Pharmacokinetics Of Levofloxacin Research Articles

Assessing potential drug-drug interactions between clofazimine and other frequently used agents to treat drug-resistant tuberculosis.

Clofazimine is included in drug regimens to treat rifampicin/drug-resistant tuberculosis (DR-TB), but there is little information about its interaction with other drugs in DR-TB regimens. We evaluated the pharmacokinetic interaction between clofazimine and isoniazid, linezolid, levofloxacin, and cycloserine, dosed as terizidone. Newly diagnosed adults with DR-TB at Klerksdorp/Tshepong Hospital, South Africa, were started on the then-standard treatment with clofazimine temporarily excluded for the initial 2 weeks. Pharmacokinetic sampling was done immediately before and 3 weeks after starting clofazimine, and drug concentrations were determined using validated liquid chromatography-tandem mass spectrometry assays. The data were interpreted with population pharmacokinetics in NONMEM v7.5.1 to explore the impact of clofazimine co-administration and other relevant covariates on the pharmacokinetics of isoniazid, linezolid, levofloxacin, and cycloserine. Clofazimine, isoniazid, linezolid, levofloxacin, and cycloserine data were available for 16, 27, 21, 21, and 6 participants, respectively. The median age and weight for the full cohort were 39 years and 52 kg, respectively. Clofazimine exposures were in the expected range, and its addition to the regimen did not significantly affect the pharmacokinetics of the other drugs except levofloxacin, for which it caused a 15% reduction in clearance. A posteriori power size calculations predicted that our sample sizes had 97%, 90%, and 87% power at P < 0.05 to detect a 30% change in clearance of isoniazid, linezolid, and cycloserine, respectively. Although clofazimine increased the area under the curve of levofloxacin by 19%, this is unlikely to be of great clinical significance, and the lack of interaction with other drugs tested is reassuring.

Population pharmacokinetics and dose optimization of levofloxacin in elderly patients with pneumonia.

Levofloxacin is a quinolone antibiotic with a broad antibacterial spectrum. It is frequently used in elderly patients with pneumonia. The pharmacokinetic profile of elderly patients changes with age, but data on the pharmacokinetics of levofloxacin in these patients are limited. The aim of this study was to establish a population pharmacokinetic model of levofloxacin in elderly patients with pneumonia and to optimize individualized dosing regimens based on this newly developed model. This is a prospective, open-label pharmacokinetic study in elderly patients with pneumonia. Blood samples were collected using an opportunistic approach. The plasma concentrations of levofloxacin were determined by high-performance liquid chromatography. A population pharmacokinetic model was established using nonlinear mixed-effect model software. Monte Carlo simulations were used for dose simulation and dose optimization. Data from 51 elderly patients with pneumonia were used for the population pharmacokinetic analysis. A one-compartment model with first-order elimination was most suitable for describing the data, and the estimated glomerular filtration rate was the only covariate that had a significant impact on the model. The final model estimated that the mean clearance of levofloxacin in elderly patients with pneumonia was 5.26 L/h. Monte Carlo simulation results showed that the optimal dosing regimen for levofloxacin was 750 mg once a day in elderly patients with pneumonia, with a minimum inhibitory concentration of 2 mg/L. The population pharmacokinetic model of levofloxacin in elderly patients with pneumonia was established, and the dose optimization of levofloxacin was completed through Monte Carlo simulation.

Pharmacokinetics of levofloxacin through oral route of administration in dual purpose chicken by the LCMS/MS analytical technique

Pharmacokinetics of levofloxacin through oral route of administration in dual purpose chicken by the LCMS/MS analytical technique

Towards therapeutic drug monitoring of antibiotic levels - analyzing the pharmacokinetics of levofloxacin using DUV-resonance Raman spectroscopy.

