-39, 2014 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-24756682

RESUMO

Fifty samples of finished drinking waters (FDWs) from Spain covering 12 million inhabitants were tested for 53 pharmaceuticals pertaining to 12 different Anatomical Therapeutic Chemical (ATC) classification system codes. The studied compounds are a combination of most commonly consumed pharmaceuticals with other barely reported in the literature. Five compounds, azithromycin, clarithromycin, erythromycin, sulfamethoxazole, and ibuprofen were tentatively identified by liquid chromatography coupled to tandem mass spectrometry (LC-MS/MS) in some samples (2 to 15 %), but only ibuprofen and azithromycin could be confirmed when analyzed by liquid chromatography-high-resolution mass spectrometry (LC-HRMS) with a quadrupole-Orbitrap instrument. Concentration levels of ibuprofen in the positive samples ranged from 12 to 17 ng/L (n = 6) while for azithromycin values from 5 to 9.5 ng/L (n = 3) were found. Ibuprofen fragmentation behaviour in different mass spectrometry instrument configurations (triple quadrupole, quadrupole-ion trap, and quadrupole-Orbitrap) was evaluated.


Assuntos
Água Potável/química , Monitoramento Ambiental/estatística & dados numéricos , Preparações Farmacêuticas/análise , Poluentes Químicos da Água/análise , Azitromicina/análise , Cromatografia Líquida/métodos , Claritromicina/análise , Monitoramento Ambiental/métodos , Eritromicina/análise , Ibuprofeno/análise , Espanha , Sulfametoxazol/análise , Espectrometria de Massas em Tandem/métodos
17.
BMC Pharmacol Toxicol ; 15: 13, 2014 Mar 05.
Artigo em Inglês | MEDLINE | ID: mdl-24593851

RESUMO

BACKGROUND: Access to good-quality medicines in many countries is largely hindered by the rampant circulation of spurious/falsely labeled/falsified/counterfeit (SFFC) and substandard medicines. In 2006, the Ministry of Health of Cambodia, in collaboration with Kanazawa University, Japan, initiated a project to combat SFFC medicines. METHODS: To assess the quality of medicines and prevalence of SFFC medicines among selected products, a cross-sectional survey was carried out in Cambodia. Cefixime, omeprazole, co-trimoxazole, clarithromycin, and sildenafil were selected as candidate medicines. These medicines were purchased from private community drug outlets in the capital, Phnom Penh, and Svay Rieng and Kandal provinces through a stratified random sampling scheme in July 2010. RESULTS: In total, 325 medicine samples were collected from 111 drug outlets. Non-licensed outlets were more commonly encountered in rural than in urban areas (p < 0.01). Of all the samples, 93.5% were registered and 80% were foreign products. Samples without registration numbers were found more frequently among foreign-manufactured products than in domestic ones (p < 0.01). According to pharmacopeial analytical results, 14.5%, 4.6%, and 24.6% of the samples were unacceptable in quantity, content uniformity, and dissolution test, respectively. All the ultimately unacceptable samples in the content uniformity tests were of foreign origin. Following authenticity investigations conducted with the respective manufacturers and medicine regulatory authorities, an unregistered product of cefixime collected from a pharmacy was confirmed as an SFFC medicine. However, the sample was acceptable in quantity, content uniformity, and dissolution test. CONCLUSIONS: The results of this survey indicate that medicine counterfeiting is not limited to essential medicines in Cambodia: newer-generation medicines are also targeted. Concerted efforts by both domestic and foreign manufacturers, wholesalers, retailers, and regulatory authorities should help improve the quality of medicines.


Assuntos
Cefixima/análise , Claritromicina/análise , Medicamentos Falsificados , Omeprazol/análise , Piperazinas/análise , Sulfonas/análise , Combinação Trimetoprima e Sulfametoxazol/análise , Camboja , Rotulagem de Medicamentos , Medicamentos Essenciais/análise , Fraude , Vigilância em Saúde Pública , Purinas/análise , Controle de Qualidade , Citrato de Sildenafila
18.
Mar Pollut Bull ; 85(2): 710-9, 2014 Aug 30.
Artigo em Inglês | MEDLINE | ID: mdl-24467856

RESUMO

This work deals with the environmental distribution of nonionic surfactants (nonylphenol and alcohol ethoxylates), their metabolites (NP, nonylphenol; NPEC, nonylphenol ethoxycarboxylates; and PEG, polyethylene glycols) and a selection of 64 pharmaceuticals in the Long Island Sound (LIS) Estuary which receives important sewage discharges from New York City (NYC). Most target compounds were efficiently removed (>95%) in one wastewater treatment plant monitored, with the exception of NPEC and some specific drugs (e.g., hydrochlorothiazide). Concentrations of surfactants (1.4-4.5 µg L(-1)) and pharmaceuticals (0.1-0.3 µg L(-1)) in seawater were influenced by tides and sampling depth, consistent with salinity differences. Surfactants levels in suspended solids samples were higher than 1 µg g(-1), whereas only most hydrophobic or positively charged pharmaceuticals could be found (e.g., tamoxifen, clarithromycin). Maximum levels of target compounds in LIS sediments (PEG at highest concentrations, 2.8 µg g(-1)) were measured nearest NYC, sharply decreasing with distance from major sewage inputs.


