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1.
Molecules ; 28(21)2023 Oct 28.
Artigo em Inglês | MEDLINE | ID: mdl-37959728

RESUMO

Polymers, including non-linear copolymers, have great potential in the development of drug delivery systems with many advantages, but the design requires optimizing polymer-drug interactions. Molecular dynamics (MD) simulations can provide insights into polymer-drug interactions for designing delivery systems, but mimicking formulation processes such as drying is often not included in in silico studies. This study demonstrates an MD approach to model drying of systems comprising either hydrophilic tinidazole or hydrophobic clotrimazole drugs with amphiphilic hyperbranched copolyethers. The simulated drying protocol was critical for elucidating drug encapsulation and binding mechanisms. Experimentally, two polymers were synthesized and shown to encapsulate clotrimazole with up to 83% efficiency, guided by interactions with the hydrophobic core observed in simulations. In contrast, tinidazole is associated with surface regions, indicating capacity differences between drug types. Overall, this work highlights MD simulation of the drying process as an important tool for predicting drug-polymer complex behaviour. The modelled formulation protocol enabled high encapsulation efficiency and opened possibilities for the design of delivery systems based on computationally derived binding mechanisms. This demonstrates a computational-experimental approach where simulated drying was integral to elucidating interactions and developing optimized complexes, emphasizing the value of molecular modelling for the development of drug delivery formulations.


Assuntos
Micelas , Simulação de Dinâmica Molecular , Tinidazol , Clotrimazol , Polímeros/química , Interações Hidrofóbicas e Hidrofílicas , Portadores de Fármacos/química , Polietilenoglicóis/química
2.
Int J Pharm ; 644: 123296, 2023 Sep 25.
Artigo em Inglês | MEDLINE | ID: mdl-37553058

RESUMO

Bacterial vaginosis (BV) is a common dysbiosis of the human vaginal microbiota characterized by depletion of hydrogen peroxide and lactic acid-producing Lactobacillus bacteria and an overgrowth of certain facultative anaerobic bacteria. Although short-term cure rates following treatment with frontline antibiotics (most notably oral metronidazole (MNZ), clindamycin vaginal cream, and MNZ vaginal gel) are generally high, longer-term recurrence rates are an issue. The development of vaginal formulations offering continuous/sustained administration of antibiotic drugs over one or more weeks might prove useful in reducing recurrence. Here, we report the manufacture and preclinical testing of matrix-type vaginal rings offering sustained release of four 5-nitroimidazole antimicrobial drugs either being used clinically or having potential in treatment of BV - MNZ, tinidazole (TNZ), secnidazole (SNZ) and ornidazole (ONZ). All four drugs showed good compatibility with a medical-grade addition-cure silicone elastomer based upon thermal analysis experiments, and matrix-type rings containing 250 mg (3.125 %w/w) of each drug were successfully manufactured by reaction injection molding. 28-day in vitro drug release studies demonstrated root-time kinetics, with daily release rates of 25, 22, 9 and 6 mg/day½ for SNZ, ONZ, MNZ and TNZ, respectively. The rank order of drug release from rings correlated with the simple molecular permeability parameter S/V, where S is the measured drug solubility in silicone fluid and V is the drug molecular volume. The relative merits of SNZ and ONZ over MNZ (the current reference treatment) are discussed. The data support development of vaginal rings for sustained release of 5-nitroimidazole compounds for treatment of BV.


Assuntos
Dispositivos Anticoncepcionais Femininos , Ornidazol , Vaginose Bacteriana , Feminino , Humanos , Vaginose Bacteriana/tratamento farmacológico , Elastômeros de Silicone , Preparações de Ação Retardada/uso terapêutico , Administração Intravaginal , Metronidazol , Antibacterianos , Tinidazol , Ornidazol/uso terapêutico
4.
Sci Rep ; 13(1): 12192, 2023 07 27.
Artigo em Inglês | MEDLINE | ID: mdl-37500681

