RP-HPLC测定甲硝唑阴道泡腾片中甲硝唑含量

目的 采用反相高效液相色谱法测定甲硝唑阴道泡腾片中甲硝唑的含量。方法 采用Alltima C₁₈色谱柱（150 mm×4.6 mm,5 μm）,以甲醇-水（20∶80）为流动相,流速1.0 mL·min^-1,紫外检测器检测波长为320 nm。结果 RP-HPLC测定的线性范围为0.13～0.40 mg·mL^-1,r＝1.000;样品溶液在24 h内稳定;平均回收率为100.1％,RSD为1.0％（n＝9）;日内和日间RSD分别为0.7％和1.2％。结论 采用RP-HPLC测定甲硝唑阴道泡腾片中甲硝唑的含量,专属性强,结果准确可靠。     

HPLC法同时测定氯甲醑中氯霉素和甲硝唑的含量

目的：建立HPLC法同时测定氯甲醑中氯霉素及甲硝唑的含量。方法：采用HPLC法,色谱柱为Nov-pak C18（150mm×4.6 mm,5μm）,流动相为甲醇∶水（75∶25）,流速为1.0 ml·min-1,检测波长为297 nm,柱温：30℃,进样量20μl。结果：甲硝唑和氯霉素线性范围分别为5~80μg·ml-1（r=0.999 7）和50~800μg·ml-1（r=0.999 8）;平均回收率分别为100.83%（RSD=1.82%,n=6）和100.20%（RSD=0.55%,n=6）。结论：本法快速方便、精密度高、重复性和稳定性好,可用于同时测定氯甲醑中氯霉素和甲硝唑的含量。     

反相高效液相色谱法测定甲硝唑胶囊中甲硝唑含量

目的 采用反相高效液相色谱法（RP-HPLC法）测定甲硝唑胶囊的含量。方法 采用Shim-pack CLC-ODS柱，流动相为甲醇一水（30：70），检测波长为290nm，外标法测定。结果 甲硝唑的线性范围为50～500μg／mL（r=0．9995），平均回收率为99．5％，RSD=1．0％（n=6）。结论 RP-HPLC法测定甲硝唑胶囊中甲硝唑含量，方法准确，操作简便，结果可靠。     

HPLC法测定氯甲霜中氯霉素和甲硝唑的含量

目的：建立高效液相色谱法测定氯甲霜中氯霉素和甲硝唑含量.方法：色谱柱Diamonsil C18（250 mm×4.6 mm,5μm）,流动相为0.1%庚烷磺酸钠溶液（0.1%庚烷磺酸钠溶液500 ml与二甲基甲酰胺5 ml,冰醋酸0.5 ml）-乙腈（80：20）,流速为1.0 ml·min-1,检测波长为278 nm.结果：氯霉素和甲硝唑浓度在30～150μg·ml-1范围内均呈良好的线性关系,r=0.999 6和r=0.998 1 平均回收率分别为101.23%（RSD=0.69%）,99.63%（RSD=0.61%）（n=9）.结论：本方法简便,准确,可用于氯甲霜中氯霉素和甲硝唑的含量测定.     

HPLC法测定复方氯霉素阴道泡腾片中己烯雌酚的含量

目的:建立高效液相色谱法测定复方氯霉素阴道泡腾片中己烯雌酚的含量。方法:色谱柱为DIONEX C₁₈（250mm×4.6mm,5μm）;流动相为甲醇-水（75:25）;流速为1.0 ml·min^-1;检测波长为239nm;进样量为50μl。结果:己烯雌酚的线性范围为1.1～8.6μg·ml^-1（r=0.9999）;平均回收率为100.8%（RSD=1.9%）。结论:本方法结果准确可靠,可作为复方氯霉素阴道泡腾片中己烯雌酚的含量测定方法。     

