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Objective:To prepare N-trimethyl chitosan (TMC)-coated sparfloxacin (SL) nanoliposomes in situ gels(ISG)and in-vestigate the drug release in vitro.Methods:SL liposomes were prepared by a pH gradient method , and then homogenized to nanolipo-somes by high pressure .TMC was used as the coating material to prepare TMC-coated SL nanoliposomes .Poloxamer 407 was used as the gel base, and the optimal amount was selected according to the gelation temperature .TMC-coated SL nanoliposomes ISG was pre-pared using a cold method , and the morphology , size, zeta potential and entrapment efficiency of TMC-coated SL nanoliposomes were studied.A membraneless model was used to study the drug release in vitro, and the result was compared with that of TMC-coated SL nanoliposomes.Results:The optimal amount of poloxamer 407 in the formula was 25%, and the gelation temperature was 23.6℃in the artificial tears and 33 .5℃in the diluted artificial tears .The morphology of TMC-coated SL nanaoliposomes in the ISG was spherical with the mean diameter of (96.8 ±1.5) nm, zeta potential of (46.2 ±1.4) mV and entrapment efficiency of (76.6 ±2.4) %, and the indices had no significant difference when compared with those of TMC-coated SL nanoliposomes .Both the drug release in vitro and gel dissolution profile of TMC-coated SL nanoliposomes ISG exhibited the characteristics of zero-order kinetics, and compared with that of TMC-coated SL nanoliposomes , the sustained release property of the ISG was more significant .Conclusion:TMC-coated SL nanoli-posomes ISG has promising gelation temperature and notable sustained release property .
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Objective:To study the in vitro corneal permeation and antibacterial activity of N-trimethyl chitosan(TMC)-coated sparfloxacin lactate(SL)nanoliposomes. Methods:Franz diffusion cells were used with rabbit cornea as the barrier to study the in vitro corneal permeation of TMC-coated SL nanoliposomes,and the permeation parameters were calculated. Eseheriehia eoli,staphylo-eoeeus aureus,pseudomonas aeruginosa and baeillus subtilis were used as the tested bacterial strains and the in vitro antibacterial activity of the SL preparations was investigated to obtain the minimum inhibitory concentration(MIC),the minimum bactericidal concentration (MBC)and the relationship of bacterial inhibitory rate and time. Results:The order of steady permeation rate(J),corneal perme-ation coefficient(P)and corneal retention rate was TMC-coated SL nanoliposomes > SL nanoliposomes > SL eye drop. The order of lag time(τ)and corneal diffusion coefficient(D)was SL nanoliposomes > SL eye drop > TMC-coated SL nanoliposomes. The in vitro an-tibacterial activity showed the order of TMC-coated SL nanoliposomes > SL nanoliposomes > SL eye drop. Conclusion:Compared with the eye drop,liposomes can enhance the corneal permeation and storage of SL with improved antibacterial activity,and TMC-coating can further improve the permeation and antibacterial activity,which is worthy of further study.
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Objective To investigate clinical effect of sparfloxacin on the treatment of ureaplasma urealyticum prostatitis.Methods 96 cases with ureaplasma urealyticum prostatitis, which admitted in our hospital, were selected as the research object and divided into observation group ( n =48 cases) and control group ( n=48 cases) randomly.The control group was given the ofloxacin for treatment and the observation group was given the sparfloxacin for treatment.The clinical effect of the two groups after treatment was analyzed.Results The total effective rate of the observation group (97.92%) was significantly higher than that of the control group (72.92%) (P0.05).Conclusion Patients with ureaplasma urealyticum prostatitis, the treatment effect of sparfloxacin is significant, with lower adverse reactions rate and the security is higher, which is recognized in the medical community, can be worthy of popularization and application in clinic.