Therapeutic drug monitoring (TDM) plays an important role in clinical practice. Here, pharmacokinetics has a decisive influence on the effective antibiotic concentration during treatment. Moreover, different kinetics exist for different administration forms. Accordingly, adjusting the correct concentration depends, in addition to gender, age, weight, clinical picture, etc., on the dosage form of the antibiotic. This study investigates the capability of deep UV resonance Raman spectroscopy (DUV-RRS) to simulate the pharmacokinetics of fluoroquinolone levofloxacin after two different administration forms (intravenous and oral). Three different pre-processing methods were applied, and the best agreement with the simulation was achieved using the extended multiplicative scatter correction. The resulting spectra were used for partial least squares (PLS) regression and ordinary least squares (OLS) regression. The kinetic parameters were compared with the simulated data, with PLS showing the best performance for intravenous administration and a comparable result to OLS for oral administration, while the errors are smaller. The acquired results show the potential of DUV-RRS in combination with PLS regression as a promising supportive method for TDM.

Population Pharmacokinetics of Levofloxacin and Moxifloxacin, and the Probability of Target Attainment in Ethiopian Patients with Multidrug-Resistant Tuberculosis.

This study aimed to explore the population pharmacokinetic modeling (PopPK) of levofloxacin (LFX) and moxifloxacin (MXF), as well as the percent probability of target attainment (PTA) as defined by the ratio of the area under the plasma concentration-time curve over 24 h and the in vitro minimum inhibitory concentration (AUC0-24/MIC) in Ethiopian multidrug resistant tuberculosis (MDR-TB) patients. Steady state-plasma concentration of the drugs in MDR-TB patients were determined using optimized liquid chromatography-tandem mass spectrometry. PopPK and simulations were run at various doses, and pharmacokinetic parameters were estimated. The effect of covariates on the PK parameters and PTA for maximum mycobacterial kill and resistance prevention was also investigated. LFX and MXF both fit in a one-compartment model with adjustments. Serum-creatinine (Cr) influenced (p = 0.01) the clearance of LFX, whereas body mass index (BMI) influenced (p = 0.01) the apparent volume of distribution (V) of MXF. The PTA for LFX maximal mycobacterial kill at the critical MIC of 0.5 mg/L with the simulated 750 mg, 1000 mg, and 1500 mg doses were 29%, 62%, and 95%, respectively, whereas the PTA for resistance prevention at 1500 mg was only 4.8%, with none of the lower doses achieving this target. At the critical MIC of 0.25 mg/L, there was no change in the PTA for maximum bacterial kill when the MXF dose was increased (600 mg, 800 mg, and 1000 mg), but the PTA for resistance prevention was improved. The standard doses of LFX and MXF may not provide adequate drug exposure. PopPK of LFX is more predictable for maximum mycobacterial kill, whereas MXF's resistance prevention target increases with dose. Cr and BMI are likely important covariates for dose optimization in Ethiopian patients.

Oral levofloxacin: population pharmacokinetics model and pharmacodynamics study in bone and joint infections.

This study aimed at characterizing the pharmacokinetics (PK) of oral levofloxacin in adult patients in order to optimize dosing scheme and explore the PK/pharmacodynamics (PD) of levofloxacin in bone and joint infections (BJIs). From November 2015 to December 2019, all patients hospitalized in Cochin Hospital, treated with levofloxacin and who had at least one dosage for therapeutic drug monitoring were included. PK was described using non-linear mixed-effect modelling. In a subgroup of patients with BJIs, the association between PK, MIC for the isolated pathogen and clinical outcome was investigated. Monte Carlo simulations investigated dosing regimens to achieve the PK/PD target (AUC/MIC ratio >100). One hundred and two patients were included (199 measurements), including 32 treated for BJI. A one-compartment model with first-order absorption and elimination best described the data. Effects of estimated creatinine clearance (eCLCR) and age were significant on levofloxacin clearance. In BJI patients, no significant association was found between levofloxacin PK/microbiological parameters and either clinical outcome or adverse events. Based on our model, we proposed optimized oral levofloxacin dosing regimens according to renal function, to reach the PK/PD target AUC/MIC ratio >100 for three frequent causative pathogens (Staphylococcus aureus, Enterobacterales and Pseudomonas aeruginosa). Our results reinforce the need of determining the MIC and using therapeutic drug monitoring in complex infections caused by P. aeruginosa.

