吉米沙星是韩国LG Life Science公司研制的第四代氟喹诺酮类抗菌新药,它同时作用于细菌DNA旋转酶和DNA拓扑异构酶IV,提高了抗菌活性,降低耐药率。吉米沙星除了保持对革兰阴性菌的强大抗菌活性外,对包括多重耐药性肺炎链球菌在内的革兰...吉米沙星是韩国LG Life Science公司研制的第四代氟喹诺酮类抗菌新药,它同时作用于细菌DNA旋转酶和DNA拓扑异构酶IV,提高了抗菌活性,降低耐药率。吉米沙星除了保持对革兰阴性菌的强大抗菌活性外,对包括多重耐药性肺炎链球菌在内的革兰阳性菌也具有良好的活性。吉米沙星具有良好的药动学性质,组织渗透性强,能强力杀灭感染部位致病菌。它的药物间相互作用少,有较好的安全性和耐受性,是临床上治疗慢性支气管炎急性发作、社区获得性肺炎和急性鼻窦炎的良好药物。展开更多
Background Gemifloxacin is a fluoroquinolone antibiotic with broad spectrum of antibacterial activity.The aim of the study was to evaluate the comparative effectiveness and safety of gemifloxacin for the treatment of ...Background Gemifloxacin is a fluoroquinolone antibiotic with broad spectrum of antibacterial activity.The aim of the study was to evaluate the comparative effectiveness and safety of gemifloxacin for the treatment of patients with community-acquired pneumonia （CAP） or acute exacerbation of chronic bronchitis （AECB）.Methods We performed a meta-analysis of randomized controlled trials （RCTs） comparing gemifloxacin with other approved antibiotics.The PubMed,EMBASE,Chinese Biomedical Literature Database and the Cochrane Central Register of Controlled Trials were searched,with no language restrictions.Results Ten RCTs,comparing gemifloxacin with other quinolones （in 5 RCTs） and β-lactams and/or macrolides （in 5 RCTs）,involving 3940 patients,were included in this meta-analysis.Overall,the treatment success was higher for gemifloxacin when compared with other antibiotics （odds ratio 1.39,95% confidence interval 1.15-1.68 in intention-to-treat patients,and 1.33,1.02-1.73 in clinically evaluable patients）.There was no significant difference between the compared antibiotics regarding microbiological success （1.19,0.84-1.68） or all-cause mortality （0.82,0.41-1.63）.The total drug related adverse events were similar for gemifloxacin when compared with other quinolones （0.89,0.56-1.41）,while lower when compared with β-lactams and/or macrolides （0.71,0.57-0.89）.In subgroup analyses,administration of gemifloxacin was associated with fewer cases of diarrhoea and more rashes compared with other antibiotics （0.66,0.48-0.91,and 2.36,1.18-4.74,respectively）.Conclusions The available evidence suggests that gemifloxacin 320 mg oral daily is equivalent or superior to other approved antibiotics in effectiveness and safety for CAP and AECB.The development of rash represents potential limitation of gemifloxacin.展开更多
The electrochemical oxidation behavior and voltammetric assay of gemifloxacin were investigated using differential-pulse and cyclic voltammetry on a screen-printed carbon electrode.The effects of pH,scan rates,and con...The electrochemical oxidation behavior and voltammetric assay of gemifloxacin were investigated using differential-pulse and cyclic voltammetry on a screen-printed carbon electrode.The effects of pH,scan rates,and concentration of the drug on the anodic peak current were studied.Voltammograms of gemifloxacin in Tris-HCl buffer（pH 7.0） exhibited a well-defined single oxidation peak.A differential-pulse voltammetric procedure for the quantitation of gemifloxacin has been developed and suitably validated with respect to linearity,limits of detection and quantification,accuracy,precision,specificity,and robustness.The calibration was linear from 0.5 to 10.0 μM,and the limits of detection and quantification were 0.15 and 5.0 μM.Recoveries ranging from 96.26% to 103.64% were obtained.The method was successfully applied to the determination of gemifloxacin in pharmaceutical tablets without any pre-treatment.Excipients present in the tablets did not interfere in the assay.展开更多
Simple and sensitive stability-indicating high performance thin layer chromatography (HPTLC) assay was developed and validated for quantitative determination of the antibacterial drug, gemifloxacin mesylate (GFX) in p...Simple and sensitive stability-indicating high performance thin layer chromatography (HPTLC) assay was developed and validated for quantitative determination of the antibacterial drug, gemifloxacin mesylate (GFX) in presence of its degradation products and ambroxol hydrochloride. The chromatographic separation was performed on HPTLC precoated silica gel plate 60F254 as stationary phase. The mobile phase consisted of a mixture of ethyl acetate: methanol: 25% ammonia, (8:4.5:3, v/v/v). The detection was performed using fluorescence mode and the emission intensity was measured using optical filter K400 after excitation at 342 nm. The Rf value for GFX was 0.47 ± 0.03. Good correlation coefficient was obtained over the concentration range of 1.5 - 180 ng/band. The LOD and LOQ of the proposed method were 0.28 and 0.86 ng/band, respectively. The proposed method was successfully applied for the analysis of GFX in its single and combined dosage forms. Moreover, it was utilized to investigate the kinetics of acidic, alkaline, neutral, oxidative and photolytic degradation of the drug. The apparent kinetic-order rate constants and half-life times of the degradation process were calculated. Furthermore, the proposed method was successfully applied for investigating the factors affecting the storage of GFX.展开更多
