Antibacterial Activity Of Ciprofloxacin Research Articles

Enhancement of the Antibacterial Activity of Ciprofloxacin against Staphylococcus aureus by 3-Alkyl Esters and 3-Aryl Esters of Hexahydroquinoline Derivatives

In this study, 3-alkyl and 3-aryl esters of hexahydroquinoline derivatives were screened for their ability to decrease bacterial resistance to ciprofloxacin (CAS 85721-33-1), which is extensively used to treat bacterial infections. A group of 3-alkyl and 3-aryl esters of hexahydroquinoline derivatives in which 2-aryl thiazole is substituted at 4-position were synthesized. The enhancement of the antibacterial activity of ciprofloxacin by these new synthetic compounds was evaluated against a resistant clinical strain of Staphylococcus aureus. The agar disk diffusion method was used to determine the antibacterial activity of different synthetic compounds in the absence and presence of ciprofloxacin. These results indicate that the antibacterial effect of ciprofloxacin is enhanced by two 3-alkyl esters of hexahydroquinoline derivatives (7b-3 and 7b-4).The enhancing effect of 7b-4 on the antibacterial activity of ciprofloxacin was greater than that of compound 7b-3. In comparison to the other synthetic compounds, 7b-4 showed a 5.61-fold increase of the inhibition zone on the ciprofloxacin supplemented plates. The result demonstrated that compounds 7b (3 and 4) could serve as valuable probes to study the structure-function relationships of agents that reverse the resistance to ciprofloxacin.

ZnO nanoparticles enhanced antibacterial activity of ciprofloxacin against Staphylococcus aureus and Escherichia coli

Nanoparticle metal oxides offer a wide variety of potential applications in medicine due to the unprecedented advances in nanobiotechnology research. In this work, the effect of zinc oxide (ZnO) nanoparticles prepared by mechano-chemical method on the antibacterial activity of different antibiotics was evaluated using disk diffusion method against Staphylococcus aureus and Escherichia coli. The average size of ZnO nanoparticles was between 20 nm and 45 nm. Although ZnO nanoparticles (500 microg/disk) decreased the antibacterial activity of amoxicillin, penicillin G, and nitrofurantoin in S. aureus, the antibacterial activity of ciprofloxacin increased in the presence of ZnO nanoparticles in both test strains. A total of 27% and 22% increase in inhibition zone areas was observed for ciprofloxacin in the presence of ZnO nanoparticles in S. aureus and E. coli, respectively. The enhancing effect of this nanomaterial on the antibacterial activity of ciprofloxacin was further investigated at three different contents (500, 1000, and 2000 microg/disk) against various clinical isolates of S. aureus and E. coli The enhancing effect of ZnO nanoparticles on the antibacterial activity of ciprofloxacin was concentration-dependent against all test strains. The most enhancing activities were observed in the contents of the 2000 microg/disk.

The physicochemical and antibacterial properties of Ciproflaxacin-Mg<sup>2*</sup> complex

Co-administration of quinolone antibiotics with cation-containing medicaments such as, antacids has been reported to influence the overall bioavailability leading to subtherapeutic plasma concentrations of these antibiotics in humans. The present work was designed to evaluate the binding constant, binding molar ratio, influence of temperature on the binding constant of ciprofloxacin-Mg2+ and to determine the antimicrobial activity of ciprofloxacin and ciprofloxacin-Mg2+. Job's method of continuous variation and Bonesi-Hildebrand equation were adopted to determine the molar ratio and stability constant respectively. The antibacterial activity was determined by the Agar diffusion method. A complexation molar ratio of 1:1 was obtained for ciprofloxacin-Mg2+ complex. The stability constants were 3.59 and 3.50 at 25 degrees C and 60 degrees C respectively. There was a significant difference between the zones of inhibition of ciprofloxacin-Mg2+ complex and that of ciprofloxacin alone against E. coli, P. aeruginosa, and S. aureus (p < 0.05). This difference showed that the complex formed was not as active as ciprofloxacin. The present studies have shown that ciprofloxacin readily complex with Mg2+ and that the stability constant was temperature dependent. The antibacterial activity of ciprofloxacin was markedly reduced in the presence of Mg2+. Concomitant administration of ciprofloxacin with Mg2. containing medicaments should be avoided to prevent resistance.

