Penetration of 0. 3% ciprofloxacin, 0. 3% ofloxacin, and 0. 5% moxifloxacin into the cornea and aqueous humor of enucleated human eyes

We aimed to quantify the penetration of ciprofloxacin, ofloxacin, and moxifloxacin into the cornea and aqueous humor of cadaver eyes. A total of 60 enucleated eyes, not eligible for corneal transplantation, were divided into three groups and immersed in commercial solutions of 0.3% ciprofloxacin, 0.3% ofloxacin, or 0.5% moxifloxacin for 10 min. Whole corneas and samples of aqueous humor were then harvested and frozen, and drug concentrations analyzed by liquid chromatography tandem mass spectrometry. The mean corneal concentration of moxifloxacin was twice as high as ofloxacin, and the latter was twice as high as ciprofloxacin. The mean concentration of moxifloxacin in the aqueous humor was four times higher than the other antibiotics, and the mean concentrations of ciprofloxacin and ofloxacin were statistically similar. The amount of drug that penetrated the anterior chamber after a 10-min immersion was far below the safe limit of endothelial toxicity of each preparation. Moxifloxacin demonstrated far superior penetration into the cornea and anterior chamber of cadaver eyes compared to ciprofloxacin and ofloxacin. One should not expect endothelial toxicity with the commercial eye drops of ciprofloxacin, ofloxacin, and moxifloxacin that reach the anterior chamber through the cornea.

Development and evaluation of bilayer tablets of combination of antibiotics for the treatment of sexually transmitted disease

ABSTRACT The present research work was envisaged to develop bilayer tablets to improve therapeutic efficacy of antibiotic combination for the treatment of sexually transmitted diseases. The combination of two antibiotics i.e. cefixime trihydrate and ofloxacin were used for the preparation of bilayer tablets which act against genito-urinary infections. The formulations comprise of cefixime trihydrate as immediate release layer formulated using different superdisintegrants and ofloxacin as extended release layer containing HPMC K100M. Evaluation of bilayer tablets were performed for the immediate release cefixime layer and sustain release ofloxacin layer with optimization of excipients. The immediate release layer of cefixime showed complete release within 30 min and ofloxacin release was extended up to 24 hours. The similarity factor value of ofloxacin sustained release layer was found to be 87.01 for initial and 80.35 after 3 months stability when compared with marketed reference product. The present study revealed that cefixime trihydrate and ofloxacin bilayer tablets were successfully developed for the use against sexually transmitted infections.

Interaction study between levofloxacin and omeprazole using urinary pharmacokinetic data

The objective of this study was to observe the drug interaction between levofloxacin and omeprazole using urinary excretion data. Levofloxacin tablet and omeprazole capsule were administered separately as well as in combination in fasting condition with a wash out period of two weeks after each administration. Urine was collected at different time intervals of 0, 0-2, 2-4, 4-8, 8-12, 12-24, 24-36 and 36-48 hr post-dose and analyzed using a validated HPLC with UV detection. Different pharmacokinetic parameters for both drugs were determined using non-compartmental method. The maximum rate of excretion [R[max]] of levofloxacin was not decreased significantly when co-administered with omeprazole [p>0.05]. Similarly no significant difference [p = 0.350] was observed for R[max] of omeprazole when co-administered with levofloxacin. Again the fraction of levofloxacin excreted [f[e]/f] was not changed significantly [p = 0.953] due to the co-administration of omeprazole. Similarly fraction of omeprazole excreted [f[e] /f] also remained unaffected [p = 0.672] when co-administered with levofloxacin. No significant change was observed for the area under the rate of excretion versus midpoint of time interval curve from zero to 48 hours [AURC[0-48] for levofloxacin and omeprazole [p = 0.816 and 0.792 respectively] when administered separately and co-administered with each other. The study clearly revealed that levofloxacin and omeprazole do not undergo any kind of interactions when administered together. So it can be concluded that these two drugs can be prescribed together to achieve optimum therapeutic activity