RESUMO

Infections by Entamoeba histolytica (E. histolytica) lead to considerable morbidity and mortality worldwide and treatment is reliant on a single class of drugs, nitroimidazoles. Treatment failures and intermittent reports of relapse from different parts of world indicate towards development of clinical drug resistance. In the present study, susceptibility testing of clinical isolates of E. histolytica was carried against metronidazole and tinidazole. Additionally, anti-amoebic property of active compounds of Andrographis paniculata was also evaluated. Prevalence of metronidazole resistance gene (nim) in patients attending hospital was also done to get comprehensive insight of present situation of drug resistance in E. histolytica. Mean inhibitory concentration 50 (IC50) value of E. histolytica isolates against metronidazole and tinidazole was 20.01 and 16.1 µM respectively. Andrographolide showed minimum mean IC50 value (3.06 µM). Significant percentage inhibition of E. histolytica isolates by andrographolide was seen as compared to metronidazole (p = 0.0495). None of E. histolytica isolates showed presence of nim gene. However, in stool samples from hospital attending population, prevalence of nimE gene was found to be 76.6% (69/90) and 62.2% (56/90) in diarrheal and non-diarrheal samples respectively. Inhibitory concentration of commonly used nitroimidazoles against clinical isolates of E. histolytica are on rise. Percentage inhibition of E. histolytica isolates by andrographolide was significantly higher than control drug metronidazole.


Assuntos
Entamoeba histolytica , Abscesso Hepático Amebiano , Nitroimidazóis , Humanos , Nitroimidazóis/farmacologia , Nitroimidazóis/uso terapêutico , Entamoeba histolytica/genética , Abscesso Hepático Amebiano/diagnóstico , Abscesso Hepático Amebiano/tratamento farmacológico , Metronidazol/farmacologia , Metronidazol/uso terapêutico , Tinidazol/uso terapêutico , Reposicionamento de Medicamentos
5.
Int Marit Health ; 74(2): 89-91, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37417841

RESUMO

A unique report of Schönlein-Henoch purpura (SHP) associated with a recent Giardia lamblia enteric infection is described and discussed on the ground of the available literature. Tinidazole plus an appropriate probiotic therapy, including Lactobacillus reuteri and vitamin D, proved to be effective in the condition. SHP is an immunocomplex-mediated disorder characterised by a number of differently associated signs and symptoms, leading to the possible involvement of the skin, joints, abdomen and kidneys. Recent bacterial, viral, or protozoan infections may trigger the disease onset in patients of all ages. The paper describes the first case of SHP triggered by a giardiasis. Tinidazole plus an appropriate probiotic therapy, i.e. L. reuteri and vitamin D proved to be effective in this condition. To our knowledge, this is the first reported case of lambliasis-associated SHP described in an international traveller.


Assuntos
Giardíase , Vasculite por IgA , Humanos , Vasculite por IgA/complicações , Vasculite por IgA/diagnóstico , Giardíase/complicações , Tinidazol , Vitamina D , Itália
6.
Antimicrob Agents Chemother ; 67(4): e0000623, 2023 04 18.
Artigo em Inglês | MEDLINE | ID: mdl-37070857

RESUMO

Mycoplasma genitalium is a sexually transmitted reproductive tract pathogen of men and women. M. genitalium infections are increasingly difficult to treat due to poor efficacy of doxycycline and acquired resistance to azithromycin and moxifloxacin. A recent clinical trial suggested that metronidazole may improve cure rates for women with pelvic inflammatory disease and reduced the detection of M. genitalium when included with standard doxycycline plus ceftriaxone treatment. As data regarding susceptibility of mycoplasmas to nitroimidazoles are lacking in the scientific literature, we determined the in vitro susceptibility of 10 M. genitalium strains to metronidazole, secnidazole, and tinidazole. MICs ranged from 1.6 to 12.5 µg/mL for metronidazole, 3.1 to 12.5 µg/mL for secnidazole, and 0.8 to 6.3 µg/mL for tinidazole. None of these agents was synergistic with doxycycline in checkerboard broth microdilution assays. Tinidazole was superior to metronidazole and secnidazole in terms of MIC and time-kill kinetics and was bactericidal (>99.9% killing) at concentrations below reported serum concentrations. Mutations associated with nitroimidazole resistance were identified by whole-genome sequencing of spontaneous resistant mutants, suggesting a mechanism for reductive activation of the nitroimidazole prodrug by a predicted NAD(P)H-dependent flavin mononucleotide (FMN) oxidoreductase. The presence of oxygen did not affect MICs of wild-type M. genitalium, but a nitroimidazole-resistant mutant was defective for growth under anaerobic conditions, suggesting that resistant mutants may have a fitness disadvantage in anaerobic genital sites. Clinical studies are needed to determine if nitroimidazoles, especially tinidazole, are effective for eradicating M. genitalium infections in men and women.