Population Pharmacokinetics Modeling of Levofloxacin In Rabbit By Intravenous Bolus Injection and Peroral Administration

The population-based approach has been widely applied to describe the pharmacokinetic profile of many drugs. The aim of this current research was to study the implementation of the population-based pharmacokinetics of levofloxacin in rabbits administered by intravenous bolus injection and peroral delivery.&#x0D; Modeling analyses were performed using Monolix, one of the alternative tools for the population-based approach. Monolix works based on the Stochastic Approximation Expectation-Maximization (SAEM) method. The analysis was performed based on the population model using one-compartmental and two-compartmental disposition models. The combination error model was used during the analyses. Modeling appropriateness was determined based on the goodness of fit analyses, i.e., 1) the individual fit, 2) the observed versus population prediction values; and 3) the observed versus individual prediction values&#x0D; Plasma concentration profiles of levofloxacin by intravenous bolus injection and oral administration are better described by an appropriate model using a two-compartmental disposition model. All goodness of fit analyses demonstrates the power of the chosen model. However, the estimated disposition parameter values obtained based on the intravenous bolus injection and peroral administration are different for each subject. To confirm this phenomenon, we performed a simultaneous fitting of all intravenous bolus as well as peroral administration data. The goodness of fit analyses indicates an adequate fitting of all data.

Comparative pharmacokinetics of levofloxacin in the saliva and blood plasma of patients with pneumonia

BACKGROUND: Levofloxacin concentrations do not always reach desired levels when administered at a standard dose; therefore, measuring levofloxacin levels in the blood plasma or other alternative matrices, such as the saliva, can help clinicians make informed decisions concerning the dosage and mode of administration. Saliva, as an object of research, is of particular interest due to the simplicity and non-invasiveness of sampling for analysis.&#x0D; AIM: This study aimed to determine the comparative pharmacokinetics of levofloxacin in the blood plasma and saliva of patients with community-acquired pneumonia (CAP) and assess the possibility of using saliva as an alternative sampling matrix in pharmacokinetic studies.&#x0D; MATERIALS AND METHODS: Levofloxacin concentration in the blood plasma and saliva of patients with CAP and volunteers was determined using high-performance liquid chromatography on an Agilent 1200 liquid chromatography (Agilent, USA) with an ultraviolet detector. Sample preparation of bioassays was performed using protein precipitation. Patients and volunteers took 1 tablet (500 mg dose) of levofloxacin per os in the morning, on an empty stomach. Blood and saliva samples were taken at the initial blood sample and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, and 24 h after taking the drug. The pharmacokinetic parameters were determined, namely Cmax as the peak concentration of the drug; Тmax as the time-to-peak concentration; AUC0t as the area under the pharmacokinetic curve in the range from 0 to the last experimental point on the curve; AUC0 as the total area under the pharmacokinetic curve from zero to infinity; t1/2 as half-life period; MRT as mean residence time of the drug in the blood (h); Cl/F as clearance; and Vss/F as the total distribution volume.&#x0D; RESULTS: The maximum blood plasma and saliva concentration of patients was reached 1 h after taking the drug and amounted to Сmax=5.982.89 g/ml and Сmax=4.413.83 g/ml, respectively. Additionally, the maximum concentrations in blood plasma and saliva were recorded 1 h after taking the drug as 5.523.07 g/ml and 3.250.85 g/ml, respectively, in healthy volunteers. The correlation coefficient (r) between the mean values of the levofloxacin concentrations in the blood plasma and the saliva of patients with CAP was 0.953 and that of healthy volunteers was 0.977.&#x0D; DISCUSSION: Pharmacokinetic parameters were calculated based on blood plasma and saliva concentrations. Their comparative analysis revealed almost the same absorption rate from the gastrointestinal tract in patients and healthy volunteers. Correlation-regression analysis revealed a high correlation between the average values of Cmax in saliva and plasma both in the patient (r=0.96) and healthy volunteer group (r=0.98).&#x0D; CONCLUSIONS: With statistically significant differences in the areas under pharmacokinetic curves in blood plasma and saliva, the remaining pharmacokinetic parameters of saliva and blood plasma did not significantly differ between patients with CAP and healthy volunteers. A significant direct correlation was revealed between the mean concentration and pharmacokinetic parameters in saliva and blood plasma in both groups. The study demonstrated the possibility of using saliva as a biomaterial in the study of levofloxacin pharmacokinetics.