Novel in vitro pharmacodynamic model simulating ofloxacin pharmacokinetics in the treatment of Pseudomonas aeruginosa biofilm-associated infections

The conventional in vitro models simulate pharmacodynamics of antibiotics in the treatment of planktonic Pseudomonas aeruginosa. In this study, we propose a novel pharmacodynamic model of ofloxacin activity in the treatment of P. aeruginosa biofilm. P. aeruginosa biofilm carrying coupons were suspended in a continuous flow central compartment bioreactor [CCB]. In the CCB, the pharmacokinetics of different ofloxacin dosing regimens were simulated. Samples from the coupons and the CCB were assessed for viability of the biofilm and the shedding planktonic cells, respectively, over 24 h. In addition, ofloxacin concentrations were assessed in each sample withdrawn for the CCB using bioassay method. The microbiological outcomes on P. aeruginosa biofilm and the shedding planktonic cells in response to different ofloxacin dosing regimens were not parallel and this may explain the non-coincidence of microbiological and clinical outcomes with biofilm associated infections. The current study has introduced unprecedented novel dynamic model for the assessment of the microbiological outcome on both biofilm and shedding planktonic cells of P. aeruginosa in response to different dosing regimens of ofloxacin which in turn can simulate the clinical outcomes in biofilm associated infections of P. aeruginosa, e.g. cystic fibrosis. Furthermore, different scenarios of antibiotic dosing regimens against biofilm related infections can be mimicked using such model

Pharmacokinetics, tissue residue and plasma protein binding of ofloxacin in goats

Ofloxacin was administered to six male goats intravenously (5 mg/kg) to determine its kinetic behavior, tissue residue, in vitro plasma protein binding and to compute a rational dosage regimen. The concentration of ofloxacin in plasma and tissue samples collected at prescheduled time were estimated by using HPLC. The pharmacokinetic parameters were determined by non-compartmental model and plasma protein binding was estimated by equilibrium dialysis technique. The therapeutic concentration (> or = 0.5 microgram/ml) was maintained up to 36 h and the initial concentration at 2.5min (14.76 +/- 0.47 microgram/ml) declined to 0.05 +/- 0.03 microgram/ml at 96 h with a secondary peak (0.64 +/- 0.15 microgram/ml) at 24 h. The mean AUC, AUMC, t1/2, MRT, Cl and Vd were calculated to be 58.94 +/- 19.43 microgram h/ml, 1539.57 +/- 724.69 microgram h2/ml, 15.58 +/- 1.87 h, 22.46 +/- 2.71 h, 135.60 +/- 31.12 ml/h/kg and 2.85 +/- 0.74 L/kg respectively. Significantly high concentration of drug was detected in different tissues after 24 h of intravenous dosing of 5mg/kg, at 24 h interval for 5 days. The in vitro plasma protein binding of ofloxacin was found to be 15.28 +/- 0.94%. Based on these kinetic parameters, a loading dose of 5mg/kg followed by the maintenance dose of 3mg/kg at 24 h dosing interval by intravenous route is recommended.

novel HPLC method for the determination of levofloxacin in blood and its bioequivalence studies

Bioequivalence study was performed for Levofloxacin Tablets 250mg. For this purpose one reference formulation manufactured in Pakistan, by a local Pharmaceutical Company which is also a brand leader, was compared with test formulation manufactured by another Pharmaceutical Industry. The study was formated in accordance to the draft guidance provided by FDA [CDER] for biovailability and bioequivalence studies. The test formulation was administered orally, in fasting state, to 7 healthy volunteers and the blood samoles were drawn at appropriate intervals upto 30hrs, Reference product [Cravit] was administered to the same group of volunteer after a wash out period of one week. Samples were analysed on HPLC for the determination of drug conncentrations. The Pharmacokinetic parameter such as Cmax, Tmax and AUC were calculated. The data generated was analysed statistically by ANOVA and paired t test. Results of Pharmacokinetic parameter indicated that both products Test [A] and Reference [B] are bioequivalent. Statisyical analysis supports this conclusion