Assuntos
Infecções por Mycoplasma , Mycoplasma genitalium , Nitroimidazóis , Masculino , Feminino , Humanos , Nitroimidazóis/farmacologia , Nitroimidazóis/uso terapêutico , Doxiciclina/farmacologia , Doxiciclina/uso terapêutico , Metronidazol/farmacologia , Metronidazol/uso terapêutico , Tinidazol/farmacologia , Tinidazol/uso terapêutico , Mycoplasma genitalium/genética , Antibacterianos/farmacologia , Antibacterianos/uso terapêutico , Infecções por Mycoplasma/tratamento farmacológico , Farmacorresistência Bacteriana/genética
7.
Sex Transm Dis ; 50(4): 243-246, 2023 04 01.
Artigo em Inglês | MEDLINE | ID: mdl-36730040

RESUMO

ABSTRACT: We describe a case of persistent 5-nitroimidazole-resistant trichomoniasis cured after 14 days of oral secnidazole and intravaginal boric acid. Secnidazole may be an important treatment option for resistant trichomoniasis, particularly in women who fail other regimens, including higher doses of oral metronidazole and tinidazole for longer durations of time.


Assuntos
Tricomoníase , Vaginite por Trichomonas , Feminino , Humanos , Metronidazol/uso terapêutico , Tricomoníase/tratamento farmacológico , Tinidazol/farmacologia , Tinidazol/uso terapêutico , Vaginite por Trichomonas/tratamento farmacológico
8.
Anal Sci ; 39(6): 893-900, 2023 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-36807896

RESUMO

In this study, octanoic acid (OA) was used as an extraction solvent for the pre-concentration and determination of three antibiotic drugs (levofloxacin, metronidazole, and tinidazole) in urine samples. To extract the antibiotic drugs, a green solvent was used as the extraction solvent in the continuous sample drop flow microextraction method, followed by a high-performance liquid chromatography photodiode array detector. According to the findings, the present study offers an environmentally friendly analytical method with a high capacity for the microextraction of the antibiotic drugs at very low concentrations. The calculated detection limits were 6.0-10.0 µg/L and the linear range was found between 20 and 780 µg/L. The proposed method showed excellent repeatability with the RSD values ranging from 2.8 to 5.5%. The relative recoveries were between 79.0 and 92.0% in the urine samples with spiked levels of 40.0-100.0 µg/L for metronidazole and tinidazole, and 100.0-200.0 µg/L for levofloxacin.


Assuntos
Levofloxacino , Metronidazol , Solventes/química , Tinidazol , Antibacterianos
9.
Sex Transm Dis ; 50(6): 370-373, 2023 06 01.
Artigo em Inglês | MEDLINE | ID: mdl-36849257

RESUMO

BACKGROUND: The only drugs approved by the US Food and Drug Administration for oral treatment of trichomoniasis belong to the 5-nitroimidazole group. Most individuals infected with Trichomonas vaginalis can be cured with a standard treatment of metronidazole or tinidazole, but it is estimated that more than 159,000 people fail treatment each year. Although a minimal lethal concentration (MLC) corresponding to treatment failure has been reported for metronidazole, the MLC for tinidazole associated with treatment failure has not been determined. We conducted a study using T. vaginalis isolates from women with reported treatment success or failure to determine these values. METHODS: We measured MLCs of 47 isolates obtained from women who had failed metronidazole treatment, 33 isolates from women who had failed tinidazole treatment, and 48 isolates from women successfully cured with metronidazole. The cutoff was calculated as the 95th percentile of MLCs of susceptible isolates for each drug. RESULTS: Our data confirmed that the MLC previously associated with metronidazole treatment failure is ≥50 µg/mL and identified the MLC associated with tinidazole treatment failure as ≥6.3 µg/mL. For metronidazole, the agreement between laboratory result and treatment outcome was 93.7%; for tinidazole, this agreement was 88.9%. CONCLUSIONS: The T. vaginalis susceptibility assay is useful for determining whether 5-nitroimidazole treatment failure in persons with trichomoniasis can be attributed to drug resistance. These results are useful for establishing interpretive guidance of test results, and MLC levels can help guide appropriate patient treatment.


