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1.
Braz. J. Pharm. Sci. (Online) ; 58: e18630, 2022. tab, graf
Article in English | LILACS | ID: biblio-1364418

ABSTRACT

Abstract The objective of the present investigation was to design, optimize and characterize the gastro retentive floating levofloxacin tablets and perform in-vivo evaluation using radiographic imaging. The floating tablets were prepared by using polymers i.e hydroxy propyl methyl cellulose (HPMC-K4M) and carbopol-940 individually and in combination by nonaquous granulation method. All the Formulations were evaluated for swelling index (S.I), floating behavior and in-vitro drug release kinetics. The compatibility study of levofloxacin with other polymers was investigated by FTIR, DSC, TGA and XRD. Results from FTIR and DSC revealed no chemical interaction amongst the formulation components. The optimized formulation (F11) showed floating lag time (FLT), total floating time (TFT) swelling index (S.I) of 60 sec, >16h and approximately 75 %, respectively. Moreover, F11 showed zero order levofloxacin release in simulated gastric fluid over the period of 6 h. X-ray studies showed that total buoyancy time was able to delay the gastric emptying of levofloxacin floating tablets in rabbits for more than 4 hours. In conclusion the optimized formulation (F11) can be used for the sustained delivery of levofloxacin for the treatment of peptic ulcer.


Subject(s)
Drug Liberation , Peptic Ulcer/classification , Tablets/pharmacology , X-Rays/adverse effects , In Vitro Techniques/instrumentation , Spectroscopy, Fourier Transform Infrared , Drug Compounding/instrumentation , Process Optimization/analysis , Levofloxacin/analysis , Gastric Emptying/drug effects
2.
International Eye Science ; (12): 265-269, 2022.
Article in Chinese | WPRIM | ID: wpr-913035

ABSTRACT

@#AIM: To compare the clinical efficacy and safety of gatifloxacin eye drops and levofloxacin eye drops in the treatment of acute bacterial conjunctivitis using Meta-analysis.<p>METHODS: According to the Cochrane systematic evaluation method, “gatifloxacin” “levofloxacin” and “acute bacterial conjunctivitis” were used as keywords for literature search in Embase, Cochrane library, Pubmed, Medline, CNKI, Wanfang, VIP and CBMdisc from the establishment of the database to March 1, 2021. Randomized controlled trials(RCTs)gatifloxacin eye drops and levofloxacin eye drops in the treatment of acute bacterial conjunctivitis were included. Cochrane bias risk assessment tool was used to evaluate the quality of the included studies. RevMan5.3 software was used for combined analysis. Egger's test in Stata12 was used to assess publication bias, and the level of evidence was evaluated according to the GRADE system.<p>RESULTS: A total of 10 RCTs were included in this study with 1 149 patients. The control group was treated with levofloxacin and the experimental group was treated with gatifloxacin. The results of Meta-analysis showed that the clinical effective rate of acute bacterial conjunctivitis in gatifloxacin group was higher than that in levofloxacin group(<i>OR</i>=3.75, 95%<i>CI</i>: 2.52-5.58, <i>P</i><0.00001). Egger's test suggested there was publication bias among studies. And GRADE rating results indicated, the level of evidence was VERY LOW. The incidence of adverse drug reactions in the gatifloxacin group was lower than that in levofloxacin group(<i>OR</i>=0.37, 95%<i>CI</i>: 0.19-0.71, <i>P</i>=0.003). No publication bias was observed in Egger's test and GRADE showed the level of evidence was LOW.<p>CONCLUSION: Gatifloxacin eye drops is more effective than levofloxacin eye drops in the treatment of acute bacterial conjunctivitis, and has lower adverse effect rates. And due to the low levels of evidence included, more multicenter, randomized double-blind clinical trials are needed to improve the strength of evidence for the clinical efficacy of gatifloxacin eye drops in the treatment of acute bacterial conjunctivitis.

