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EN
Pentatrichomonas hominis, a parasitic protozoan often detected in human diarrheic stools, is the cause of severe morbidity in newborns and children, particularly in tropical zones. The flagellate is resistant to many disinfectants and anti-protozoan drugs. Therefore in this study we have synthesized three novel 4,5,6,7-tetrabromobenzimidazole (TBBI) derivatives carrying a polyfluoroalkyl substituent in position 2 of the benzimidazole scaffold, namely 2-trifluoromethyl-TBBI (CF3-TBBI), 2-nonafluorobutyl-TBBI (C4F9-TBBI), and 2-nonadecafluorononyl-TBBI (C9F19-TBBI), that next we tested for their in vitro activity against P. hominis.Widely applied anti-protozoal drug, metronidazole as a reference was used. All the investigated agents were added to 24 h P. hominis cultures; each of them was administered at three different concentrations. Number of the moving trichomonads was determined and compared with the control cultures. Different anti-trichomonal activity occurred depending on a kind of compound and its concentration. C4F9-TBBI was the most effective TBBI derivative tested: the agent, at the highest concentration 24.2 μg/ml, after 72 h reduced the number of viable trichomonads to 44.3%; C9F19-TBBI, at the concentration 24 μg/ml reduced the number of the flagellates to 58.5%. Paradoxically, metronidazole after the same time given at the highest concentration increased trophozoite counts by 464.6% in comparison with the control cultures (100%).
EN
Metronidazole belongs to the most commonly prescribed medications for bacterial and parasitic infections worldwide. It is also used in perioperative prevention prior to bowel, and head and neck surgeries. Despite the fact that the World Health Organization has placed it on its List of Essential Medicines, it is considered potentially carcinogenic. A great number of research studies have been conducted to clarify this issue, but results are inconclusive. None of the studies focused on the influence of metronidazole on oral cancer development. The aim of our study was to evaluate the impact of metronidazole on the viability of tongue cancer cells. The research was conducted on the tongue squamous cell carcinoma cell line (CAL-27). Metronidazole dissolved in growth medium was applied to the cell culture at concentrations: 1, 10, 50, 100μg/mL. Toxicity of the drug was evaluated by MTT assay and the [3H]-thymidine incorporation test. The MTT test revealed a significant increase in cell viability under the influence of metronidazole after 24h, at the highest concentration of the drug (100μg/mL), but had no impact on cell viability at other concentrations and after 48h and 72h. The results of the [3H]-thymidine incorporation test did not show significant results. Summarizing, metronidazole stimulates the viability of tongue squamous cell carcinoma cells according to its concentration and the time of incubation (results significant at the concentration 100μg/mL, after 24 hours of incubation).
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EN
We report on preparation of poly(acrylic acid-co-methyl methacrylate) (PAM) micro- and nanoparticles and, in the subsequent stage, complexation reaction with the active substance - metronidazole (MET). The drug release behavior of MET - loaded PAM micro- and nanoparticles was evaluated in water and phosphate buffered saline (PBS, 0.9% NaCl) at 37ºC. It has been found that introduction of MET into PAM micro- and nanoparticles enabled gradual and controlled release of the active substance. Structural analysis using FT-IR (ATR) and 1H NMR, as well as surface morphology assessment by SEM, were performed.
EN
Soil contamination with medicines can occur when unused or expired medications are improperly disposed of or when pharmaceutical manufacturing waste is inadequately treated or managed. Moreover, the largest percentage of damaged and expired medical materials in the sanitary landfill area during the COVID-19 period in the study region were Metronidazole (Flagyl) and Amoxicillin. The disposal of numerous drugs and medical waste from Al-Jazeera Pharmaceuticals Company, which were examined and found to have a higher concentration of the compound Metronidazole (Flagyl) and Amoxicillin, This study aimed to analyze the results of the impact of Metronidazole (Flagyl) and Amoxicillin concentrations on the chemical and geotechnical properties of soil. Undisturbed soil samples was collected and then cured by mixing 10 mg/l of Metronidazole (Flagyl) and 25 mg/l of Amoxicillin to the time period from 15 to 135 days. The obtained geotechnical tests results of natural and contaminated silty clay soil showed that the soil became softer, the cohesiveness between the particle sizes of soil decreased due to the absorption of the soil by the Metronidazole (Flagyl) and Amoxicillin concentration. Moreover, the results indicate that the soil collapse rose from 5.6 to 9.5 after 150 days of curing.