Assuntos
Tricomoníase , Vaginite por Trichomonas , Trichomonas vaginalis , Feminino , Humanos , Metronidazol/farmacologia , Metronidazol/uso terapêutico , Tinidazol/uso terapêutico , Vaginite por Trichomonas/tratamento farmacológico , Preparações Farmacêuticas , Resistência a Medicamentos , Tricomoníase/tratamento farmacológico , Falha de Tratamento , Técnicas In Vitro
10.
Dalton Trans ; 52(7): 2087-2097, 2023 Feb 14.
Artigo em Inglês | MEDLINE | ID: mdl-36692493

RESUMO

This paper describes the recognition process of tetrahedral [CuII(tnz)2X2] (X = Cl, Br) complexes by a DNA chain, analyzing the specific interaction between the DNA bases and backbone with the metal and the tinidazole (tnz) ligand. We identified the coordination of the copper metal center with one or two phosphates as the first recognition site for the tinidazole copper(II) complexes, while the ligands present partial intercalation into the minor groove. Also, we discuss a novel trigonal copper(I) tnz bromide complex, obtained by reducing the previously reported [Cu(tnz)2Br2]. This complex sheds light on the mechanism of action of tnz metal complexes as one of the most stable DNA-complex adducts depicts a trigonal geometry around the copper ion.


Assuntos
Complexos de Coordenação , Cobre , Tinidazol , Metais , DNA , Ligantes , Cristalografia por Raios X
11.
J AOAC Int ; 106(2): 309-315, 2023 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-36355444

RESUMO

BACKGROUND: Tinidazole (TIN) has amoebicidal, giardicidal, antifungal, and antimicrobial activities. It is marketed in the form of tablets. Analytical methods to assess the quality of TIN-based products are essential for correct pharmacotherapy. OBJECTIVE: The objective of this review is to show an overview of the existing analytical methods for evaluating TIN, according to the quality control (QC) analysis routine and green analytical chemistry (GAC). RESULTS: Official compendia show a method for evaluating TIN in tablets by nonaqueous titration, which has limitations (materials on the mg scale using solvents considered not recommended and harmful). The literature shows some analytical methods for evaluating TIN, both physicochemical and microbiological. The most used physicochemical method is UV (41%), and second is HPLC (28%). Among the microbiological methods, agar diffusion and turbidimetric methods are equally divided. The most studied matrix is TIN tablets (73%), and the most used solvent is methanol. CONCLUSIONS: The literature shows space for the development of analytical methods according to GAC for evaluating TIN, optimizing time, resources, and materials, reducing waste generation, and opting for less aggressive reagents, solvents, and diluents. HIGHLIGHTS: This review shows the status of analytical methods, both physicochemical and microbiological, for the analysis of TIN in pharmaceutical matrix, in the context of routine analysis of the chemical-pharmaceutical industries and of GAC.


Assuntos
Tinidazol , Antifúngicos , Cromatografia Líquida de Alta Pressão/métodos , Solventes , Comprimidos/análise , Tinidazol/análise
12.
Environ Res ; 215(Pt 2): 114262, 2022 12.
Artigo em Inglês | MEDLINE | ID: mdl-36100108

RESUMO

Antibiotics (tinidazole (TNZ)) in wastewater, exhibit adverse effects on humans and ecosystem. The current study was aimed to synthesize photocatalysts mrGO/BiOCl and mrGO/BiOCl/Ag. mrGO was coupled with BiOCl by hydrothermal method and Ag was deposited over it. The synthesized mrGO/BiOCl and mrGO/BiOCl/Ag were confirmed by Pzc analysis (5.5 and 4.4 for mrGO/BiOCl and mrGO/BiOCl/Ag, respectively), surface area analysis (380 m2 g-1, 227.7 m2 g-1, 220 m2 g-1 for mrGO, mrGO/BiOCl and mrGO/BiOCl/Ag respectively), elemental analysis (Ag, O, Bi, Fe), surface morphology (rough ball like sphere of mrGO/BiOCl and cubic Ag nanoparticles in mrGO/BiOCl/Ag), functional groups and band gap (Eg) determination. The Eg was determined using Kubelka-Munk equation as 3.5 and 2.8 eV for mrGO/BiOCl and mrGO/BiOCl/Ag respectively. During the adsorption study, the best experimental conditions for various operating parameters such as pH (2), contact time (5 min for mrGO/BiOCl and 10 min for mrGO/BiOCl/Ag under UV irradiation), TNZ concentration (18 µgL-1) and catalyst dosage (0.001 g) were achieved. Kinetic study revealed that both composites followed pseudo second order kinetics (R2 = 0.9979 and 0.9986, respectively). Data of rGO/BiOCl was fitted to Freundlich adsorption model (R2 = 0.9687) and rGO/BiOCl/Ag fitted to Langmuir adsorption model (R2 = 0.9994). Moreover, thermodynamic parameters confirmed that a photodegradation phenomenon was spontaneous and exothermic. The results confirmed that rGO/BiOCl and rGO/BiOCl/Ag are appropriate composites for TNZ removal from the aqueous environment with removal efficiency of 97 and 24%, respectively.