Aqueous solubility of ciprofloxacin in the presence of metal cations

Purpose: Though the complexation of ciprofloxacin with metal cations has been extensively studied, the effect of this complexation on the aqueous solubility of ciprofloxacin which is an important factor affecting drug distribution has not been well documented. We have thus set out in this study to investigate the aqueous solubility of ciprofloxacin in the presence of metal cations. Method: The measurements were done spectrophometrically after shaking ciprofloxacin alone or in the presence of varying amounts of different metal cations for five hours to attain equilibrium. The amount of ciprofloxacin in the saturated solution in each case was then measured spectrophotometrically Results: The solubility of ciprofloxacin in 0.05M H2SO4 at 37.0 ± 0.20C was 46.65 mgml-1 (0.12M). Except for magnesium sulphate, all the cations investigated progressively increased the aqueous solubility of ciprofloxacin. Ferrous ion had the greatest increase. It was followed by ferric, calcium and aluminium ions. Potassium and sodium ions had very slight increase in ciprofloxacin solubility. As the amount of magnesium sulphate increased, the aqueous solubility of ciprofloxacin increased slightly initially but then decreased progressively. Conclusion: The observed solubility profiles can be attributed to the type and extent of complexes formed between ciprofloxacin and the metal cations. This increase in the aqueous solubility of ciprofloxacin can have profound effect on the enteric absorption of ciprofloxacin and on its antibacterial activity when these metal cations are present, and may contribute to the observed poor availability and antibacterial activity of ciprofloxacin when co-administered with these cations. Keywords: Ciprofloxacin, aqueous solubility, ciprofloxacin-metal cation, interaction, antibacterial activity, gastrointestinal absorption.> Tropical Journal of Pharmaceutical Research Vol. 4 (1) 2005: pp. 349-354

Pharmacodynamics of trovafloxacin, ofloxacin, and ciprofloxacin against Streptococcus pneumoniae in an in vitro pharmacokinetic model.

An in vitro pharmacokinetic model was used to simulate the pharmacokinetics of trovafloxacin, ofloxacin, and ciprofloxacin in human serum and to compare their pharmacodynamics against eight Streptococcus pneumoniae strains. The MICs of ofloxacin and ciprofloxacin ranged from 1 to 2 micrograms/ml. Trovafloxacin was 8- to 32-fold more potent, with MICs of 0.06 to 0.12 microgram/ml. Logarithmic-phase cultures were exposed to peak concentrations of trovafloxacin, ofloxacin, or ciprofloxacin achieved in human serum after 200-, 400-, and 750-mg oral doses, respectively. Trovafloxacin was dosed at 0 and 24 h, and ofloxacin and ciprofloxacin were dosed at 0, 12, and 24 h. Human elimination pharmacokinetics were simulated, and viable bacterial counts were measured at 0, 2, 4, 6, 8, 12, 24, and 36 h. Trovafloxacin was rapidly and significantly bactericidal against all eight strains evaluated, with viable bacterial counts decreasing at least 5 logs to undetectable levels. Times to 99.9% killing were only 1 to 3 h. Although the rate of killing with ofloxacin was substantially slower than that with trovafloxacin, ofloxacin was also able to eradicate all eight strains from the model, despite a simulated area under the inhibitory curve/MIC ratio (AUC/MIC) of only 49. In contrast, ciprofloxacin eradicated only five strains (AUC/MIC = 44) from the model. Against the other three strains (AUC/MIC = 22), the antibacterial activity of ciprofloxacin was substantially diminished. These data corroborate clinical data and suggest that trovafloxacin has a pharmacodynamic advantage over ciprofloxacin and ofloxacin against S. pneumoniae in relation to its enhanced antipneumococcal activity.

Comparative Study of theIn VitroAntibacterial Activity of Ciprofloxacin and Thirteen other Antimicrobial Drugs with Respect to Recently Isolated Pathogens

The in vitro antibacterial activity of ciprofloxacin and 13 other antimicrobial drugs was evaluated with respect to 569 pathogens, mainly isolated from urine. Ciprofloxacin was found active in 96.1% of all of the Gram-positive and Gram-negative strains tested, amikacin in 90.6%, ceftazidime in 89.8%, ceftriaxone in 85.3%, piperacillin in 82.7%, tobramycin in 82.6%, gentamicin in 81.5%, aztreonam in 78.3%, nitrofurantoin in 72.6%, cotrimoxazole in 71.6%, cinoxacin in 71.0%, pipemidic acid in 70.6%, nalidixic acid in 66.7%, ampicillin in 50.1%. Ciprofloxacin was found to be the most active of the drugs studied against the bacterial strains which cause urinary, respiratory and other infections.

The in vitro and in vivo activity of ciprofloxacin

The antibacterial activity of ciprofloxacin (Bay o 9867) was compared with those of norfloxacin, nalidixic acid, trimethoprim-sulfamethoxazole, cefaclor, sisomicin and cefotaxime in in vitro and mouse protection studies. Approximately 300 clinical isolates of clinically important gram-positive and gram-negative species were used. The median MICs of ciprofloxacin against gram-positive and gram-negative bacteria ranged from less than or equal to 0.015-1 mg/l. Ciprofloxacin was 2-8 fold more active than norfloxacin and 100-fold more active than nalidixic acid. It also had a wider spectrum of activity against gram-positive organisms including even enterococci. No cross-resistance was observed between ciprofloxacin and beta-lactam antibiotics or aminoglycosides. Only acidic pH conditions decreased its activity. Ciprofloxacin showed rapid bactericidal action against organisms in both the logarithmic and stationary growth phases. In mouse protection studies (intraperitoneal infection) ciprofloxacin was significantly more effective than norfloxacin, ampicillin, trimethoprim-sulfamethoxazole, and also showed excellent activity against Pseudomonas infections.