Population pharmacokinetics of oral levofloxacin in healthy volunteers and dosing optimization for multidrug-resistant tuberculosis therapy.

Levofloxacin is considered a key component of a multidrug-resistant tuberculosis (MDR-TB) regimen. However, there is considerable concern regarding the subtherapeutic concentrations of the currently used doses and the development of drug resistance. Therefore, this study aimed to describe the population pharmacokinetics (PPK) of oral levofloxacin in healthy volunteers and to evaluate the probability of target attainment (PTA) in an attempt to optimize the dosing regimens for MDR-TB therapy. Data of levofloxacin in healthy volunteers from a previous study were used to construct a PPK model. Monte Carlo simulations were performed to derive the PTAs of various regimens. A two-compartment model with linear elimination and transit absorption compartments best described the pharmacokinetics (PK) of levofloxacin. The estimated PK parameters (interindividual variability, %) were: apparent clearance 8.32Lh-1 (22.6%), apparent central volume of distribution 35.8L (45.2%), apparent peripheral volume of distribution 39.7L, intercompartmental clearance 40.6Lh-1 (43.8%), absorption rate constant 7.45h-1 (150%), mean absorption transit time 0.355h (52.4%), and total number of transit compartments 6.01 (131.9%). Monte Carlo simulations using levofloxacin 750-1000mg yielded a probability of achieving a target free area under the concentration-time curve/minimum inhibitory concentration (MIC) of 100 at greater than 90% for Mycobacterium tuberculosis with an MIC < 0.5mg L-1 , while a dose of 1500mg was required for strains with an MIC of 1mg L-1 . A higher dose of levofloxacin might be needed to treat tuberculosis. However, further studies on the efficacy and safety of this dose are needed to confirm our findings.

Pharmacokinetics of levofloxacin mesylate in healthy adult giant panda after single-dose administration via different routes.

The pharmacokinetics of levofloxacin mesylate in healthy adult giant panda is unknown. In this study, the pharmacokinetics of levofloxacin after intramuscular administration at a dose of 2mg/kg and oral administration at a dose of 3mg/kg in healthy adult giant pandas was determined. Levofloxacin concentrations in plasma were determined using liquid chromatography. In the levofloxacin intramuscular administration group, the absorption and elimination half-lives of the drug were determined to be 0.123 (range: 0.02) hr and 5.402 (range: 0.70) hr, respectively. In the levofloxacin oral administration group, the absorption and elimination half-lives were determined to be 0.325 (range: 0.02) hr and 7.143 (range: 0.63) hr, respectively. Furthermore, the blood-drug concentration of levofloxacin was found to be above 1μg/ml after 8hr of intramuscular administration and above 0.5μg/ml after 12hr of oral administration. In this study, HPLC conditions and pretreatment methods of plasma samples were optimized and a detection method was established. Our results indicated that in healthy adult giant pandas, levofloxacin was rapidly absorbed and slowly eliminated. This study will therefore provide to be a guide in veterinary research and will be helpful in the rational use of levofloxacin in giant panda.