Assuntos
Nanopartículas Metálicas , Prata , Adsorção , Antibacterianos , Bismuto , Ecossistema , Grafite , Humanos , Fenômenos Magnéticos , Tinidazol , Águas Residuárias , Água
13.
Helicobacter ; 27(5): e12920, 2022 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-35939548

RESUMO

BACKGROUND: Resistance of Helicobacter pylori (H. pylori) to antibiotics is an evolving and dynamic process. Presence of antibiotic resistance impacts the success rate of initial eradication strategies in the clinic. AIM: To improve the success rate of initial eradication therapy and explore new antibiotic regimens, a large sample-based study utilizing antimicrobial susceptibility testing was performed. A total of 2508 H. pylori strains from patients subjected to initial eradication therapy were isolated, cultured, and tested for drug susceptibility from 2017 to 2021. The minimal inhibitory concentration (MIC) was recorded. H. pylori susceptibility profiles and its change trends from initial eradication patients were analyzed. The relationships between drug resistance, year of sample collection, age, and sex of patients were analyzed. RESULTS: The overall resistance rates were as follows: amoxicillin (9.25%), clarithromycin (38.48%), levofloxacin (42.86%), furazolidone (11.28%), doxycycline (8.56%), rifampicin (10.81%), tinidazole (74.32%), gatifloxacin (61.71%), tetracycline (0%), metronidazole (78.71%), ornidazole (97.87%), and fosfomycin (31.67%). Only 38.04% of the strains were pansusceptible to amoxicillin, clarithromycin, levofloxacin, and furazolidone, followed by those of mono resistance (29.90%), double resistance (24.96%), triple resistance (6.34%), and quadruple resistance (0.76%). Significant differences in the resistance rate and MIC were also observed in different age and sex groups. Time of collection and patient age and sex were associated with the distribution of antibiotic resistance. CONCLUSION: With the increasing resistance rate and multiple resistance of H. pylori to commonly used antibiotics, drug susceptibility testing is imperative to permit individualized therapy, and a regimen containing the combination of amoxicillin, furazolidone, tetracycline, doxycycline, or rifampicin is reasonable for initial empirical eradication therapy.


Assuntos
Fosfomicina , Infecções por Helicobacter , Helicobacter pylori , Mycobacterium tuberculosis , Ornidazol , Amoxicilina/farmacologia , Amoxicilina/uso terapêutico , Antibacterianos/farmacologia , Antibacterianos/uso terapêutico , Claritromicina/uso terapêutico , Doxiciclina/uso terapêutico , Farmacorresistência Bacteriana , Fosfomicina/uso terapêutico , Furazolidona/uso terapêutico , Gatifloxacina/uso terapêutico , Infecções por Helicobacter/tratamento farmacológico , Infecções por Helicobacter/epidemiologia , Humanos , Levofloxacino/uso terapêutico , Metronidazol/uso terapêutico , Testes de Sensibilidade Microbiana , Ornidazol/uso terapêutico , Rifampina , Tinidazol/uso terapêutico
14.
Microbiol Spectr ; 10(4): e0091222, 2022 08 31.
Artigo em Inglês | MEDLINE | ID: mdl-35863010

