Stability and antibacterial potency of ceftazidime and vancomycin eyedrops reconstituted in BSS® against Pseudomonas aeruginosa and Staphylococcus aureus

Purpose: We aimed to study the stability and the in vitro antibacterial potency of ceftazidime and vancomycin eyedrops against Pseudomonas aeruginosa and Staphylococcus aureus, respectively, under different storage temperatures and light conditions. Methods: Solutions of ceftazidime 50 mg/ml and vancomycin 50 mg/ml were prepared by reconstituting with balanced salt solution (BSS^®) and stored at 4 °C and at 24 °C with and without exposure to light. The minimum bactericidal concentrations against P. aeruginosa and S. aureus were measured to evaluate the antimicrobial potency over a 4‐week period. Changes in the pH values and physical characteristics of the solutions were recorded over the same period of time. Results: The antibacterial potency of ceftazidime decreased significantly from days 3 and 7 onwards at storage temperatures of 24 °C and 4 °C, respectively, but was not affected by light exposure. The pH value progressed from acidic to alkaline, peaking at day 3, in all solutions. The antibacterial potency of vancomycin remained stable during the 4‐week period, but its pH showed a slight progression from acidic to less acidic, in all solutions. Conclusions: Ceftazidime eyedrops in BSS^® appear to remain effective against P. aeruginosa for ≥ 7 days when stored at 4 °C, but were less effective when stored at 24 °C. Loss of antibacterial potency coincides with the appearance of visual and olfactory signs of degradation. The transient rise in pH at day 3 is a matter of possible concern, however, as it may affect patient tolerance. By contrast, vancomycin eyedrops in BSS^® can be safely used for ≥ 4 weeks, stored at either 4 °C or 24 °C.     

氟康唑滴眼液的制备及临床应用

目的：将氟康唑制成0．2％滴眼液,用于治疗真菌性角膜溃疡,观察其临床疗效。方法：以无菌方法配置成滴眼液,选用紫外分光光度计（uv -200）测定滴眼液含量,对21例真菌性角膜溃疡进行对照分组疗效观察。结果：氟康唑滴眼液制备,含量测定方法简便,可靠,结果准确,对真菌性角膜溃疡总有效率为95．2％。结论：氟康唑滴眼液是一种可供临床选用的真菌性角膜溃疡用药。     

含加替沙星方案治疗耐药肺结核临床观察

目的观察和分析含加替沙星方案治疗耐药肺结核的疗效。方法对2004年7月-2006年12月期间收治资料完整的120例耐药肺结核病例,分为治疗组60例,对照组60例。治疗组应用含加替沙星联合抗结核化学药物,对照组应用含环丙沙星的抗结核化学药物。两组其他抗结核药物组成相同。疗程1年。结果两组病例疗程结束时,痰结核菌转阴率治疗组93.3%,明显高于对照组85.0%（P〈0.05）。治疗组病灶吸收和空洞闭合率分别为98.4%和65.6%;对照组病灶吸收率和空洞闭合率分别为75.0%和45.5%（P〈0.05）。结论在痰菌阴转、病灶吸收、空洞闭合方面含加替沙星方案均明显优于含环丙沙星方案。并且在完成强化期治疗时,含加替沙星方案痰菌阴转情况明显优于含环丙沙星方案。     

Determination of drug concentration in aqueous humor of cataract patients administered gatifloxacin ophthalmic gel