Transdermal delivery acts as an alternative to oral delivery of drugs and possibly provids also an alternative to hypodermic injection. Transdermal delivery when compared to oral route has a variety of advantages name...Transdermal delivery acts as an alternative to oral delivery of drugs and possibly provids also an alternative to hypodermic injection. Transdermal delivery when compared to oral route has a variety of advantages namely: avoiding the degradation of drugs in the stomach environment, providing steady plasma levels, avoiding first-pass metabolism, increaseing patient compliance, easy to use, non-invasive and inexpensive, increasing the therapeutic index with a simultaneous decrease in drug side effects. Despite these advantages, one of the greatest challenges to transdermal delivery is that only a limited number of drugs are amenable to administration by this route. Gemifloxacin, a broad spectrum fourth generation quinolone antibacterial agent has pharmacokinetic characteristics (particularly its low maximum plasma concentration, obtained following repeat oral dose of 320 mg) that makes it a potential target for transdermal delivery. The objective of the study was to explore the possibility of surfactants (anionic, cationic and nonionic) acting as dermal enhancers of gemifloxacin assuming that the drug is to be formulated into topical or transdermal pharmaceutical dosage form. To accomplish the objective, gemifloxacin was partitioned between chloroform and surfactants containing varying concentrations of sodium lauryl sulfate, cetyltrimethylammonium bromide, polysorbate-20 and polysorbate-80. The data obtained were used to estimate the dermal permeability coefficient. The partitioning was carried out by shake flask method at room temperature. It was observed that all the surfactants decreased the partition behavior of gemifloxacin when compared to that of water alone. Sodium lauryl sulfate produced the most decreasing partition effect at the highest concentration studied (2% w/v). The permeability coefficient (Kp) was estimated from the partition coefficient data and the molecular weight of the drug. As permeability coefficient is an important descriptor for evaluating dermal absorption of drugs employed in clinical展开更多
文摘吉米沙星是韩国LG Life Science公司研制的第四代氟喹诺酮类抗菌新药,它同时作用于细菌DNA旋转酶和DNA拓扑异构酶IV,提高了抗菌活性,降低耐药率。吉米沙星除了保持对革兰阴性菌的强大抗菌活性外,对包括多重耐药性肺炎链球菌在内的革兰阳性菌也具有良好的活性。吉米沙星具有良好的药动学性质,组织渗透性强,能强力杀灭感染部位致病菌。它的药物间相互作用少,有较好的安全性和耐受性,是临床上治疗慢性支气管炎急性发作、社区获得性肺炎和急性鼻窦炎的良好药物。
文摘Background Gemifloxacin is a fluoroquinolone antibiotic with broad spectrum of antibacterial activity.The aim of the study was to evaluate the comparative effectiveness and safety of gemifloxacin for the treatment of patients with community-acquired pneumonia （CAP） or acute exacerbation of chronic bronchitis （AECB）.Methods We performed a meta-analysis of randomized controlled trials （RCTs） comparing gemifloxacin with other approved antibiotics.The PubMed,EMBASE,Chinese Biomedical Literature Database and the Cochrane Central Register of Controlled Trials were searched,with no language restrictions.Results Ten RCTs,comparing gemifloxacin with other quinolones （in 5 RCTs） and β-lactams and/or macrolides （in 5 RCTs）,involving 3940 patients,were included in this meta-analysis.Overall,the treatment success was higher for gemifloxacin when compared with other antibiotics （odds ratio 1.39,95% confidence interval 1.15-1.68 in intention-to-treat patients,and 1.33,1.02-1.73 in clinically evaluable patients）.There was no significant difference between the compared antibiotics regarding microbiological success （1.19,0.84-1.68） or all-cause mortality （0.82,0.41-1.63）.The total drug related adverse events were similar for gemifloxacin when compared with other quinolones （0.89,0.56-1.41）,while lower when compared with β-lactams and/or macrolides （0.71,0.57-0.89）.In subgroup analyses,administration of gemifloxacin was associated with fewer cases of diarrhoea and more rashes compared with other antibiotics （0.66,0.48-0.91,and 2.36,1.18-4.74,respectively）.Conclusions The available evidence suggests that gemifloxacin 320 mg oral daily is equivalent or superior to other approved antibiotics in effectiveness and safety for CAP and AECB.The development of rash represents potential limitation of gemifloxacin.