3.
Chinese Journal of Digestion ; (12): 103-110, 2022.
Article in Chinese | WPRIM | ID: wpr-934138

ABSTRACT

Objective:Taking clinical strains of Helicobacter pylori ( H. pylori) with different antimicrobial resistance as the research object, to explore the new genes related to the resistance of H. pylori to clarithromycin (CLA) and levofloxacin (LVX) based on whole-genome sequencing. Methods:From September 1st, 2016 to August 31st, 2019, 1 749 patients with upper gastrointestinal symptoms and positive 13C urea breath test who visited the Department of Gastroenterology and Hepatology, the University of Hong Kong-Shenzhen Hospital were enrolled. After gastric mucosal biopsy, H. pylori was isolated and cultured from gastric mucosa. Ninety H. pylori strains were successfully preserved. According to the results of in vitro drug sensitivity test, a total of 40 strains including 10 strains with single-drug resistance to CLA (CLA group), 10 strains with single-drug resistance to LVX (LVX group), 10 strains with dual-resistance to CLA and LVX (dual resistance group) and 10 strains sensitive to CLA, LVX, amoxicillin, furazolidone, tetracycline and metronidazole (all sensitive group) were screened out. By whole-genome sequencing and comparison to the comprehensive antibiotic research database (CARD), single nucleotide variations (SNV) and indels were analyzed, genes related to H. pylori resistance to CLA and LVX were screened out and the differences of new genes among 4 groups were analyzed. Independent sample t test, one-way analysis of variance, least significant difference method and chi-square test were used for statistical analysis. Results:Among the 4 groups there were no statistically significant differences in the number of SNV (74 952.00±8 755.21, 77 128.10±3 191.35, 78 639.90±601.23 and 77 474.60±2 421.05) and Indels (2 582.20±265.45, 2 653.60±108.37, 2 667.10±43.82 and 2 641.10±80.25) (all P>0.05). Compared to CARD, a total of 223 drug resistance-related genes were detected, of which 19 genes related to CLA mono-resistance in CLA group, 24 genes related to LVX mono-resistance in LVX group, 16 genes related to CLA mono-resistance, 14 genes related to LVX mono-resistance, and 12 dual resistance-related genes in dual resistance group, and 11 genes related to CLA mono-resistance, 17 genes related to LVX mono-resistance, and 13 dual resistance-related genes in all sensitive group. Among the genes related to CLA mono-resistance, the detection rates of erythromycin esterase gene ( ere)B in CLA group, LVX group, dual resistance group and all sensitive group were 0/10, 0/10, 3/10, 0/10, respectively, and the difference was statistically significant( χ2=5.79, P=0.049). The detection rate of erythromycin ribosomal methylase gene ( erm) family in CLA group and dual resistance group was higher than that in LVX group and all sensitive group (45.0%, 9/20 vs. 10.0%, 2/20), and the difference was statistically significant ( χ2=6.14, P=0.013). The detection rates of free methionine-(R)-sulfoxide reductase gene ( msrC) in CLA group, LVX group, dual resistance group and all sensitive group were 10/10, 7/10, 6/10, 4/10, respectively, and the difference was statistically significant ( χ2=8.97, P=0.030). Among the genes related to LVX mono-resistance, the detection rate of quinolone resistance pentapeptide repeat protein gene ( qnr) family in LVX group and dual resistance group was higher than that in CLA group and all sensitive group (60.0%, 12/20 vs. 25.0%, 5/20), and the difference was statistically significant ( χ2=5.01, P=0.025). The detection rates of qnrB4 in CLA group, LVX group, dual resistance group and all sensitive group were 1/10, 3/10, 7/10, 1/10, respectively, and the difference was statistically significant ( χ2=10.17, P=0.010). The number of efflux transporter genes related to CLA mono-resistance in 4 groups were less than those of LVX mono-resistance and dual drug resistance (11 vs. 29 and 11 vs. 23), and the differences were statistically significant ( χ2=11.87, 5.80; P=0.001, 0.016). The detected numbers of LVX resistance-related efflux transport genes in CLA group, LVX group, dual resistance group and all sensitive group were 28, 40, 24 and 27, respectively, and the difference was statistically significant ( χ2=10.26, P=0.016). Conclusions:Erm family and msrC may be important genes that mediate the resistance of H. pylori to CLA, and qnr family is related to mediating the resistance of H. pylori to LVX. Efflux transport genes may play a synergistic role in the process of drug efflux, and are more likely to mediate H. pylori resistance to LVX.

4.
Article in Chinese | WPRIM | ID: wpr-876163

ABSTRACT

Objective:To understand the trend of Helicobacter pylori (Hp) resistance to clarithromycin and levofloxacin and to provide guidance for Hp eradication therapy. Methods:From January 2014 to December 2018, a total of 66 515 patients with gastrointestinal symptoms were enrolled in the First People's Hospital of Wenling. The patients were divided into the following groups: childhood (0 to 6 years old); juvenile (7 to 17 years old); youth (18 to 40 years old),middle age (41 to 65 years old),and old age (≥66 years old). All patients received gastroscopy, gastric mucosal biopsy, Hp culture and drug sensitivity test of clarithromycin and levofloxacin. Results:The Hp positive rate showed a significant downward trend in 2016, 2017 and 2018 (χ2=14.317, 47.079, 88.054, all P<0.05). The average resistance rate of Hp to clarithromycin from 2014 to 2018 was 22.72% (4 732/20 831) showing an increasing trend, but the increase was slower after 2017. The average resistance rate to levofloxacin was 30.55% (6 364/20 831), and the overall trend showed a sharp rise from 2015 to 2017 (χ2=38.383, 49.569, both P<0.05), and a significant decline was detected after 2017 (χ2=18.841, P<0.05). The resistance rate of Hp to levofloxacin in patients increased with age. The clarithromycin resistance rate first decreased and then increased with age, and the resistance rate in old age (32.52%, 763/2 346) was higher than that in youth (22.09%, 1 086/4 916) and middle age patients (21.21%, 2 854/13 458), and the differences were significant (χ2=991.071, 144.968, both P<0.05). The resistance rate of Hp rose from 12.73% (14/110) in juvenile to 43.31% (1 016/2 346) in old age (χ2=228.867, P<0.05). Conclusion:In recent years, the positive rate of Hp infection in Wenling area has a decreasing trend. Although the resistance rate of Hp to clarithromycin and levofloxacin has been rising slowly or decreasing, it is still at a high level. In the selection of Hp eradication program, the differences between patients in different age groups should be considered with particular attention on the minors.