Herb-drug interaction: The effect of Polygonum capitatum extract on pharmacokinetics of levofloxacin in rats

Polygonum capitatum is a traditional medicinal plant of the Miao people and has been used to treat a variety of urological disorders in China for many years. Preparations made from water-soluble P. capitatum extracts, Relinqing® granules, are often used in combination with levofloxacin to treat urinary tract infections, and have demonstrated better clinical efficacy than either drug alone. As there is no information on the pharmacokinetics of both drugs after co-administration, a sensitive and reliable ultra-performance liquid chromatography-tandem mass spectrometry method was developed and validated to study the potential herb-drug interactions between P. capitatum and levofloxacin. This analytical method delivered high levels of specificity, recovery, accuracy, precision and preserved sample stability. When applied to study pharmacokinetic interactions after oral co-administration of P. capitatum extract (1.86 g kg−1) and levofloxacin (42 mg kg−1) in rats, the results indicated significant reductions in Cmax and AUC0−24h of levofloxacin, and significant increases in MRT, Tmax, CLz/F and Vz/F. Moreover, pretreatment with P. capitatum extract orally did not alter the intravenous pharmacokinetics of levofloxacin. Combined and compared oral pharmacokinetic parameters, suggesting that the interacting targets might localized in the intestine during absorption. Overall, the results revealed a potential herb-drug interaction between P. capitatum and levofloxacin.

Levofloxacin pharmacokinetics and tissue residue concentrations after oral administration in Bilgorajska geese

ABSTRACT 1. The aim of this study was to assess the pharmacokinetics of levofloxacin, a third-generation fluoro-quinolone antimicrobial drug, in geese (n = 26) after either single intravenous or oral administration, and to evaluate the depletion profile in goose muscle, heart, liver, kidney and lung after a single oral dose. 2. The pharmacokinetic study involved 16 geese which were randomly divided into two groups (n = 8/group), the first received levofloxacin (2 mg/kg) intravenously while the second was treated with orally (5 mg/kg). The tissue depletion study involved 10 geese which were dosed orally (5 mg/kg) and two animals were killed at different time-points in order to collect the selected tissues. Levofloxacin was quantified in all the matrices tested by a validated high-performance liquid chromatography (HPLC) method, using a spectrofluorimetric detector. The pharmacokinetics were analysed using a non-compartmental model. 3. Plasma concentrations were quantified after up to 24 h in animals administered intravenously and up to 48 h after oral treatment. Levofloxacin was rapidly absorbed after oral administration (Tmax = 0.38 h) showing high bioavailability (95.57 ± 20.61%). The drug showed a moderate volume of distribution (1.40 ± 0.28 ml/g) and rapid clearance (0.28 ± 0.06 ml/g/h). No statistical differences in estimates were found between the two different administration methods (P > 0.05). Drug residues were highest at 6 h and decreased constantly up to 48 h in all the selected tissues. Liver and kidney had the highest levofloxacin concentrations. 4. According to the pharmacokinetic/pharmacodynamic surrogate index (AUC/MIC) the levofloxacin dose regimen (after oral administration) used in the present study could be active against bacteria at a minimum inhibitory concentration (MIC) > 0.24 μg/ml in geese. In addition, drug accumulation in the liver might be controlled using an estimated preliminary withdrawal time of 90 h.

Study of the pharmacokinetics of levofloxacin when combined with st. John’s wort preparations in healthy volunteers and in patients with lower respiratory tract infection

In patients with pneumonia and concomitant diseases, the administration of antimicrobial agents together with other medications accompanied by the risk of side effects and drug-drug interactions. We studied the pharmacokinetics (PK) of levofloxacin when combined with a herbal preparation (common St. Johns wort extract) in healthy volunteers and in patients with community-acquired pneumonia on the days 1 and 5 of the drugs intake. Individual differences in the average concentrations (AUC analog) of the antibiotic before and after the course of administration of the St. Johns wort extract within each group were quite significant; however, the group-average differences were statistically insignificant. Intergroup differences in PK with St. Johns wort intake were also statistically insignificant. To search for factors that make a significant contribution to the variations observed in PK indices, we used a statistical multivariate analysis of variance which included factors such as gender, age, body mass index, smoking history, and cardiovascular system parameters. We found that smoking only and, to a lesser extent, the patients gender had an effect on levofloxacin PK, while the intake of St. Johns wort completely eliminated this effect. Other factors played an insignificant role in the antibiotic PK regardless of the St. Johns wort administration.