RESUMO

Infections with the sexually transmitted parasite Trichomonas vaginalis are normally treated with metronidazole, but cure rates are suboptimal and recurrence rates following treatment are high. Therefore, our objective was to assess the in vitro antitrichomonas activities of three other 5-nitroimidazole drugs and compare them with metronidazole. T. vaginalis isolates (n = 94) isolated from South African women presenting with vaginal discharge syndrome at two sexually transmitted disease clinics in KwaZulu-Natal were grown from frozen stock. Twofold serial dilutions (16 to 0.25 mg/L) of metronidazole, tinidazole, ornidazole, and secnidazole were prepared in Diamond's broth. The MICs were read after 48 h of anaerobic incubation at 37°C. An MIC of <2 mg/L was defined as susceptible, an MIC of 2 mg/L was defined as intermediate, and an MIC of >2 mg/L was defined as resistant. Sixty-one percent (57/94) of the T. vaginalis isolates were susceptible to metronidazole, 80% (75/94) were susceptible to tinidazole, 75% (71/94) were susceptible to secnidazole, and 89% (84/94) were susceptible to ornidazole. Resistance levels were 11%, 2%, and 1% for metronidazole, tinidazole, and secnidazole, respectively, while no resistance was observed for ornidazole. Intermediate scores were 28% for metronidazole, 18% for tinidazole, 24% for secnidazole, and 11% for ornidazole. Isolates from a proportion of women with bacterial vaginosis (BV) had higher MICs, and no isolates from women coinfected with another sexually transmitted infectious organism were resistant to any of the antimicrobials tested. This study showed that among T. vaginalis isolates in KwaZulu-Natal, there is no in vitro resistance to ornidazole. Of the 5-nitroimidazoles, metronidazole showed the highest level of resistance. The very low levels of resistance for the other three antimicrobials indicate that all three are viable options as a replacement for metronidazole if these in vitro findings are found to correlate with clinical outcomes. IMPORTANCE Trichomonas vaginalis is the most common nonviral sexually transmitted infection associated with reproductive sequelae and HIV acquisition risk worldwide. Despite its role in reproductive health, a high prevalence in South Africa, and the reported metronidazole resistance worldwide, no alternative regimens have been tested against T. vaginalis in our setting. This study compared the susceptibility patterns of three other 5-nitroiminazoles (secnidazole, tinidazole, and ornidazole), which are active against T. vaginalis with metronidazole in vitro. Metronidazole, the drug of choice for the treatment of trichomoniasis, showed the highest level of resistance, while the three regimens showed very low levels of resistance. These data indicate that all three are viable options as a replacement for metronidazole if these in vitro findings are found to correlate with clinical outcomes.


Assuntos
Nitroimidazóis , Ornidazol , Trichomonas vaginalis , Feminino , Humanos , Metronidazol/farmacologia , Metronidazol/uso terapêutico , Nitroimidazóis/farmacologia , Ornidazol/farmacologia , África do Sul , Tinidazol/farmacologia , Tinidazol/uso terapêutico
15.
Acta Crystallogr B Struct Sci Cryst Eng Mater ; 78(Pt 3 Pt 2): 490-498, 2022 Jun 01.
Artigo em Inglês | MEDLINE | ID: mdl-35702966

RESUMO

The crystal structures of bis[1-ethyl-6-fluoro-4-oxo-7-(piperazin-1-ium-4-yl)-1,4-dihydroquinoline-3-carboxylato]copper(II) sulfate heptahydrate, [Cu(C16H18FN3O3)2]SO4·7H2O or [Cu(nor)2]SO4·7H2O (nor is norfloxacin), and bis{1-[2-(ethylsulfonyl)ethyl]-2-methyl-5-nitroimide}dinitratocopper(II), [Cu(NO3)2(C8H13N3O4S)2] or [Cu(NO3)2(tnz)2] (tnz is tinidazole), were solved by X-ray diffraction. Both complexes crystallize in the space group P21/c, with Z = 4 (for nor) and Z = 2 (for ntz) molecules per unit cell. In [Cu(nor)2]SO4·7H2O, the CuII ion is at the centre of a square-planar environment, trans coordinated to two independent norfloxacin molecules in the zwitterionic form acting as bidentate ligands through one of the carboxyl (cbx) and the carbonyl (cb) O atoms. The solid is further stabilized by an extensive network of N-H...O(sulfate), N-H...O(cbx), N-H...OW, OW-H...O(sulfate) and OW-H...OW hydrogen bonds. The [Cu(NO3)2(tnz)2] complex is centrosymmetric, with the CuII ion in a square planar environment, coordinated to a tinidazole molecule acting as a monodentate ligand through its imidazole N atom and to one nitrate O atom. The vibrational FT-IR absorption spectra and thermal behaviour of the complexes were also studied and are briefly discussed based on the crystal structures.


Assuntos
Cobre , Tinidazol , Cobre/química , Cristalografia por Raios X , Ligantes , Estrutura Molecular , Norfloxacino , Pós , Espectroscopia de Infravermelho com Transformada de Fourier , Sulfatos , Difração de Raios X
16.
Water Sci Technol ; 85(12): 3357-3369, 2022 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-35771051

RESUMO

The cathode is the key component in the electro-peroxone process (E-Peroxone), which is popularly constructed with carbon materials. This study developed an innovative method to fabricate a cathode with waste-tire carbon (WTC) whose performance was evaluated for the degradation of tinidazole (TNZ), an antibiotic frequently detected in water. It was found that the addition of WTC in the cathode can significantly promote the yield of H2O2 and the current efficiency: around 2.7 times that of commercial carbon black at the same loading. The critical influencing factors were studied, including the current density, ozone concentration, initial pH value, chlorine ions and initial TNZ concentration. The scavenger tests demonstrated the possible involvement of •OH and O2•-. Some transformation products of TNZ were identified with UPLC-MS and the degradation pathway was proposed accordingly. These results demonstrated the potential of WTC for developing E-Peroxone cathodes.