5.
International Eye Science ; (12): 2012-2017, 2021.
Article in Chinese | WPRIM | ID: wpr-887406

ABSTRACT

@#AIM:To investigate the main clinical features, pathogen distribution and drug sensitivity of lacrimal angiitis, and to provide evidence for clinical diagnosis and treatment.<p>METHODS:Retrospective study. A total of 45 patients(45 eyes)diagnosed with lacrimal angiitis in Hebei Eye Hospital from December 2016 to October 2020 were selected to analyze the general information, clinical manifestations and previous treatment history, bacterial culture results, and drug sensitivity test results.<p>RESULTS:All 45 patients had monocular disease, including 21 eyes with tears, increased secretion, conjunctival congestion in inner canthus, 14 eyes with red and swollen inner canthus, 6 eyes similar to eyelid cyst, and 4 eyes were found and diagnosed during routine preoperative examination. 27 eyes were previously diagnosed with other eye diseases, and the misdiagnosis rate was 60.0%. The positive rate of bacterial culture was 80.0%(36/45), Staphylococcus epidermidis was the most common, followed by Streptococcus; 52.8%(19/36)of the patients were infected with multidrug-resistant bacteria. The sensitivity rate of bacteria to fluoroquinolones(82.9%, 97/117)was higher than that of aminoglycosides(70.1%, 68/97)and cephalosporins(68.1%, 111/163). Except vancomycin, rifampicin, levofloxacin and chloramphenicol were highly sensitive to Gram-positive bacteria.<p>CONCLUSION: Staphylococcus epidermidis is the most common pathogen of dacryocystitis, followed by Streptococcus. Levofloxacin and rifampicin can be the first choice antibiotics for local anti-infection. Rational drug use can reduce the formation of multidrug-resistant bacteria. The cure rate can be improved by complete removal of stones by incision and plasty of lacrimal canaliculus.

6.
Article | IMSEAR | ID: sea-200531

ABSTRACT

Background: Drug-induced reproductive organs toxicities is an important aetiology in investigation of male infertility. The aim is to study levofloxacin effect on male reproductive system in comparison to ciprofloxacin.Methods: Twenty-five male wister rats weighted 230±20 gm and aged 8 weeks were randomly divided into five groups of five. The first group received ciprofloxacin with dose 78.23 mg/kg/day in 2 doses (therapeutic dose). The second group received the double dose of the first group ciprofloxacin. The third group received levofloxacin with dose 39.11 mg/kg/day once daily (OD) (therapeutic dose). The Fourth group received the double dose of the third group levofloxacin. However, the fifth group served as a control and received normal saline with carboxymethylcellulose OD. All treatments were administered orally for 14 days. On the 15th day, blood samples and reproductive organs were obtained from all rats. Testicular tissues were prepared for genetic testing and chemical and microscopical examination.Results: Ciprofloxacin and levofloxacin negatively altered reproductive organ weights, sperm parameters and serum follicle stimulating hormone (FSH) and luteinizing hormone (LH) level (p<0.05). Additionally, serum testosterone level was significantly deceased in ciprofloxacin-treated group (the double dose) (p<0.05) relative to control. The difference between ciprofloxacin and levofloxacin was significant in seminal vesicle weight and serum LH and FSH level (p<0.05). Testicular histopathological changes were also found with the two drugs with different degrees. Effects of levofloxacin and ciprofloxacin were dose-dependent.Conclusions: Both ciprofloxacin and levofloxacin adversely affect andrological function that should be monitored and controlled during application of these drugs.

7.
Chinese Pharmaceutical Journal ; (24): 451-456, 2020.
Article in Chinese | WPRIM | ID: wpr-857754

ABSTRACT

OBJECTIVE: To develop an UPLC-MS/MS method for simultaneous determination of 3 anti-tuberculosis drugs [isoniazid (INH) pyrazinamide (PZA) and levofloxacin(LFX)] in sputum by HPLC-MS/MS. METHODS The drugs(INH,PZAand LFX)were extracted by methanol/acetonitrile (V-V=1∶1). All of them separated on ACQUITY UPLC HSS T3 1.8 μm column (2.1 mm×100 mm,Waters Corporation) with the mobile phase of aqueous solution (containing 0.1% formic acid)-acetonitrile (containing 0.1% formic acid) at a flow rate of 0.35 mL•min-1. Multiple reaction monitoring (MRM) mode was performed combined with electrospray ionization source operating in the positive ionization mode. Furthermore, it was blindly collected 7 sputum samples, and analyzed the drug concentration by the built method in this work. RESULTS: The liner calibration curves of INHPZALFX were obtained in the concentration range of 48-6 000 ng•mL-1(r=0.998 8)480-60 000 ng•mL-1(r=0.999 3)120-15 000 ng•mL-1(r=0.999 5), respectively. The CV of intra- and inter-day precision was less than 15% and the absolute recovery was 97.21%-107.80%. In the 7 clinical samples, the concentration of INH is 44.74, 120.1, 301.5, 481, 595.5, 1 220 and 1 570 ng•mL-1, 104.2, 6 273.34 and 3 185 ng•mL-1 for PZA, and 199.86 for LFX, respectively. CONCLUSION: In this work, it is built a LC-MS method to simultaneously quantify INH, PZA and LFX, which is simple, sensitive and accurate. This method is successfully applied to analyze the clinical samples.