HPLC双波长切换法同时测定复方唑克搽剂中甲硝唑和盐酸克林霉素的含量

目的：建立高效液相色谱法同时测定复方唑克搽剂中甲硝唑和盐酸克林霉素的含量.方法：采用Thermo Syncronics C18（250 mm×4.6 mm,5 μm） 色谱柱;流动相为0.05 mol·L-1磷酸二氢钾溶液（用25%氢氧化钾调节pH至7.5）-乙腈（55：45）;流速为1.0 ml·min-1;柱温为30℃;波长切换,0～5 min在230 nm波长下测定甲硝唑含量,5～10 min在210 nm波长下测定盐酸克林霉素含量.结果：甲硝唑在198.50～1 389.50 μg·ml-1（r=0.999 9）,盐酸克林霉素在102.74～719.18 μg· ml-1（r=0.999 9）的浓度范围内呈良好的线性关系;甲硝唑的平均加样回收率为98.09%,RSD为0.37%（n=9）,盐酸克林霉素的平均加样回收率为98.05%,RSD为0.60%（n=9）.结论：该方法简便、准确,结果稳定,可为复方唑克搽剂的质量评价提供依据.     

RP—HPLC法测定复方甲硝唑片中甲硝唑和维生素B6的含量

目的 建立RP-HPLC法测定复方甲硝唑片中甲硝唑和维生素B6的含量.方法 采用Shim-pack CLC-ODS柱(4.6 mm×200 mm, 5 μm),甲醇-水(30∶70)为流动相,290 nm为检测波长,外标法测定含量.结果 甲硝唑和维生素B6的线性范围分别为50～500 μg*ml-1(r=0.999 6),5～50 μg*ml-1(r=0.999 8),平均回收率分别为100.2%(RSD=0.93%),99.5% (RSD=0.42%),n=6.结论 RP-HPLC法测定复方甲硝唑片中甲硝唑和维生素B6的含量,方法准确,操作简便,结果可靠.     

高效液相色谱法测定复方甲硝唑栓中甲硝唑及诺氟沙星的含量

目的建立测定复方甲硝唑栓中甲硝唑及诺氟沙星含量的高效液相色谱法.方法采用Symmetry C18色谱柱(4.6 mm×150 mm,5μm),以乙腈-0.03 mol·L-1磷酸溶液(用三乙胺调节pH 3.0)(15;85)为流动相,流速为1.0 mL·min-1,检测波长为315 nm.结果甲硝唑及诺氟沙星在浓度范围内,峰面积与其浓度线性均关系良好(甲硝唑r=0.999 9,诺氟沙星r=1.000 0),平均回收率分别为100.64%和100.29%,精密度试验RSD分别为0.1%和0.2%,重复性试验RSD分别为1.5%和0.92%.结论该方法准确,简便,快速,专属性强,灵敏度高,适用于复方甲硝唑栓中甲硝唑及诺氟沙星的含量测定.     

高效液相色谱法测定甲硝唑乳膏中甲硝唑的含量

目的建立高效液相色谱法测定医院制剂甲硝唑乳膏中甲硝唑的含量。方法色谱柱为Hy-persil BDS-C18（250 mm×4.6 mm,5μm）;流动相为甲醇-水（20∶80）;流速为1.0 mL/min;检测波长为320 nm;柱温为30℃;进样体积为20μL。结果甲硝唑在5.02～40.16μg/mL（r=0.999 9）范围内线性关系良好,平均回收率（n=9）为98.2%（RSD=2.5%）。结论本方法操作简便、结果准确,可作为甲硝唑乳膏的质量控制方法。     

甲硝唑克霉唑凝胶的制备及其含量测定

目的制备甲硝唑克霉唑凝胶,并建立其质量控制方法。方法凝胶基质中加入甲硝唑、克霉唑制得甲硝唑克霉唑凝胶,用高效液相色谱仪测定甲硝唑、克霉唑的含量。色谱柱：Lichrosorb RP-18柱（4.6mm×200mm,5μm）;流动相：乙腈-缓冲液=30∶70;流速：1.0mL.min^-1;波长：260nm;进样量：20μL。结果甲硝唑在49.50-495.00μg.mL^-1线性关系良好,回归曲线Y=21.307X-1.8158（r=0.9999）,平均回收率为98.6%,RSD为1.55%（n=9）;克霉唑在39.6-396.00μg.mL^-1线性关系良好,回归曲线Y=14.028X-27.785（r=0.9999）,平均回收率为100.8%,RSD为1.29%（n=9）。结论处方组成合理,制剂稳定,含量测定方法准确。     