Pharmacokinetics of levofloxacin in non-lactating goats and evaluation of drug effects on resistance in coliform rectal flora

This study aimed to evaluate the pharmacokinetics/pharmacodynamics (PK/PD) of levofloxacin in non-lactating goats. Using a randomized cross-over study design, each group of animals (n = 7) received 2 mg/kg of levofloxacin intravenously (IV) and subcutaneously (SC). Plasma concentrations of levofloxacin were quantified by High Performance Liquid Chromatography with fluorescence detector (HPLC-FL). Rectal swabs were collected prior and after the treatment to identify the main bacterial population and to evaluate in vitro antimicrobial susceptibility using minimal inhibitory concentration (MIC) method. Mean values of terminal half-life for IV and SC groups were 4.56 and 5.14 h, respectively. After SC administration, the peak plasma concentration was achieved at 2 h, with a Cmax of 3681 ng/mL. Mean bioavailability was 92.12%. Bacteria isolation showed the presence of Escherichia coli (E. coli) that quickly becomes resistant to levofloxacin potentially rendering the drug ineffective. Results seem to suggest that levofloxacin is able to reach considerable plasma concentrations after both IV and SC administration, but it must be considered that both routes of administration can lead to a reversible selection of resistance in gastro-intestinal bacteria.

Pharmacokinetics of levofloxacin after single intravenous and oral administration, and its interaction with sucralfate in mixed-breed dogs

The study aims to establish the plasma pharmacokinetic parameters of levofloxacin in mixed-breed dogs, at a single dose of 5 mg/kg, intravenously, orally only and orally with sucralfate pre-treatment (1 g per animal), to evaluate its influence on antimicrobial absorption. Concentrations of levofloxacin in plasma were determined using high-performance liquid chromatography (HPLC) with fluorescence detection. After iv of levofloxacin, the mean (±SD) of AUC0–24, Vz, t½λz and MRT, was 19.05 ± 6.4 µg-h/ml, 2.43 ± 0.5 L/kg, 7.93 ± 1.41 hours and 8.7 ± 1.5 hours, respectively. After oral administration, the C max, t½λz and bioavailability were 1.95 ± 0.7 µg/ml, 7.65 ± 1.38 hours and 71.93 ± 9.75%, respectively. In animals given an oral dose of levofloxacin with sucralfate pre-treatment, there was a significant decrease (p < 0.05) in C max (0.57 ± 0.23 µg/ml), AUC (5.73 ± 2.26 µg-h/ml) and bioavailability (31.92 ± 14.19%). In the dogs studied, it is suggested that the dose 5 mg/kg of levofloxacin for both routes is inadequate to meet PK–PD targets for susceptible bacteria using breakpoints established by the Institute of Clinical and Laboratory Standards (CLSI).

Influence of Renal Function and Age on the Pharmacokinetics of Levofloxacin in Patients with Bone and Joint Infections

Despite its efficacy and toxicity being exposure-related, levofloxacin pharmacokinetics in patients with bone and joint infections has been poorly described to date, so the possible need for a dose adjustment is unknown in this population. A prospective population pharmacokinetic study was conducted in 59 patients to answer this question. The final model consisted of a one-compartment model with first-order absorption and elimination. Mean parameter estimates (% interindividual variability) were 0.895 h−1 for the absorption rate constant (Ka), 6.10 L/h (40%) for the apparent clearance (CL/F), 90.6 L (25%) for the apparent distribution volume (V/F). Age and glomerular filtration rate (GFR), estimated by the modification of diet in renal disease formula, were related to CL/F by power models, and CL/F was found to increase for increasing GFR and decreasing age. For a similar GFR, the simulated area under the curve (AUC) was 55% higher in 70 years-old patients compared to 30 year-old patients. Based on this model, a 750 mg dose should provide an optimal exposure (AUC/ minimum inhibitory concentration (MIC) ≥100), with the possible exception of patients older than 60 years and with GFR <70 mL/min/m² who may necessitate a dose reduction, and patients with infections caused by bacteria with MIC close to 1 mg/L who may need an increase in the dose.