8.
Article in Chinese | WPRIM | ID: wpr-846024

ABSTRACT

Objective: To investigate the clinical efficacy of Xueniaoan Capsule combined with levofloxacin in the treatment of chronic bacterial prostatitis. Methods: A total of 126 patients with chronic bacterial prostatitis were randomly divided into control group (n = 60) and observation group (n = 66). The control group was treated with levofloxacin hydrochloride tablets (0.6 g/d, po) and the observation group was treated with Xueniaoan Capsule (4.2 g/d, po) combined with levofloxacin hydrochloride tablets (0.6 g/d, po). Both groups were continuously treated for eight weeks. The clinical efficacy of the two groups was evaluated through the NIH-CPSI score, prostatic fluid bacterial culture negative conversion rate, and serological parameters. Results: After treatment, the clinical efficacy in the control and treatment groups were 66.67% and 89.39%, respectively, and there were statistical differences between two groups (P < 0.05); Statistical analysis showed that the pain symptom score (5.45 ± 1.12), urination symptom score (3.31 ± 0.70) and quality of life score (3.08 ± 0.55) of NIH-CPSI scale in the observation group were significantly lower than those of the control group (P < 0.05); The negative conversion rate of prostatic fluid bacterial culture was 71.67% in the control group and 92.42% in the observation group, and the difference between the two groups had statistical significance (P < 0.05); The serum levels of interleukin-6 (IL-6), interleukin-8 (IL-8), and high-sensitivity C-reactive protein (hs-CRP) in the two groups were significantly lower than those before treatment (P < 0.05), while the levels of inflammatory factors in the observation group were significantly lower than those in the control group (P < 0.05). Conclusion: Xueniaoan Capsule combined with levofloxacin is effective in the treatment of chronic bacterial prostatitis, and can effectively relieve the clinical symptoms, improve the rate of prostatic fluid bacterial clearance, and reduce the level of serum inflammatory factors, which has a certain clinical application value.

9.
International Eye Science ; (12): 1680-1683, 2020.
Article in English | WPRIM | ID: wpr-825321

ABSTRACT

@#AIM:To evaluate the levofloxacin eye drop into human eye penetration, levofloxacin eye drop concentrations in human ocular aqueous of 33 patients undergoing cataract surgery were measured by high performance liquid chromatography(HPLC).<p>METHODS:Totally 33 volunteer patients who scheduled for phacoemulsification surgery received one drop of levofloxacin every 6h for 3d before and on the day of surgery, administration of drug was stopped 1h before surgery. Levofloxacin concentration in aqueous humor was measured by HPLC method with fluorescence detector. <p>RESULTS:A simple, effective and sensitive HPLC method for determination of levofloxacin in human ocular aqueous was validated. Linearity was shown for levofloxacin concentration over a wide range of 1.95×10-3-1.50 μg/mL. The mean aqueous level of levofloxacin was 0.3399±0.03405 μg/mL. <p>CONCLUSION:Results from the present study demonstrate that topical administration of levofloxacin 0.5% before cataract surgery with routine dose(one drop every 6h)unable to reach MIC90 for most common microorganism causing acute bacterial endophthalmitis.

10.
Infectio ; 23(4): 405-408, Dec. 2019. tab
Article in Spanish | LILACS, COLNAL | ID: biblio-1040011

ABSTRACT

Resumen Mujer quien inició tratamiento de rescate de segunda línea para Helicobacter pylori con levofloxacina un gramo cada 12 horas, amoxicilina 500 mg cada 8 horas y lansoprazol 40 mg cada 24 horas. Al quinto día de tratamiento manifestó mialgias generalizadas seguido por artralgias y limitación del movimiento en rodillas y codos. Al séptimo día, sin mejora, la paciente suspende la medicación y presenta resolución completa de los síntomas una semana después. No hubo secuelas, ni complicaciones, ni re-exposición al medicamento. El caso fue clasificado como probable, con un puntaje de siete en la escala de Naranjo. Este caso nos recuerda que la administración de fluoroquinolonas puede asociarse con artralgias y artropatía reversible aguda, y debería ser la primera sospecha diagnóstica en pacientes sin comorbilidad.


Abstract Woman who initiated second-line rescue therapy for Helicobacter pylori with levofloxacin one gram every 12 hours, amoxicillin 500 mg every 8 hours and lansoprazole 40 mg every 24 hours. On the fifth day of treatment, she manifested generalized myalgia followed by bilateral knee and elbow arthralgia with limitation of movements. On the seventh day, without improvement, the patient discontinues the medication and achieve complete resolution of the symptoms one week later. There were no sequelae, no complications, no re-exposure to the drug. The case was classified as probable attaining a score of seven under the Naranjo's scale. This case reminds us that administration of fluoroquinolones may be associated with arthralgia and acute reversible arthropathy and should be the first diagnostic suspicion in patients without comorbidity.