莫西沙星与加替沙星治疗女性尿路感染的疗效比较

目的评价莫西沙星、加替沙星对女性尿路感染的临床疗效。方法将299例单纯性、急性、非淋菌性和混合性尿路感染女性患者随机分为莫西沙星组150例和加替沙星组149例,分别口服莫西沙星和加替沙星400mg／d,疗程均为7d。结果莫西沙星组与加替沙星组临床总有效率分别为96．00％和95．30％,病原菌清除率分别为89．89％和87．10％,不良反应率分别为8．00％和8．72％,组间比较均无显著性差异（P〉0．05）。结论莫西沙星与加替沙星治疗女性尿路感染安全有效,均可作为第一线药物使用。     

In vitro activity of gatifloxacin compared with gemifloxacin, moxifloxacin, trovafloxacin, ciprofloxacin and ofloxacin against uropathogens cultured from patients with complicated urinary tract infections

Minimum inhibitory concentrations (MICs) of gatifloxacin were compared with those of gemifloxacin, moxifloxacin, trovafloxacin, ciprofloxacin and ofloxacin using an agar dilution method for 400 uropathogens cultured from the urine of urological patients with complicated and/or hospital-acquired urinary tract infections (UTI). The collection of strains was made up of Enterobacteriaceae (34.5%), enterococci (31.5%), staphylococci (21.2%) and non-fermenting bacteria (12.8%). The antibacterial activity of the three newer fluoroquinolones, gatifloxacin, gemifloxacin, and moxifloxacin, were similar, but showed some drug specific differences. Gemifloxacin was most active against Escherichia coli, but less so against Proteus mirabilis. In this series all isolates of E. coli were inhibited at a MIC of 0.25 mg/l gatifloxacin and moxifloxacin and by 0.125 mg/l gemifloxacin. The MIC distribution of all fluoroquinolones showed a bimodal distribution for staphylococci, enterococci and Pseudomonas aeruginosa. The two modes for P. aeruginosa were 1 and 64 mg/l for gemifloxacin and moxifloxacin and 0.5 and 64 mg/l for gatifloxacin. For staphylococci the two modes were 0.125 and 2 mg/l for gatifloxacin, 0.03 and 4 mg/l for gemifloxacin, and 0.03 and 2 mg/l for moxifloxacin; for enterococci, 0.25 and 16 mg/l for gatifloxacin, 0.06 and 2 mg/l for gemifloxacin, and 0.25 and 8 mg/l for moxifloxacin. Compared with trovafloxacin the MICs were similar, but the newer fluoroquinolones were more active than ciprofloxacin and ofloxacin against Gram-positive bacteria. Of the newer fluoroquinolones gatifloxacin had the highest rate of renal excretion and could be considered a promising alternative fluoroquinolone agent for the treatment of UTI.     

Efficacy of moxifloxacin or gatifloxacin as prophylaxis against experimental murine Brucella melitensis infection

The prophylactic potential of moxifloxacin and gatifloxacin was assessed in comparison with doxycycline, an established therapeutic antibiotic, to limit or control infection by Brucella melitensis in an experimental mouse model, determined by reduced bacterial burden in the spleen. Although moxifloxacin was found to have a small protective effect when administered 6 h following infection, neither moxifloxacin nor gatifloxacin showed significant efficacy in vivo. In comparison, doxycycline provided significant protection when prophylaxis was started at 6 h, 7 days or 14 days following infection. Overall, these results confirm the utility of doxycycline in the prophylaxis of brucellosis and suggest that neither moxifloxacin nor gatifloxacin are likely to be valuable for post-exposure prophylaxis of Brucella infection.     