Assuntos
Ozônio , Poluentes Químicos da Água , Carbono , Cromatografia Líquida , Eletrodos , Peróxido de Hidrogênio , Oxirredução , Espectrometria de Massas em Tandem , Tinidazol , Poluentes Químicos da Água/análise
17.
J AOAC Int ; 105(3): 675-687, 2022 Apr 27.
Artigo em Inglês | MEDLINE | ID: mdl-34918094

RESUMO

BACKGROUND: Helicobacter pylori infection is a common cause of peptic ulcer disease and dyspepsia. In addition, it may result in gastric cancer and gastric mucosa associated lymphoid tissue lymphoma. First-line therapy usually consists of triple therapy containing clarithromycin or amoxicillin, one of the proton pump inhibitors, and metronidazole or tinidazole. In addition to the triple therapy, an analgesic is required to relieve pain such as naproxen. OBJECTIVE: A sensitive and selective method needs to be developed and validated for simultaneous determination of four drugs (amoxacillin, tinidazole, naproxen and lansoprazole), used for treating Helicobacter pylori infection, in their combined dosage forms. METHODS: With the aid of experimental design, the cited drugs were separated and quantified. HPLC with a diode array detector was used and metronidazole, one of the drugs also used for treatment, was the internal standard (IS). A Thermo Scientific BDS Hypersil C18 column (5 µm, 250 mm x 4.6 mm) with mobile phase composed of acetonitrile-water (40 + 60, by volume), pH 5 adjusted with phosphoric acid, at 30°C was used for the separation of the cited drugs. RESULTS: The method was linear over the concentration ranges 10-500 µg/mL for amoxacillin, 10-350 µg/mL for tinidazole, 10-250 µg/mL for naproxen, and 2-20 µg/mL for lansoprazole. The proposed method was fully validated according to International Conference of Harmonization (ICH) guidelines. Statistical analysis revealed no significant difference between the results obtained and the four reference methods for the investigated drugs. CONCLUSION: The method can be easily implemented in QC studies of the cited drugs in their dosage forms. HIGHLIGHTS: Experimental design was applied using Plackett-Burman design for preliminary screening of factors followed by Box-Behnken design for chromatographic method optimization.


Assuntos
Antiulcerosos , Infecções por Helicobacter , Helicobacter pylori , Amoxicilina , Antibacterianos , Antiulcerosos/uso terapêutico , Cromatografia Líquida de Alta Pressão/métodos , Quimioterapia Combinada , Infecções por Helicobacter/tratamento farmacológico , Humanos , Lansoprazol/uso terapêutico , Metronidazol , Naproxeno/uso terapêutico , Omeprazol/farmacologia , Omeprazol/uso terapêutico , Projetos de Pesquisa , Tinidazol/farmacologia , Tinidazol/uso terapêutico
18.
Biomed Res Int ; 2021: 4171019, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34888378

RESUMO

Studies have shown that COX-2 expression is upregulated in gastric cancer (GC) as well as in precancerous lesions and in Helicobacter pylori-induced inflammation, suggesting that cyclooxygenase-2 (COX-2) may play an important role in gastric carcinogenesis. We attempted to investigate the role of clarithromycin with tinidazole on Helicobacter pylori-related gastritis from the aspects of clinical effect and COX-2 expression. From January 2016 to January 2019, 130 patients with Helicobacter pylori-related chronic gastritis were collected and grouped into the observation group (OG) and the control group (CG). Altogether, 80 patients in the OG were treated with clarithromycin with tinidazole, while 50 patients in the CG were treated with amoxicillin with metronidazole. Clinical symptom improvement time, content of COX-2 and B cell lymphoma-2 (BCL-2), content of inflammatory factors interleukin-1 (IL-1), IL-4, and C-reactive protein (CRP), expression level of nutritional indicators serum albumin (ALB), realbumin (PA), and transferrin (TF), clearance of Helicobacter pylori, total effective rate, and incidence of adverse reactions were detected. Compared with the CG, the OG had shorter clinical symptom improvement time, lower COX-2 and Bcl-2, lower expression of inflammatory factors IL-1, IL-4, and CRP, higher expression of nutritional indicators ALB, TF, and PA, higher clearance rate of Helicobacter pylori, higher total effective rate, and lower incidence of adverse reactions. Clarithromycin combined with tinidazole can effectively improve the clinical effect of Helicobacter pylori-related gastritis and reduce the expression level of COX-2.