Subject(s)
Humans , Female , Helicobacter pylori , Arthralgia , Levofloxacin , Fluoroquinolones , Myalgia , Gastritis , Anti-Bacterial Agents , Anti-Bacterial Agents/adverse effects
11.
Article | IMSEAR | ID: sea-210515

ABSTRACT

Recommended and widely used first-line treatment of Helicobacter pylori consists of a proton pump inhibitor, clarithromycin, and amoxicillin/metronidazole. Recent reports suggest an increase in resistance to these antibiotics, especially to clarithromycin which has adversely affected the effectiveness of this standard regimen, hence levofloxacin containing regimens have also been introduced. Our objective was to assess the appropriateness of clarithromycin and levofloxacin containing regimens for H. pylori eradication by considering the factors such as dose, duration of treatment, patient medication adherence, and H. pylori induced symptom relief. In this prospective observational study, 120 patients were enrolled on the basis of H. pylori induced symptoms, positive campylobacter-like organism (CLO) test, or histology proven H. pylori infection. Besides socio-demographic characteristics, endoscopic findings, CLO test results and H. pylori induced symptom eradication were documented. Majority of the patients (85.83%) received an eradication regimen consisting of clarithromycin + amoxicillin + pantoprazole and the remaining patients were prescribed levofloxacin containing regimens. H. pylori eradication regimen containing clarithromycin was more effective in symptom control. Based on both symptom relief and a negative CLO test on treatment completion, only 40% of the patients received benefit from the regimens. Moreover, overall therapy was unsatisfactory due to inappropriate dose, duration, or sub-optimal adherence.

12.
Indian J Med Microbiol ; 2019 Sep; 37(3): 337-344
Article | IMSEAR | ID: sea-198910

ABSTRACT

Purpose: Helicobacter pylori causes various gastro-intestinal diseases. Antibiotic resistance to commonly used antibiotics for the treatment of H. pylori infection is the major cause for treatment failure. The aim of this study is to determine the antimicrobial susceptibility pattern for clarithromycin and levofloxacin and find the evolutionary relationship of the partial sequence of 23S rRNA and gyraseA gene of H. pylori by phylogenetic analysis. Materials and Methods: A total of 46 H. pylori strains were tested for clarithromycin and levofloxacin susceptibility pattern and phylogenetic tree were reconstructed by PhyML software. Results: In this study, we observed that only 6.5% of North-East Indian H. pylori strains were resistant for clarithromycin showing mutation at A2143G and T2182C positions of 23S rRNA gene. Resistance for levofloxacin was observed in 89.1% of the H. pylori strains showing mutations at asparagine to lysine at 87 and aspartic acid to glycine/tyrosine/asparagine at 91 positions of gyraseA gene. The phylogenetic tree of the partial sequence of 23S rRNA and gyraseA gene depicts that the North-East Indian strains falls in different cluster when compared to other countries. Conclusions: Resistance for clarithromycin was less in North-East Indian strains but high for levofloxacin indicating that first-line therapy may be best and effective for eradication of H. pylori in this region. This study is the first report that showed antibiotic susceptibility pattern for clarithromycin and levofloxacin by mutation analysis. By partial sequencing of 23s rRNA and gyraseA gene, we found that North-East Indian strains are geographically distinct.

13.
Article | IMSEAR | ID: sea-202331

ABSTRACT

Introduction: Various regimens have been used for H-pylorieradication. Sequential therapy is an alternative to classicaltriple therapy. This study was designed for evaluatingthe efficacy of levofloxacin based sequential therapyvs clarithromycin based sequential therapy in H-pylorieradication.Material and methods: It is a randomized clinical trial. Twohundred H. Pylori infected patients diagnosed by rapid ureasetest (RUT) on UGI endoscopy were randomly divided intotwo groups A and B. Group B Levofloxacin based sequentialregimen and group A clarithromycin based sequential regimen.H-pylori eradication status was evaluated with rapid ureasetest on UGI endoscopy 6 weeks after completion of sequentialtherapy.Results: As per protocol, eradication rates for group B and Awere 86% and 81% respectively. Eradication rate for H-pyloriis greater with levofloxacin based sequential therapy ascompared to that of clarithromycin based sequential therapybut it is not statistically significant p >0.05.Conclusion: Levofloxacin based sequential therapy has highereradication rate than clarithromycin based sequential therapy.Although not statistically significant in our study, levofloxacinbased sequential therapy could be better alternative forthe treatment of H-pylori in areas with high clarithromycinresistance.

14.
Braz. J. Pharm. Sci. (Online) ; 55: e18295, 2019. tab, graf, ilus
Article in English | LILACS | ID: biblio-1011644

ABSTRACT

Inorganic and carbon based nanomaterials are widely used against several diseases, such as cancer, autoimmune diseases as well as fungi and bacteria colonization. In this work, Santa Barbara Amorphous mesoporous silica (SBA), Halloysite Nanotubes (HNTs) and Multiwalled Carbon Nanotubes (CNTs) were loaded with fluoroquinolone Levofloxacin (LVF) to be applied as antimicrobial agents. The prepared via adsorption nanocarriers were characterized by Fourier-Transformed Spectroscopy, Scanning Electron Microscopy as well as High Pressure liquid Chromatography. In vitro release studies were carried out using Simulated Body Fluid at 37oC and data analyzed by various kinetic models showing slow dissolution over 12-24 hours. Antimicrobial studies showed improved antibacterial activity against Escherichia coli, Enterococcus faecalis, Listeria monocytogenes, Staphylococcus aureus, and Staphylococcus epidermidis compared to neat nanomaterials. CNTs were found to be the most promising candidates for LVF delivery and they were chosen to be further studied for their acute oral toxicity and histopathological examination using C57/Black mice. Histological examination depicted that drug loading did not affect mice organs morphology as well as hepatocyte degeneration, central vein degeneration and parenchymal necrosis scores. To conclude, the prepared nanomaterials present significant characteristics and can act as antimicrobial drug carriers; CNTs found to be safe candidates when orally fed to mice.