Oral levofloxacin in the treatment of community-acquired pneumonia

We evalueted the efficacy of oral levofloxacin (500mg/day for 7-21 days) in the treatment of adults patients with community-acquired pneumonia (CAP) requiring hospitalization in an open prospective stydy. The microbiological cause of the pneumonia was identified in 14/20 patients using lower respiractory tract secretions obtained by bronhoscopy (12) and/or blood culture (2). Eight patients has S.pneumoniae, 2 P.aeruginosa, 1 H.influenzae, 1 S.aureus, 1 mixed S.aureus and K.pneumoniae, and 1 E.coli and Grp.D Streptococcus. All of the patients evaluated were judged to be improved or cured. Levofloxacin is an additional option as monotherapy for the treatment of CAP.

Infecciones respiratorias adquiridas en la comunidad: relación con agentes etiológicos y antibióticos con especial atención a levofloxacino / Community acquired respiratory infections: relationship to causal agents and antibiotics with special focus on levofloxacine

Los microorganismos involucrados en infecciones del tracto respiratorio alto y bajo, incluyen tanto bacterias "típicas" tales como Streptococcus pneumoniae, Haemophilus influenzae, Streptococcus pyogenes y Moraxella catarrhalis, y bacterias "atípicas", como Mycoplasma pneumoniae, Chlamydia pneumoniae y Legionella pneumophila. El primer grupo ha adquirido resistencia, tanto a nivel mundial como nacional, a los antimicrobianos de uso habitual en el tratamiento de estas infecciones, como son penicilina, ampicilina, cotrimoxazol, cefuroxima y cefotaxima, entre otros. Debido a lo anterior, se han desarrollado nuevas moléculas siendo una de ellas levofloxacino, una nueva quinolona, levoisómero de D-L racemato de ofloxacino. Este compuesto posee un amplio espectro "in vitro" contra bacteria Gram positivas, incluyendo S. pneumoniae resistente a penicilina, bacterias Gram negativas, bacterias atípicas y algunas bacterias anaerobias. Su biodisponibilidad en forma oral es de 100 por ciento. Es metabolizada en el hígado y su excreción a nivel renal es de 80 por ciento. En estudios clínicos levofloxacino ha demostrado eficacia y seguridad incluso con erradicación microbiológica demostrada en infecciones respiratorias adquiridas en la comunidad, lo que la convierte en una alternativa real de tratamiento

Estudo comparativo entre lomefloxacina e ofloxacina no tratamento da prostatite bacteriana crônica / Clinical trial comparing lomefloxacin and ofloxacin in the treatment of chronic bacterial prostatitis

Foram tratados 33 pacientes com prostatite bacteriana crônica, sintomáticos, diagnosticados pelo método de Meares-Stamey, com lomefloxacina 400 mg, uma vez ao dia, ou ofloxacina 200 mg, duas vezes ao dia, num estudo randomizado, por um período de 42 dias. Todos os microorganismos eram sensíveis a ambas as drogas. Os pacientes foram seguidos por seis meses com exames bacteriológicos de urina e líquido prostático pelo método descrito. Após seis meses a taxa de cura foi de 66,6 por cento para lomefloxacina e 60 por cento para ofloxacina. Nenhum paciente com infecçäo causada por P. aeruginosa foi curado e sem computar estes pacientes a taxa de cura seria 70,5 por cento e 64 por cento, respectivamente. Os efeitos colaterais observados foram em pequeno número e de pequena intensidade, em nenhuma ocasiäo obrigando à suspensäo do tratamento. Ambas as fluoroquinolonas se mostraram eficientes no tratamento desta difícil infecçäo bacteriana. A lomefloxacina, que pode ser administrada em dose única, provavelmente é mais prática para o paciente e resulta em melhor aderência a este longo tratamento