Assuntos
Estuários , Sedimentos Geológicos/química , Preparações Farmacêuticas/análise , Tensoativos/análise , Poluentes Químicos da Água/análise , Claritromicina/análise , Geografia , New York , Fenóis/análise , Polietilenoglicóis/análise , Rios , Água do Mar/química , Esgotos/química , Tamoxifeno/análise , Urbanização , Eliminação de Resíduos Líquidos , Águas Residuárias , Purificação da Água
19.
J Investig Clin Dent ; 5(1): 23-31, 2014 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-23097216

RESUMO

OBJECTIVE: As the risk involved with systemic antimicrobials (high doses, microbial resistance, adverse reactions, etc.) restricts their use and local delivery of antimicrobials into periodontal pockets improves periodontal health, this study was designed to investigate the effects of subgingivally delivered clarithromycin (CLM; 0.5%) as an adjunct to nonsurgical mechanotherapy in chronic periodontitis subjects. METHODS: Ninety-eight patients were categorized into two treatment groups: scaling and root planing (SRP) plus 0.5% CLM (test; group 1) and SRP plus placebo (control; group 2). Clinical parameters included gingival index (GI), sulcus bleeding index (SBI), plaque index (PI), probing depth (PD), and periodontal attachment level (PAL), recorded at 4, 8 and 12 weeks. The concentration of 0.5% CLM in gingival fluid was estimated by reverse-phase high pressure liquid chromatography. anova, the chi-square test and the Scatterthwaite test were used for statistical analysis. RESULTS: Patients treated with SRP + CLM showed enhanced reductions in GI, SBI, and PD, and gains in PAL (P < 0.001) over time, as compared with the placebo group. However, no statistically significant differences were noted for PI. The mean concentration of CLM was detected in gingival crevicular fluid for up to 7 weeks, fulfilling the conditions for a controlled-release device. CONCLUSION: Adjunctive use of 0.5% CLM as a controlled drug delivery system enhanced the clinical outcome up to 3 months.


Assuntos
Antibacterianos/administração & dosagem , Periodontite Crônica/terapia , Claritromicina/administração & dosagem , Raspagem Dentária/métodos , Aplainamento Radicular/métodos , Administração Tópica , Adulto , Antibacterianos/análise , Claritromicina/análise , Terapia Combinada , Preparações de Ação Retardada , Índice de Placa Dentária , Método Duplo-Cego , Sistemas de Liberação de Medicamentos , Feminino , Seguimentos , Líquido do Sulco Gengival/química , Humanos , Ácido Láctico/química , Masculino , Pessoa de Meia-Idade , Perda da Inserção Periodontal/terapia , Índice Periodontal , Bolsa Periodontal/terapia , Placebos , Ácido Poliglicólico/química , Copolímero de Ácido Poliláctico e Ácido Poliglicólico
20.
Sci Total Environ ; 468-469: 19-27, 2014 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-24012892

RESUMO

The presence of pathogenic antibiotic-resistant bacteria in aquatic environments has become a health threat in the last few years. Their presence has increased due to the presence of antibiotics in wastewater effluents, which are not efficiently removed by conventional wastewater treatments. As a result there is a need to study the possible ways of removal of the mixtures of antibiotics present in wastewater effluents and the antibiotic-resistant bacteria, which may also spread the antibiotic resistance genes to other bacterial populations. In this study the degradation of a mixture of antibiotics i.e. sulfamethoxazole and clarithromycin, the disinfection of total enterococci and the removal of those resistant to: a) sulfamethoxazole, b) clarithromycin and c) to both antibiotics have been examined, along with the toxicity of the whole effluent mixture after treatment to the luminescent aquatic bacterium Vibrio fischeri. Solar Fenton treatment (natural solar driven oxidation) using Fenton reagent doses of 50 mg L(-1) of hydrogen peroxide and 5 mg L(-1) of Fe(3+) in a pilot-scale compound parabolic collector plant was used to examine the disinfection and antibiotic resistance removal efficiency in different aqueous matrices, namely distilled water, simulated and real wastewater effluents. There was a faster complete removal of enterococci and of antibiotics in all aqueous matrices by applying solar Fenton when compared to photolytic treatment of the matrices. Sulfamethoxazole was more efficiently degraded than clarithromycin in all three aqueous matrices (95% removal of sulfamethoxazole and 70% removal of clarithromycin in real wastewater). The antibiotic resistance of enterococci towards both antibiotics exhibited a 5-log reduction with solar Fenton in real wastewater effluent. Also after solar Fenton treatment, there were 10 times more antibiotic-resistant enterococci in the presence of sulfamethoxazole than in the presence of clarithromycin. Finally, the toxicity of the treated wastewater to V. fischeri remained very low throughout the treatment time.


Assuntos
Claritromicina/metabolismo , Farmacorresistência Bacteriana , Enterococcus/metabolismo , Sulfametoxazol/metabolismo , Microbiologia da Água , Poluentes Químicos da Água/análise , Purificação da Água/métodos , Aliivibrio fischeri/efeitos dos fármacos , Bioensaio , Cromatografia Líquida de Alta Pressão , Claritromicina/análise , Desinfecção/métodos , Peróxido de Hidrogênio/metabolismo , Ferro/metabolismo , Oxirredução , Sulfametoxazol/análise , Espectrometria de Massas em Tandem , Poluentes Químicos da Água/toxicidade
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