Subject(s)
Nanotubes/adverse effects , Nanostructures/analysis , Projects , Toxicity , Levofloxacin/agonists , In Vitro Techniques/classification , Anti-Infective Agents
15.
China Pharmacy ; (12): 1347-1351, 2019.
Article in Chinese | WPRIM | ID: wpr-816939

ABSTRACT

OBJECTIVE: To establish a method for the concentration determination of levofloxacin in rat plasma and compare the pharmacokinetic difference between Levofloxacin tablets and gastric floating sustained-release pellets in rats. METHODS: SD rats were randomly divided into Levofloxacin tablets group and Levofloxacin gastric floating sustained-release pellets group, with 6 rats in each group. They were given relevant medicine intragastrically 40 mg/kg (taking normal saline as solvent), and the blood samples 0.3 mL were collected before medication and 0.25, 0.5, 1, 2, 4, 8, 12, 24 h after medication. The plasma concentration of levofloxacin in rats was determined by UPLC. The determination was performed on Waters Acquity UPLC BEH C18 column with mobile phase consisted of 0.1% formic acid-acetonitrile (78 ∶ 22,V/V) at the flow rate of 0.3 mL/min. The detection wavelength was set at 294 nm, and column temperature was 40 ℃. The sample size was 2 μL. The pharmacokinetic parameters of rats were calculated by using DAS 3.0 software, and the difference between them were detected by F-test. RESULTS: The linear range of levofloxacin was 0.20-20.12 μg/mL, and limit of quantitation was 0.20 μg/mL. The limit of detection was 0.04 μg/mL. The intra-day and inter-day RSDs were less than 10%. The recoveries were all in line with the related requirements of quantitation analysis of the biological samples stated in 2015 edition of Chinese Pharmacopeia. Average drug concentration-time curves of single dose of Levofloxacin tablets group and Levofloxacin gastric floating sustained-release pellets group were all in line with two-compartment model after intragastric administration. The pharmacokinetic parameters cmax were (12.13±1.67) and (8.76±1.13) μg/mL; tmax were(0.86±0.15) and (2.48±0.45)h; t1/2β were(4.67±0.95) and (6.67±1.01)h; AUC0-t were (42.95±4.21) and (126.48±9.44) μg·h/mL; AUC0-∞ were (50.66±6.72) and (132.61±10.63) μg·h/mL, respectively. Compared with Levofloxacin tablets, cmax of Levofloxacin gastric floating sustained-release pellets were decreased significantly, and tmax, t1/2β, AUC and mean retention time were prolonged or increased significantly (P<0.05), and relative bioavailability was 294%. CONCLUSIONS: Established UPLC method is simple, specific, sensitive and precise, and can be used for the determination of levofloxacin concentration in rat plasma and its pharmacokinetic study. After levofloxacin is made into gastric floating sustained-release pellets, pharmacokinetic parameters are changed significantly, retention time is prolonged significantly and bioavailability is improved significantly.

16.
China Pharmacy ; (12): 1555-1558, 2019.
Article in Chinese | WPRIM | ID: wpr-816924

ABSTRACT

OBJECTIVE: To establish a method for the determination of levofloxacin concentration in human pleural effusion, to study its pharmaceutical characteristics. METHODS: Totally 6 patients with infectious pleural effusion received levofloxacin 0.4 g qd intravenous drip. Pleural effusion was collected at 0.5, 1, 2, 4, 8, 12 and 24 hours after administration. After treated with methanol precipitation protein, HPLC was used to determine the concentration of levofloxacin. The determination was performed on Agilent ZORBAX SB-C18 column with mobile phase consisted of methanol-0.02 mmol/L KH2PO4 buffer (containing 0.3% triethylamine, 70 ∶ 30, V/V at the flow rate of 1.0 mL/min. The detection wavelength was set at 294 nm, and the column temperature was 35 ℃. The sample size was 20 μL. The pharmacokinetic parameters were calculated with WinNonlin 5.2 software. RESULTS: Under this chromatogram condition, retention time of levofloxacin was about 4.9 min, the peak shape was good, the baseline was stable, and the determination of endogenous substances in pleural effusion had no interference. The linear range of levofloxacin were 0.625-20 μg/mL(R2=0.998 9). The relative recovery rates were (83.75±1.66)%-(87.73±2.43)% for low, medium and high concentration samples (n=3); RSDs of intra-day were 2.23%-4.96% (n=5); RSDs of inter-day were 4.10%-4.78%(n=5); the accuracy ranged (97.76±4.85)%-(100.87±2.25)%(n=5); RSD of concentration was no more than 5% in stability test (n=3) for low, medium and high quality control sample. The pharmacokinetic parameters of levofloxacin included cmax were (2.21±0.87) μg/mL; AUC0-24 h were (37.31±11.94) μg·h/mL; t1/2 were (4.50±0.21) h. CONCLUSIONS: Established method is simple, reliable and sensitive, and can be used for the determination of levofloxacin concentration in human pleural effusion and its pharmacokinetic study.