Assuntos
Claritromicina/uso terapêutico , Ciclo-Oxigenase 2/metabolismo , Gastrite/tratamento farmacológico , Infecções por Helicobacter/tratamento farmacológico , Helicobacter pylori/efeitos dos fármacos , Tinidazol/uso terapêutico , Adulto , Amoxicilina/uso terapêutico , Antibacterianos/uso terapêutico , Quimioterapia Combinada/métodos , Feminino , Gastrite/metabolismo , Gastrite/microbiologia , Infecções por Helicobacter/metabolismo , Humanos , Masculino , Metronidazol/uso terapêutico , Estômago/metabolismo , Estômago/microbiologia , Neoplasias Gástricas/metabolismo , Neoplasias Gástricas/microbiologia
19.
Anal Methods ; 13(44): 5343-5350, 2021 11 18.
Artigo em Inglês | MEDLINE | ID: mdl-34730130

RESUMO

In this study, titanium nanotube electrodes were decorated with silver nanoparticles (AgNPs/TiO2NTs) and used as an electrocatalyst for the reduction of tinidazole. AgNPs/TiO2NTs are constructed by anodization of titanium sheet metal and photochemical deposition of AgNPs on TiO2NTs. The structural and elemental analysis characteristics of the AgNPs/TiO2NT electrode have been studied by scanning electron microscopy (SEM), energy dispersive X-ray spectroscopy (EDS), and X-ray diffraction (XRD) methods. Based on the cyclic voltammetric data, it has been confirmed that the AgNPs/TiO2NT electrode has good electrocatalytic activity to reduce tinidazole. Two liner concentration ranges of 0.2-55.0 µM and 55.0-111.2 µM were obtained by amperometric method. A detection limit of 60.9 nM was obtained for measuring tinidazole at the AgNPs/TiO2NT electrode surface. In addition, the designed sensor has been successfully used for quantitative measurement of tinidazole in pharmaceutical and human urine samples.


Assuntos
Nanopartículas Metálicas , Nanotubos , Humanos , Nanopartículas Metálicas/química , Nanotubos/química , Prata/química , Tinidazol , Titânio/química
20.
Clin Invest Med ; 44(3)2021 10 03.
Artigo em Inglês | MEDLINE | ID: mdl-34600464

RESUMO

Purpose: To investigate the therapeutic effects of minocycline combined with tinidazole in the treatment of chronic periodontitis (CP). Methods: Seventy-three CP patients treated May 2018­December 2019 at Yuyao People's Hospital (Yuyao, China) were enrolled in this study: 34 were treated with minocycline alone (control group; CG) and 39 were treated with a combination of minocycline and tinidazole (observation group; OG). Both groups were treated continuously for four weeks and plaque index (PLI), bleeding index (BI), periodontal pocket depth (PD), periodontal attachment level (PAL) and alveolar bone height were compared before and after treatment. Pain was evaluated using the visual analogue scale (VAS). Levels of TNF-α and IL-6 before and after treatment were determined using an enzyme-linked immunosorbent assay. Adverse reactions were compared. Results: In each group, PLI, BI, PD, PAL and alveolar bone height were lower after treatment (P<0.05), and those in OG were lower than those in CG (P<0.05). TNF-α and IL-6 levels in both groups were lower after treatment (P<0.05), and the levels in serum of the OG were lower than those of the CG (P<0.05). After treatment, the VAS in OG was lower than that of CG (P<0.05). There was no significant difference in adverse reactions between groups (P>0.05). Conclusion: Minocycline combined with tinidazole was more effective in treating CP than minocycline alone. This drug combination improved the periodontal indexes and inflammatory reaction of CP and relieved their pain. No significant difference in adverse reactions was seen.


Assuntos
Periodontite Crônica , Minociclina , Antibacterianos/uso terapêutico , Periodontite Crônica/tratamento farmacológico , Humanos , Minociclina/uso terapêutico , Tinidazol/uso terapêutico
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