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tom Vol. 26, no. 1
67--80
EN
Validated gradient high-performance liquid chromatography-diode array detection (HPLC-DAD) method has been developed for simultaneous determination of diloxanide furoate (DIL), mebeverine hydrochloride (MBV), and metronidazole (MET) in their pharmaceutical preparation. This method was based on a reversed-phase HPLC separation of the cited drugs on a C-18 column (150 mm × 4.6 mm, 5 μm) with a gradient elution system of 0.05 M phosphate buffer with 1% (v/v) of triethylamine adjusted to pH 3.0-methanol as the mobile phase at the flow rate of 1.0 mL min -1. The separation was carried out at ambient temperature. Quantitation was achieved with DAD detection at 260 nm for DIL and MEB, and at 320 for MET based on peak area with linear calibration curves at concentration ranges 4–30, 1–20, and 1–30 μg mL -1 for DIL, MEB, and MET, respectively. The proposed chromatographic method was successfully applied to the determination of the investigated drugs in pharmaceutical preparation. It was validated in compliance with International Conference on Harmonization (ICH) guidelines, in terms of linearity, accuracy, precision, robustness, limits of detection, and quantitation and other aspects of analytical validation.
EN
A fast reliable micellar electrokinetic methodology was investigated for the concurrent quantitation of six antimicrobial and anti-inflammatory drugs, namely, ciprofloxacin, dexamethasone, metronidazole, ornidazole, spiramycin and tinidazole. The method has the merits of rapidity, precision, and sensitivity. The separation was carried out in less than 7 min by applying a basic background electrolyte consisting of 25 mM disodium tetraborate buffer, pH 9 containing 50 mM SDS at 25 kV using photodiode array detector at 230 and 315 nm. The internal standard used during analysis was cromolyn sodium and validation was carried out following ICH guidelines. The proposed method showed linear response over the range from 0.5 to 10.0 μg mL⁻¹ reaching limits of detection and limits of quantitation in the ranges of 0.09–0.2 μg mL⁻¹ and 0.27–0.6 respectively. The method's greenness was estimated using the GAPI tool where excellent greenness was concluded. Co-formulated or single-ingredient commercial preparations were investigated and the results were statistically evaluated.
EN
A simple, rapid, and sensitive reversed-phase HPLC method was developed and validated for determination of metronidazole and tinidazole in human plasma samples under identical chromatographic conditions. This method involves liquid-liquid extraction using chloroform: isopropylalcohol (95:5). Chromatographic separation was performed using a μ-bondapack C18 (250 mm × 4.6 mm) column. The mobile phase consisted of potassium dihydrogen phosphate solution (0.005 M)/acetonitrile (80/20 v/v). The final pH of the mobile phase was adjusted to 4 ± 0.1 with orthophosphoric acid. The calibration curves were linear over the concentration range 0.1–15 μg/mL for metronidazole and tinidazole with the detection limit of 30 ng/mL. Within- and between-day precision and accuracy did not exceed 9.83% and 10.48%, respectively. Metronidazole and tinidazole were found to be stable in plasma samples with no evidence of degradation during 3 freeze-thaw cycles and 3 months storage in −70 °C. The current validated bio-analytical method was finally applied in bioequivalence studies of two different metronidazole and tinidazole products according to a standard two-way cross-over design with a two-week washout period. No statistically significant difference was observed between the logarithmically transformed AUC0-∞ and Cmax values. Therefore, generic products were considered bioequivalent with those of standards which could be used interchangeably.