Influences of tolfenamic acid and flunixin meglumine on the disposition kinetics of levofloxacin in sheep.

The pharmacokinetics of levofloxacin (4 mg/kg), administered both alone and in combination with tolfenamic acid (2 mg/kg) and flunixin meglumine (2.2 mg/kg), was established after intravenous administration in sheep. Plasma levofloxacin concentrations were assayed by high-performance liquid chromatography and analysed according to the two-compartment open model. Following the administration of levofloxacin alone, the mean distribution half-life, elimination half-life, total clearance, volume of distribution at steady state and area under the plasma concentration-time curve were 0.20 h, 1.82 h, 0.39 L/h/kg, 0.96 L/kg and 10.40 h × µg/mL, respectively. Tolfenamic acid and flunixin meglumine caused a slow elimination and increased plasma concentrations of levofloxacin in combination administration. Levofloxacin, with an alteration in the dosage regimen, can be used effectively with tolfenamic acid and flunixin meglumine for the therapy of infections and inflammatory conditions in sheep.

Effect of Terazosin on the Pharmacokinetics of Levofloxacin in the Rat Model of Prostatitis

The primary objective of the present work was to investigate the effect of terazosin on the pharmacokinetics of levofloxacin in prostate, when combined therapy of terazosin hydrochloride and levofloxacin were applied to treat bacterial prostatitis in the rat. A total of 100 rats with bacterial prostatitis were randomized into the control group and the research group, with 50 rats in each group. Levofloxacin solution was injected intravenously to the rats of both groups. Terazosin hydrochloride solution was given by gavage to the rats of the research group, while solvent was administrated by gavage to the rats of control group. After drug administration, the rat prostate was harvested and homogenized and the levofloxacin concentration was analysed. The drug-time curves in both groups were accorded with two compartments model. Compared with the control group, the t½β, Cmax and AUC0–12 was significantly higher in the research group. And there was significant difference in the levofloxacin concentration of prostate between both groups (p<0.05). The levofloxacin concentration and distribution were significantly elevated by terazosin hydrochloride, which could improve the prognosis of prostatitis and obtain better therapeutic efficacy.

The Pharmacokinetics of Topical Levofloxacin 1.5% vs Topical Moxifloxacin 0.5%

The Pharmacokinetics of Topical Levofloxacin 1.5% vs Topical Moxifloxacin 0.5%

Effect of food thickener and jelly wafer on the pharmacokinetics of levofloxacin orally disintegrating tablets

This study was designed to determine the effects of a food thickener and deglutition aid jelly for oral administration, jelly wafer, on the pharmacokinetics of levofloxacin orally disintegrating tablets. With an increase in immersion time, the disintegration time of levofloxacin orally disintegrating tablets immersed in food thickener was prolonged, whereas that of the tablets immersed in jelly wafer was shortened. The dissolution behavior of non-immersed levofloxacin orally disintegrating tablets was not similar to that of tablets immersed in food thickener, but was similar to that of tablets immersed in jelly wafer. The time to reach the maximum systemic levofloxacin concentration was the same for non-immersed orally disintegrating tablets and tablets immersed in food thickener and jelly wafer. Moreover, there was no significant difference in the maximum concentration after administration between non-immersed orally disintegrating tablets and tablets immersed in food thickener or jelly wafer. These findings suggest that drugs with a high bioavailability, such as levofloxacin, enter the systemic circulation even when administered with a food thickener or jelly wafer.