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A modified simple, selective, rapid, precise reversed phase high performance liquid chromatography method has been developed and validated for the simultaneous estimation of ketorolac and sparfloxacin. The separation was made in a Hypersil-Keystone C-18 column using a methanol: water (60:40, v/v) (pH 3.1) as mobile phase at 308 nm. The mobile-phase flow rate and the sample volume injected were 0.9 ml/min and 20 μl, respectively. Retention time of sparfloxacin and ketorolac was found to be 3.181 and 4.473 minutes respectively. The correlation coefficient of both drugs was found to be 0.999. The accuracy of ketorolac was found to be 99.82% - 100.55% whereas for sparfloxacin, it was 99.76% - 99.89%. Over all % RSD was found to be less than 2%. The method was validated according to ICH guidelines with respect to linearity, accuracy, precision, robustness, specificity, etc. The developed method can be used for routine analysis of ketorolac and sparfloxacin in their pharmaceutical dosage forms.
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The present study describes the development and subsequent validation of simple and accurate stability indicating RP-HPLC method for the determination of sparfloxacin and dexamethasone in pharmaceutical formulations in the presence of their stress-induced degradation products. Both the drugs and their stress-induced degradation products were separated within 10 minutes using C8 column and mixture of methanol and 0.02 M phosphate buffer pH 3.0 (60:40 v/v, respectively) as mobile phase at 270 nm using diode array detector. Regression analysis showed linearity in the range of 15-105 µg/mL for sparfloxacin and 5-35 µg/mL for dexamethasone. All the analytes were adequately resolved with acceptable tailing. Peak purity of the two drugs was also greater than 0.9999, showing no co-elution peaks. The developed method was applied for simultaneous determination of sparfloxacin and dexamethasone in pharmaceutical formulations for stability studies.
O presente estudo descreve o desenvolvimento e a subsequente validação de indicador de estabilidade simples e acurada por RP-HPLC para a determinação de esparfloxacino e dexametasona em formulações farmacêuticas na presença de produtos de degradação induzidos por estresse. Tanto os fármacos quanto os produtos de degradação induzidos pelo estresse foram separados em 10 minutos, utilizando coluna C8 e mistura de methanol e tampão fosfato 0,02 M, pH 3,0 (60:40 v/v, respectivamente) como fase móvel e detector de arranjo de diodo a 270 nm, A análise de regressão mostrou linearidade na faixa de 15-105 µg/mL para esparfloxacino e 5-35 µg/mL para a dexametsona. Todos os analitos foram resolvidos adequadamente com tailing aceitável. O pico de pureza dos dois foi maior que 0.9999, não mostrando picos de co-eluição. O método desenvolvido foi aplicado para a determinação simultânea de esparfloxacino e dexametasona em formulações farmacêuticas e para estudos de estabilidade.
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Dexamethasone/analysis , Chemistry, Pharmaceutical/instrumentation , Chromatography, High Pressure Liquid/methods , Pharmaceutical Preparations/analysisABSTRACT
Plasma quinolone concentrations are not routinely measured in clinical practice.However,in order to optimize quinolone treatment,monitoring of plasma concentrations could sometimes be useful particularly in critically ill patients.In this study,anti-sparfloxacin antibody was obtained by immunizing rabbits with sparfloxacin conjugated with bovine serum albumin using isobutyl chloroformate method.After the assay procedure was optimized,the standard curve of sparfloxacin was established.The practical measuring range of the competitive ELISA extended from 5 ng/mL to 2 μtg/mL.The recovery rates and coefficients of variation for rat plasma,urine and tissues were 87.7-106.2％ and 4.8-15.3％,respectively.To demonstrate the potential of the ELISA,a preliminary pharmacokinetics and tissue distribution study of sparfloxacin in rats and quantitative analysis of sparfloxacin in several pharmaceuticals were performed and compared with high-performance liquid chromatography (HPLC).The experimental data indicated that the proposed method would be a valuable tool in therapeutic drug monitoring (TDM) for sparfloxacin.
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OBJECTIVE:To assess the clinical efficacy and safety of domestic sparfloxacin for acute bacterial infections.METHODS:Domestic literatures about sparfloxacin for acute bacterial infections were retrieved by computer and their quality was evaluated to extract data(1993～2009).RevMan 4.2.2 software was used for Meta-analysis.RESULTS:A total of 10 RCT were enrolled.The comparisons of 2 groups were homogeneous in terms of clinical cure rate,clinical response rate,bacterial clearance rate and safety.There was statistical significance in comparison of combined effect variable between 2 groups in respect of cure rate,response rate and bacterial clearance rate(P0.05).CONCLUSION:The currently available evidence shows that clinical efficacy of domestic sparfloxacin for acute bacterial infections is better and incidence of ADR was lower.