EN
A high-performance liquid chromatography (HPLC) method with ultraviolet (UV) detection for simultaneous determination of metronidazole, methylparaben, and propylparaben in vaginal gel formulation was described. The chromatography was carried out on a C18 (250 mm × 4.6 mm, 5 μm) column with acetonitrile and 0.3% phosphoric acid solution (20:80 v/v) modified by 0.1% triethylamine as mobile phase, at a flow rate of 1.0 mL min-1, with detection at 260 nm. Under these chromatographic conditions, the obtained retention times were approximately 3.43 min for metronidazole, 5.17 min for propylparaben, and 15.12 min for methylparaben. Analytical parameters specificity, linearity, accuracy, and precision were determined by validation procedure and found to be satisfactory. Overall, the proposed method was found to be simple, precise, and accurate for quality control of metronidazole in the presence of preservatives in gel formulation.
PL
W pracy przedstawiono wyniki badań uwalniania radiouczulacza metronidazolu z jednowarstwowych oraz trójwarstwowych matryc kopolimeru glkolidu z laktydem do sztucznego płynu mózgowo rdzeniowego ACFs. Przeprowadzono analizę mikrostruktury łańcuchów polimerowych w oparciu o spektroskopię magnetycznego rezonansu jądrowego. Badanie uwalniania leku prowadzono w systemie dynamicznym z regularną wymianą buforu we fiolkach poddanych wytrząsaniu. Ekstrakty analizowano metodą spektrometrii UV-VIS. Równolegle prowadzono badania degradacji matryc z lekiem pod kątem oceny zmian w mikrostrukturze łańcucha polimerowego. Badania wykazały znacznie szybszą degradację matryc wykonanych z kopolimeru glikolidu z D,L-laktydem w porównaniu z matrycami z kopolimeru glikolidu z L-laktydem. Ponadto wykazano że opłaszczenie matrycy zawierającej lek polimerem bez leku (matryce trójwarstwowe) zapobiega nagłemu wyrzutowi leku z powierzchni w pierwszych dniach uwalniania.
EN
In this paper the results of radiosensitizer metronidazole release investigation from mono- and triple-layered copolymeric matrices in artificial cerebro- spinal fluid solution (ACFs) are presented. The analysis of polymeric chain microstructure by the NMR has been conducted. Drug release study was performed in the dynamic system with regular buffer exchange in constantly stirred glass ampoules. The extracts were analyzed by the UV-VIS spectrometry. Drug carrying matrices degradation research were conducted to evaluate possible changes in polymeric chain microstructure. The results showed that matrices containing poly(glycolide-co-D,L-lactide) demonstrate higher degradation rate than matrices containing poly(glycolide-co-L-lactide). It has been proved that drug carriers coated with drug-free polymer (triplelayered matrices) prevents from burst effect.
EN
Purpose: In this work our aim was to reveal the relationship between sodium alginate concentration and crosslinking level, also the ratio of release of the antibacterial additives: silver nanoparticles and metronidazole. Moreover, we examine obtained hydrogel as a potential dressing material for regenerative medicine. Design/methodology/approach: In the research specimens of hydrogels were tested to define their mechanical and physicochemical properties like antibacterial activity against gramnegative Escherichia coli and gram-positive Staphylococcus aureus, viscosity and conductivity. Findings: The concentration of alginate and presence of antibacterial additives influence on the crosslinking level. Mechanical properties of hydrogels are similar to human skin. Only hydrogels with addition of metronidazole and AgNP inhibits bacteria growth after 18 h. In case of gram-negative Escherichia coli both of the aseptic additives inhibits bacteria growth, but sodium alginate hydrogel with silver nanoparticles gives better results in tests with grampositive Staphylococcus aureus . Research limitations/implications: The presence of metronidazole in hydrogel, especially its incorporation and binding with mannuronic and guluronic acid residues must be clarified in more advanced research. Practical implications: Obtained results shows that sodium alginate hydrogels with 0.1mg/ml of alginate, due to its properties are proper as a dressing material. Based on the results, and more advanced tests with metronidazole, we can consider dressing design. Originality/value: Unique value of this work is that we completed the gap in knowledge about the relation of crosslinking level and mechanical properties with are crucial to proper tissue healing and addition of popular aseptic agents.
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