17.
International Eye Science ; (12): 1787-1790, 2019.
Article in Chinese | WPRIM | ID: wpr-750505

ABSTRACT

@#AIM: To compare the clinical curative effects of meibomian gland dysfunction(MGD)caused by evaporative dry eye by utilizing levofloxacin eye gel and Tobramycin and Dexamethasone Ophthalmic Ointment, respectively.<p>METHODS: The 180 cases(360 eyes)with dry eye(evaporative type)caused by confirmed meibomian gland dysfunction were randomly divided into two groups(<i>i.e.</i> A and B): In group A, 90 individuals with 180 eyes were treated with levofloxacin eye gel+ sodium hyaluronate eye solution; The other 90 cases in group B took Tobramycin and Dexamethasone Ophthalmic Ointment+ sodium hyaluronate eye drops for curing the MGD. In addition, the same comprehensive therapy were used to the MGD patients in groups A and B, after surface anesthesia on binoculus, secretion, obstructing meibomian gland secretions, were discharged by utilizing cotton stick to extrusion mass weekly and four times consecutive treatments were regard as a course of treatment. To remove residual the thin oil soften lipid in meibomian gland, heat can be applied to the eyelids with hot water(around 45℃)on towel for 15min and do that three times a day. After each hot compress, we use levofloxacin eye gel to the patients in group A by dropping into the conjunctival sac and apply to the root of the eyelid lashes. The group B of 90 patients were applied Tobramycin and Dexamethasone Ophthalmic Ointment to the root of the eyelid lashes. All patients were dripped odium eye drops eye into their eyes four times a day. <p>RESULTS: After treatment(<i>Z</i>= -0.64, <i>P</i>=0.524), there were no significant differences in clinical symptoms(<i>Z</i>= -1.37, <i>P</i>=0.171), secretion characteristics(<i>Z</i>= -1.06, <i>P</i>=0.288), tear film rupture time and tear secretion time between groups A and B(<i>P</i>>0.05). Corneal fluorescence staining score: group A(cured 83.3%, improved 11.1%, ineffective 5.6%)and group B(cured 55.6%, improved 27.8%, ineffective 16.7%). The therapeutic effect of group A was better than that of group B, with statistical significance(<i>Z</i>= -4.02, <i>P</i><0.001).<p>CONCLUSION: Physical therapy for meibomian gland dysfunction caused by evaporative dry eye is given priority, and medication is treated as adjunctive therapy. Generally, the patients can achieve totally anti-inflammatory, antibacterial, safe and stable, without side effects by using levofloxacin eye gel. However, the patients with worst condition and lingering illness should cured by Tobramycin and Dexamethasone Ophthalmic Ointment. In addition, statistical significant difference is not found between the two drugs on curative effects.

18.
Rev. am. med. respir ; 18(2): 111-115, jun. 2018. tab
Article in Spanish | LILACS | ID: biblio-957572

ABSTRACT

Introducción: Con frecuencia las fluoroquinolonas integran los esquemas de tratamiento de tuberculosis, tanto en aquellos con enfermedad multirresistente (parte esencial de la prescripción), como también en individuos con tuberculosis sensible e intolerancia a drogas de primera línea. Objetivos: Evaluar cuáles fueron las indicaciones para incluir fluoroquinolonas en el tratamiento antituberculosis y describir los eventos adversos relacionados con su utilización. Materiales y Métodos: Se realizó un análisis retrospectivo de pacientes que iniciaron tratamiento para tuberculosis entre el 1 de enero de 2014 y el 31 de diciembre de 2016. Definimos evento adverso como aquella condición que derivó en la suspensión de un medicamento o la necesidad de utilizar drogas específicas para su manejo. Se utilizó la prueba de c2 para las comparaciones entre grupos. Resultados: Entre los 267 pacientes que iniciaron tratamiento en el período descripto, recibieron fluoroquinolonas 24 individuos (11 hombres) representando el 9% del total; 19 se trataron con moxifloxacina 400 mg/día y el resto con levofloxacina 750 mg/día. Comparando los grupos con fluoroquinolonas vs. sin fluoroquinolonas, no hubo diferencias significativas en el porcentaje de participantes de sexo masculino (46 vs. 58%), edad (34.7 ± 12 vs. 35.1 ± 15 años), afectación pulmonar (58 vs. 68%) y proporción de abandonos (26 vs. 21%). Hubo una mayor proporción de argentinos en el grupo con fluoroquinolonas vs. sin fluoroquinolonas (71 vs. 44%, p = 0.012) y de individuos VIH positivos (46 vs. 8.6%, p < 0.05). Se indicaron fluoroquinolonas en reemplazo de rifampicina en 9 pacientes (37.5%) debido a la interacción de ésta con antirretrovirales, en 9 (37.5%) por intolerancia y en 5 (21%) por resistencia a anti TB de primera línea, en 1 por el antecedente de cirrosis (en lugar de pirazinamida). El tiempo de tratamiento con fluoroquinolonas fue de 203 ± 158 días (rango 30-660) sin observarse eventos adversos relacionados con su uso. Conclusión: En el grupo examinado el uso de fluoroquinolonas no se asoció a eventos adversos, siendo las indicaciones más frecuentes en estos pacientes las interacciones medicamentosas en pacientes VIH positivos y la intolerancia a las drogas de primera línea.