6种氟喹诺酮类药物对凝固酶阴性葡萄球菌的防耐药变异浓度分析

目的 比较6种氟喹诺酮类药物对临床分离凝固酶阴性葡萄球菌耐药突变体的选择能力.方法 选择呼吸道标本,对苯唑西林、环丙沙星敏感的凝固酶阴性葡萄球菌34株,采用标准琼脂二倍稀释法、标准琼脂平板稀释法,测定6种氟喹诺酮类药物对凝固酶阴性葡萄球菌的最低抑菌浓度(MIC)、防耐药变异浓度(MPC).结果 MPC值比较,莫西沙星最低(MPC90为1 mg/L),左氧氟沙星和环丙沙星最高(MPC90均为32 mg/L).莫西沙星、卡屈沙星和加替沙星的MPC90/MIC90较低,均为2.结论 莫西沙星、卡屈沙星和加替沙星对凝固酶阴性葡萄球菌的MPC值较低,突变选择窗范围相对较窄.     

In vivo experimental approach for the risk assessment of fluoroquinolone antibacterial agents-induced long QT syndrome

The proarrhythmic effects of fluoroquinolone antibacterial agents, sitafloxacin, gatifloxacin and moxifloxacin, were compared using three in vivo models. In the halothane-anesthetized dogs (n=5), intravenous 10-min infusion of gatifloxacin and moxifloxacin (1-3 mg/kg) prolonged the ventricular effective refractory period and the repolarization period to a similar extent, whereas sitafloxacin (1-3 mg/kg) prolonged the former only. No significant change was detected in other cardiovascular parameters. In the chronic complete atrioventricular block dogs (n=4), oral administration of 100 mg/kg of gatifloxacin (2 of 4) and moxifloxacin (3 of 4) induced torsades de pointes, which was not observed by sitafloxacin. In the alpha-chloralose-anesthetized rabbits (n=5), intravenous 20-min infusion of 60 mg/kg of gatifloxacin induced torsades de pointes (1 of 5) in the presence of methoxamine infusion, which was not observed by sitafloxacin or moxifloxacin. Thus, the halothane-anesthetized model is suitable for assessing QT prolongation, whereas the chronic complete atrioventricular block model is sensitive for detecting torsadogenic action of drugs. The alpha-chloralose-anesthetized model is the simplest and least expensive method, but its sensitivity to detect proarrhythmic action may be less great.     

Ocular penetration of moxifloxacin 0.5% and gatifloxacin 0.3% ophthalmic solutions into the aqueous humor following topical administration prior to routine cataract surgery

A prospective, double-masked, randomized, parallel-group study (n = 25) was conducted to examine the ocular penetration of moxifloxacin 0.5% ophthalmic solution and gatifloxacin 0.3% solution into the aqueous humor following topical administration prior to routine cataract surgery. One drop of antibiotic was instilled every 10 min for four doses beginning 1 h prior to surgery. Preliminary results showed aqueous humor concentrations for moxifloxacin that were significantly greater (p < 0.01) than those for gatifloxacin.     

A comparison of the fourth-generation fluoroquinolones gatifloxacin 0.3% and moxifloxacin 0.5% in terms of ocular tolerability