文摘The electrochemical oxidation behavior and voltammetric assay of gemifloxacin were investigated using differential-pulse and cyclic voltammetry on a screen-printed carbon electrode.The effects of pH,scan rates,and concentration of the drug on the anodic peak current were studied.Voltammograms of gemifloxacin in Tris-HCl buffer（pH 7.0） exhibited a well-defined single oxidation peak.A differential-pulse voltammetric procedure for the quantitation of gemifloxacin has been developed and suitably validated with respect to linearity,limits of detection and quantification,accuracy,precision,specificity,and robustness.The calibration was linear from 0.5 to 10.0 μM,and the limits of detection and quantification were 0.15 and 5.0 μM.Recoveries ranging from 96.26% to 103.64% were obtained.The method was successfully applied to the determination of gemifloxacin in pharmaceutical tablets without any pre-treatment.Excipients present in the tablets did not interfere in the assay.
文摘Simple and sensitive stability-indicating high performance thin layer chromatography (HPTLC) assay was developed and validated for quantitative determination of the antibacterial drug, gemifloxacin mesylate (GFX) in presence of its degradation products and ambroxol hydrochloride. The chromatographic separation was performed on HPTLC precoated silica gel plate 60F254 as stationary phase. The mobile phase consisted of a mixture of ethyl acetate: methanol: 25% ammonia, (8:4.5:3, v/v/v). The detection was performed using fluorescence mode and the emission intensity was measured using optical filter K400 after excitation at 342 nm. The Rf value for GFX was 0.47 ± 0.03. Good correlation coefficient was obtained over the concentration range of 1.5 - 180 ng/band. The LOD and LOQ of the proposed method were 0.28 and 0.86 ng/band, respectively. The proposed method was successfully applied for the analysis of GFX in its single and combined dosage forms. Moreover, it was utilized to investigate the kinetics of acidic, alkaline, neutral, oxidative and photolytic degradation of the drug. The apparent kinetic-order rate constants and half-life times of the degradation process were calculated. Furthermore, the proposed method was successfully applied for investigating the factors affecting the storage of GFX.
文摘Transdermal delivery acts as an alternative to oral delivery of drugs and possibly provids also an alternative to hypodermic injection. Transdermal delivery when compared to oral route has a variety of advantages namely: avoiding the degradation of drugs in the stomach environment, providing steady plasma levels, avoiding first-pass metabolism, increaseing patient compliance, easy to use, non-invasive and inexpensive, increasing the therapeutic index with a simultaneous decrease in drug side effects. Despite these advantages, one of the greatest challenges to transdermal delivery is that only a limited number of drugs are amenable to administration by this route. Gemifloxacin, a broad spectrum fourth generation quinolone antibacterial agent has pharmacokinetic characteristics (particularly its low maximum plasma concentration, obtained following repeat oral dose of 320 mg) that makes it a potential target for transdermal delivery. The objective of the study was to explore the possibility of surfactants (anionic, cationic and nonionic) acting as dermal enhancers of gemifloxacin assuming that the drug is to be formulated into topical or transdermal pharmaceutical dosage form. To accomplish the objective, gemifloxacin was partitioned between chloroform and surfactants containing varying concentrations of sodium lauryl sulfate, cetyltrimethylammonium bromide, polysorbate-20 and polysorbate-80. The data obtained were used to estimate the dermal permeability coefficient. The partitioning was carried out by shake flask method at room temperature. It was observed that all the surfactants decreased the partition behavior of gemifloxacin when compared to that of water alone. Sodium lauryl sulfate produced the most decreasing partition effect at the highest concentration studied (2% w/v). The permeability coefficient (Kp) was estimated from the partition coefficient data and the molecular weight of the drug. As permeability coefficient is an important descriptor for evaluating dermal absorption of drugs employed in clinical