Introduction: The floroquinolones are frequently used in the treatment regimes for tuberculosis (TB) in both those with multidrug-resistant TB (MDR-TB), where it forms an essential part of the regimen, as well as intolerance to first-line drugs in the TB sensitive. Objectives: To evaluate the indications to include floroquinolones in TB treatment and to describe the adverse events associated with its use. Materials and Methods: A retrospective analysis of the patients who began treatment for TB between 1 January 2014 and 31 December 2016 was performed. We define adverse event as that condition that results in the suspension of a medicine or the need to use specific drugs for its management. Group characteristics were comparing by using c2 test. Results: Among the 267 patients who began treatment in the period described, 24 (11 men) received fluoroquinolones representing 9% of the total: 19 moxifloxacin 400 mg/day and the rest levofloxacin 750 mg/day. Comparing the groups with fluoroquinolones vs. without fluoroquinolones, there were no significant differences in the percentage of men (46 vs. 58%), age (34.7 ± 12 vs. 35.1 ± 15 years), pulmonary involvement (58 vs. 68%), and proportion of dropouts (26 vs. 21%). There was a higher proportion of Argentines in the group with fluoroquinolones vs. without fluoroquinolones (71 vs. 44%, p = 0,012) and HIV-positive (46 vs. 8.6%, p < 0.05). Fluoroquinolones were indicated in replacement of rifampicin in 9 patients (37.5%) due to the interaction with antiretroviral drugs, in 9 (37.5%) by intolerance and in 5 (21%) for resistance to first-line anti-TB drugs, in 1 by the history of cirrhosis (instead of pyrazinamide). The time of treatment with fluoroquinolones was 203 ± 158 days (range 30-660) with no observed adverse events related to its use. Conclusion: The use of fluoroquinolones was not associated with adverse events in the group of patients studied, drug interactions in HIV positive patients and the intolerance to first-line drugs were the most frequent indications in the studied group.


Subject(s)
Tuberculosis , Fluoroquinolones , Levofloxacin
19.
Rev. am. med. respir ; 18(2): 116-120, jun. 2018. tab
Article in English | LILACS | ID: biblio-957573

ABSTRACT

Introduction: Fluoroquinolones are frequently used in treatment regimes for tuberculosis both in cases of multidrug-resistant tuberculosis, where they are an essential part of the regime, and also in cases of drug-sensitive tuberculosis with intolerance to first-line drugs. Objectives: To evaluate indications to include fluoroquinolones in the anti-tuberculosis treatment and to describe the adverse events associated with their use. Materials and Methods: A retrospective analysis of the patients who began treatment for tuberculosis between January 1, 2014 and December 31, 2016 was performed. We defined an adverse event as the condition that resulted in the suspension of a drug or the need to use specific drugs for its management. Group characteristics were compared by using the c2 test. Results: Of the 267 patients who began treatment in said period, 24 (11 men) received fluoroquinolones, representing 9% of the total population; 19 were treated with 400 mg/day of moxifloxacin and the rest with 750 mg/day of levofloxacin. In the comparison of the groups receiving fluoroquinolones versus the ones without fluoroquinolones, there were no significant differences in the percentage of male participants (46 vs. 58%), age (34.7 ± 12 vs. 35.1 ± 15 years), pulmonary involvement (58 vs. 68%) and withdrawal rate (26 vs. 21%). There was a higher proportion of Argentinians (71 vs. 44%, p = 0.012) and of HIV-positive individuals (46 vs. 8.6%) p < 0.05) in the group with fluoroquinolones vs. the group without fluoroquinolones. Fluoroquinolones were indicated in replacement of rifampicin in 9 patients (37.5%) due to its interaction with antiretroviral drugs, in 9 patients (37.5%) due to intolerance, and in 5 patients (21%) due to resistance to first-line anti-tuberculosis drugs. In one individual, fluoroquinolones were indicated instead of pyrazinamide due to history of cirrhosis. The time of treatment with fluoroquinolones was 203 ± 158 days (range 30-660) with no observed adverse events related to their use. Conclusion: In the group under study, the use of fluoroquinolones was not associated with adverse events. The most frequent indications in these patients were drug interactions in HIV-positive patients and intolerance to first-line drugs.


Subject(s)
Tuberculosis , Fluoroquinolones , Levofloxacin
20.
Med. interna Méx ; 34(1): 89-105, ene.-feb. 2018. tab, graf
Article in Spanish | LILACS-Express | LILACS | ID: biblio-976049

ABSTRACT

Resumen: Las quinolonas o fluoroquinolonas son un grupo de antibióticos frecuentemente prescritos y de amplio espectro que actúan inhibiendo a las enzimas encargadas de la replicación, transcripción, reparación y recombinación del ADN bacteriano. El objetivo de este artículo es presentar una revisión sistemática de los antecedentes, farmacocinética y actividad microbiológica de las tres fluoroquinolonas más representativas en nuestro medio (ciprofloxacino, levofloxacino y moxifloxacino) en sus tres indicaciones actualmente autorizadas: infecciones de vías respiratorias inferiores, de vías urinarias, de piel y tejidos blandos.


Abstract: Quinolones or fluoroquinolones are a group of commonly prescribed and broad-spectrum antibiotics drugs that act by inhibiting the enzymes responsible for the bacterial DNA replication, transcription, repair and recombination. The aim of this article is to present a systematic review of the three most representative fluoroquinolones in our country (ciprofloxacin, levofloxacin and moxifloxacin) in their three authorized indications: lower respiratory tract infections, urinary tract infections, skin and soft tissues infections.

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