PURPOSE: To compare the ocular tolerability of the commercially available ophthalmic solutions of the fourth-generation fluoroquinolones, gatifloxacin 0.3% (Zymar, Allergan, Inc., Irvine, CA) with benzalkonium chloride (BAK) and moxifloxacin 0.5% (Vigamox) without BAK. METHODS: A baseline evaluation was conducted on 30 healthy volunteers for conjunctival hyperemia, conjunctival vascularity, pupil size, and anterior chamber (AC) cell and flare. Pupils were measured under scotopic conditions with a Colvard pupillometer. Conjunctival hyperemia and vascularity, and AC reaction were measured on a Likert-like scale of 0-3. Subjects then received drops in both eyes from masked bottles of gatifloxacin ophthalmic solution 0.3% with BAK (in one eye determined randomly) and moxifloxacin ophthalmic solution 0.5% without BAK (in the contralateral eye) in a double-masked fashion. Subjects graded pain and ocular irritation in each eye on a scale of 1-10 after 5 min with their eyes closed. The examination was then repeated. RESULTS: The average age of this study population was 34.4 years. The groups of eyes receiving moxifloxacin 0.5% demonstrated an increase in mean conjunctival hyperemia (0.21 [range: 0-1] at baseline to 1.52 [range: 0-3] at 5 min.) that was significantly greater (p = 0.0005) compared with that of the group receiving gatifloxacin 0.3% (0.22 [range: 0-1] at baseline to 0.45 [range: 0-2] at 5 min). The group receiving moxifloxacin 0.5% showed an increase in conjunctival vascularity (0.55 [range: 0-1] at baseline to 1.61 [range: 0.5-3] at 5 min.) that was significantly greater (p = 0.0005) compared with that of the group receiving gatifloxacin 0.3% (0.52 [range: 0-1] at baseline to 0.68 [range: 0-2] at 5 min.). Significantly less pain (1.2 vs. 3.2, p = 0.001) and irritation (0.64 vs. 3.42, p = 0.001) occurred with gatifloxacin 0.3% than with moxifloxacin 0.5%. Pupil size was significantly reduced (5.65 mm-5.05 mm) in eyes receiving moxifloxacin 0.5% (p = 0.004) and no significant change occurred in pupil size (5.60 mm-5.65 mm) in eyes that received gatifloxacin 0.3% (p = 0.878). No AC reaction was noted with either medication. CONCLUSIONS: The group of eyes receiving gatifloxacin 0.3% with BAK demonstrated greater ocular tolerability in comparison to the group receiving moxifloxacin 0.5% without BAK. Moxifloxacin-induced pupillary miosis may be due to prostaglandin release in the anterior chamber. A limitation of this study is the relatively young age of the study population.     

Comparison of minimal inhibitory and mutant prevention drug concentrations of 4 fluoroquinolones against clinical isolates of methicillin-susceptible and -resistant Staphylococcus aureus

Staphylococcus aureus remains an important human pathogen affecting both outpatients and those hospitalized. Increasing antimicrobial resistance is global but prevalence rates are variable for different geographical areas. Fluoroquinolones have been used to treat S. aureus infections and the newer quinolones have enhanced in vitro activity against this organism. The mutant prevention concentration (MPC) defines the antimicrobial drug concentration threshold that would require an organism to simultaneously possess two mutations for growth in the presence of the drug. We tested clinical isolates of methicillin-susceptible (MSSA) and methicillin-resistant (MRSA) S. aureus by minimum inhibitory concentration (MIC) and MPC against gatifloxacin, gemifloxacin, levofloxacin and moxifloxacin. For MSSA strains, the rank order of potency based on MIC(90) values were gemifloxacin (0.063 mg/l) = moxifloxacin (0.063 mg/l) > gatifloxacin (0.05 mg/l) = levofloxacin (0.25 mg/l) and by MPC values moxifloxacin (0.25 mg/l) > gemifloxacin (0.5 mg/l) > gatifloxacin (1 mg/l) = levofloxacin (1mg/l). For 87% of the isolates the MPC value was 0.5 mg/l for gatifloxacin. The rank order of potency based on the time the serum drug concentration exceeded the MPC(90), was as follows: moxifloxacin (>24 h) > levofloxacin (>18 h) > gatifloxacin (12 h) > gemifloxacin (9 h). Serum drug concentration remained in excess of the MPC(87) for 24 h for gatifloxacin. Both MIC(90) and MPC(90) values were higher against MRSA strains and the time above the MPC(90) was significantly shorter for all agents.     

HPLC-FLD同时测定全血中加替沙星和莫西沙星含量

目的建立一种灵敏、可靠的全血中加替沙星和莫西沙星的高效液相色谱荧光检测方法。方法样品经磷酸盐缓冲液提取后,用Waters OasisMAX小柱进行净化,甲醇-乙腈-0.2%甲酸（15∶15∶70）为流动相,采用Cloversil-C18柱（3.0mm×150mm,5μm）分离,荧光检测波长：λex288nm和λem493nm,内标法定量。结果加替沙星和莫西沙星在15.0～240.0μg·L^-1内呈良好线性,方法回收率在97.7%～101.3%之间,日内RSD〈6.0%,其定量限为15.0μg·L^-1。结论本方法简便、灵敏、干扰少,特异性好,能满足血液中加替沙星和莫西沙星的检测要求。