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OBJECTIVE:To study the difference between the hydrophilic and hydrophobic fluoroquinolones(FQNLs)in?ducing resistant Klebsiella pneumoniae(Kpn)in vitro.METHODS:Hydrophilic ciprofloxacin(CIP)and hydrophobic sparfloxacin(SPFX)were used to induce FQNLs resistant mutants from a clinical susceptible isolate Kpn909with stepwise selection method,respectively,The susceptivity of bacteria to was determined by the standard method of two fold agar dilu?tion.RESULTS:The resistance of Kpn909to FQNLs was raised up gradually as FQNLs'concentration increased;Minimum inhibitory concentrations(MICs)of Kpn9098Selected by CIP at2?MIC(0.5mg/L)were16～32times higher than that of Kpn909,and showed resistant to ofloxacin(OFX),lomefloxacin(LMFX)and enofloxacin(ENX)with a MIC of8mg/L,16mg/L and8mg/L.Otherwise,SPFX-selected Kpn with a similar resistant level occurred at the concentration of8?MIC(1mg/L).The maximal selecting concentration of CIP and SPFX were128mg/L and64mg/L,and MIC of5FQNLs to the resistant mutants obtained at which were≥256mg/L and32～128mg/L,respectively.CONCLUSION:Both hydrophilic CIP and hydrophobic SPFX could induce Kpn the cross resistance to others FQNLs,but hydrophobic FQNLs may be superior to hydrophilic FQNLs to delay the resistance occurrence in Kpn.
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OBJECTIVE:To evaluate the cost-effectiveness of4oral antibiotics in the treatment of nongonococcal ure?thritis(cervicitis)(NGU).METHODS:The clinical data on both the homemade and imported oral azithromycin and sparflox_ acin in the treatment of NGU were collected and the cost-effectiveness analyses of which were conducted.RESULTS:The cure rates of the homemade azithromycin and sparfloxacin and the imported azithromycin and sparfloxacin were89.6%and83.2%,95.5%and88.3%,respectively.The cost-effectiveness ratios of which were39and139,140and220,respectively.CONCLUSION:Both the homemade and the imported azithromycin and sparfloxacin can effectively treat NGU but the cost-effectiveness of the homemade azithromycin is superior the homemade sparfloxacin,and that of the imported azithromycin is superior to the imported sparfloxacin as well.
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OBJECTIVE:To prepare compound sparfloxacin auristillae and to establish its quality control method.METHODS:The auristillae was prepared with glycerin and alcohol as solvents;the contents of econazole and sparfloxacin were determined by UV spectrophotometry with their respective detection wavelengths at360nm and297nm respectively,and the stability of which were determined as well.RESULTS:The linear concentration ranges of econazole and sparfloxacin were2～400?g/ml and0.4～80?g/ml respectively;the average recovery of econazole and sparfloxacin were100.96%(RSD=0.99%)and100.38%(RSD=0.44%)respectively.The expiry date(shelf life)of the finished products was above2years.CON?CLUSION:The preparation is simple in preparation,good in stability;and the quality control method is simple and easy,rapid,accurate and feasible.
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OBJECTIVE:To evaluate the cost-effectiveness of two therapeutic schemes for treatment of multi-drug resistant pulmonary tuberculosis.METHODS:80 multi-drug resistant pulmonary tuberculosis patients were randomly assigned to receive Sparfloxacine(trial group)or Ofloxacin(control group)plus anti-TB drugs(Rifapentine,Pyrazinamide,Sodium Aminosalicylate.Protionamide and Ethambatol)for 12 months.The curative effects and adverse drug reactions were monitored and the cost-effectiveness analyses were conducted.RESULTS:The costs in two groups(Sparfloxacin vs.Ofloxacin)were 10 143.25 and 7 841.65yuan,respectively;the negative-conversion rates of sputum bacteria after treatment for 12 months were 90.0% and 70.0%,respectively(P
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OBJECTIVE:To prepare in-situ gelling of hydrochloride sparfloxacin eye drops and establish its quality con-trol method.METHODS:The in-situ gelling of hydrochloride sparfloxacin eye drops were prepared with boric acid as buffer to regulate the pH and osmotic pressure and with sodium polymannuronate as peptizer.The content of hydrochloride sparflo-xacin was determined by ultraviolet spectrophotometry.The stability of the sustained-release eye drops was investigated as well.RESULTS:The sustained-release eye drops were colorless or yellowish limpid liquid with its test and identification results all in conformity with the related stipulation stated in Chinese Pharmacopeia(2005 edition).There was a good linear relationship within the concentration range of 3.0～8.0 ?g?mL-1 for hydrochloride sparfloxacin,and its average recovery was 99.82%(RSD=0.236%,n=6).There was no significant change for indexes in the accelerate test and sample test,yet the temperature and lighting did have slight impact on the viscosity,osmotic pressure and pH of the solution.CONCLUSION:The preparative method is simple and feasible and the quality of in-situ gelling of hydrochloride sparfloxacin eye drops is stable and controllable.
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Aim To observe the effect of hemodialysis on pharmacokinetics of sparfloxacin in thepatients contracting chronic renal failure. Methods Sparfloxacin concentrations inserum and urine of hemodialysis and non-dialysis patients were measured with a highperformance liquid chromatography method after administration a single oral dose of 200mg sparfloxacin. The pharmacokinetic parameters were computed with the programPKBP-N1.Results The main pharmacokinetic parameters in hemodialysis group wereT1/2(ka) - (1. 25 ?0. 57) h, T1/2(?) = (11. 88?4. 13) h, Tpeak = (4. 18 ? 0. 78) h,Cmax = (0.80 ? 0. 17) mg? L-1 and AUC0-= (6. 90 ? 3. 25) mg?h?L-1, while innon-dialysis group were T1/ 2(ka) = (1. 12 ? 0. 42) h, T1/ 2(?) = (15. 93 ? 5. 20) h, Tpeak =(3. 88 ? 0. 75) h, Cmax = (0. 69 ? 0. 37) mg?L -1, AUC0-= (10.05 ? 4. 13) mg?h?L-l. The original sparfloxacin discharge rats in urine within 24 h were (8. 98 ? 3. 92) % and(10. 58 ? 5. 64) % separately. T1/2(?) and AUC in hemodialysis group were markedly lowerthan in non-dialysis group (P
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Sparfloxacin is a new synthetic quinolone antimicrobial developed at the Research Laboratories of Dainippon Pharmaceutical Co, Ltd. To evaluate the efficacy and safty of sparfloxacin in acute pulmonary infection, we administered sparfloxacina(100mg) twice in a day to 30 patients who had sign and symptoms of acute pulmonary infectious diseases regardless of their underlying lung disease for 7 days. The results were : 1) A total 30 patients were enrolled in the trial. Among them 24 cases(80%) had underlying lung problems such as chronic obstructive pulmonary disease(36.4%), bronchiectasis(36.4%), bronchial asthma(3.3%), lung cancer(3.3%). 2) In 26 cases(86.6%), we observed effective improvement, and 4 cases(13.4%) show mildly effective improvement of symptoms and signs of respiratory infection. 3) In 23 cases(73.4%), we observed bacteriological eradication in culture or decreased the number of bacteria in Gram stain which found dominantly in previous Gram stain. 4) The significant side effect was not noted. The above results suggest that sparfloxacin was effective as a first line therapy in patients with acute respiratory infection.
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Humans , Bacteria , Communicable Diseases , Lung , Lung DiseasesABSTRACT
OBJECTIVE:To evaluate the cost-effectiveness of levofloxacin and sparfloxacin in the treatment of non?gonococcus urethritis(cervicitis)patients.METHODS:The clinical data of levofloxacin and sparfloxacin in the treatment of nongonococcus urethritis were collected with evidence-based medicine method and were evaluated with pharmacoeconomic cost-effectiveness analysis.RESULTS:The cure rates of two drugs were71.16%(62.00%,80.32%),81.69%(78.71%,85.21%)and cost-effectiveness ratios were2.29and2.71respectively.The?C/?E was5.57.CONCLUSION:The cost-ef?fectiveness ratio of levofloxacin was lower than that of sparfloxacin although the cure rate of sparfloxacin for nongonococcus urethritis was better.