Background Ophthalmic gel has been developed to increase the drug concentration in aqueous humor and to retard the loss of drug from the conjunctival sac.The research was to compare the drug concentration in aqueous humor of cataract patients administered 0.3% gatifloxacin ophthalmic gel with that in patients administered 0.3% gatifloxacin ophthalmic solution.Methods Ninety-six patients with cataract （96 eyes） were randomly assigned to 8 groups.The patients in groups 1-4received topical gatifloxacin 0.3% ophthalmic gel and those in groups 5-8 received gatifloxacin 0.3% ophthalmic solution.The dose regimen was 1 drop, 4 times a day for 3 consecutive days prior to cataract surgery.On the day of surgery, 1drop was applied at 15, 30, 60 or 120 minutes before commencement of cataract surgery in groups 1 and 5, groups 2 and 6, goups 3 and 7, and groups 4 and 8, respectively.Aqueous humor was extracted during the cataract surgery for the analysis of gatifloxacin concentration..Results The concentrations of gatifloxacin in aqueous humor were （0.24±0.25） μg/ml, （1.11±0.74） μg/ml, （2.32±2.01）μg/ml and （1.85±1.14） μg/ml in groups 1 to 4, and （0.16±0.25） μg/ml, （0.31±0.24） μg/ml, （0.75±0.28） μg/ml and （0.33±0.22） μg/ml in groups 5 to 8, respectively.Patients receiving gatifloxacin ophthalmic gel showed greater mean values of gatifloxacin concentration in aqueous humor than those receiving gatifloxacin solution, and such differences were significant with P 〈0.05 for all comparisons except that between groups 1 and 5.Conclusion Topical gatifloxacin ophthalmic gel can attain significantly greater drug concentrations in human aqueous humor than gatifloxacin ophthalmic solution.     

加替沙星和左氧氟沙星序贯治疗尿路感染的成本-效果比较

目的对加替沙星和左氧氟沙星序贯治疗尿路感染进行成本-效果比较分析。方法将85例尿路感染患者随机分成两组,A组42例给予加替沙星序贯疗法,B组43例给予左氧氟沙星序贯疗法,运用药物经济学方法最小成本-效果分析。结果A组和B组的总有效率分别为85．71％和88．37％,细菌清除率分别为90．48％和93．02％,不良反应发生率分别为7．14％和4．65％,成本效果比分别为2．42和1．87。结论对于尿路感染患者,采用左氧氟沙星序贯疗法比加替沙星序贯疗法具成本-效果优势,值得临床应用推广。     

加替沙星注射液的研制和质量控制

目的 :探讨加替沙星注射液的处方、制备工艺及质量控制方法。方法 :以盐酸、氢氧化钠为 pH调节剂及氯化钠为等渗调节剂制备加替沙星注射液 ;采用高效液相色谱法测定本品的含量。结果 :制备的加替沙星注射液 (pH 5 .0 )在高温 (80°C)、光照(3 60 0lx) 1 0d及室温留样考察 2 4mo ,物理及化学性质稳定。结论 :处方及工艺经中试放大制备的注射液性质稳定 ;质量控制方法准确可靠 ;可满足临床用药要求。     

单剂量加替沙星口服在Beagle犬体内药代动力学研究

目的探讨加替沙星口服后在Beagle犬体内药代动力学。方法将18只Beagle犬分为3组,分别灌服34,17,8.5mg/kg加替沙星,于给药后0.5,1,2,4,6,8,12,24,36,48,60h取血,以高效液相色谱法测定血药浓度,用3P97程序分析。结果高、中、低剂量组动物吸收相半衰期(t1/2ka)分别为(0.82±0.96),(0.78±0.77),(1.33±0.43)h,消除相半衰期(t1/2ke)分别为(7.33±1.79),(6.32±3.28),(5.34±2.60)h,达峰时间(tmax)分别为(6.32±2.32),(3.95±2.18),(5.77±1.62)h,峰浓度(Cmax)分别为(6.31±2.66),(2.67±0.64),(0.64±0.30)mg/mL。药时曲线下面积(AUC0→60)分别为(110.86±43.76),(41.93±5.58),(8.58±2.70)μg·h/mL。结论加替沙星口服易吸收,血药浓度高,代谢慢,临床使用方便。     

LSS法估算COPD患者茶碱缓释片单用及联用加替沙星时稳态药-时曲线下面积

目的用有限采样法（limited sampling strategy,LSS）估算慢性阻塞性肺疾病（COPD）患者单用茶碱缓释片及联用加替沙星时稳态药一时曲线下面积（AUC0-12^ss）。方法测得16名COPD患者口服茶碱缓释片稳态时（单用及联用加替沙星）的血药浓度,以多元线性回归法建立（AUC0-12^ss与不同时间点的血药浓度的关联数学模型,并用Jackknife法进行验证。结果单点预测时可以采用给药后2h或4h的血药浓度值预报药-时曲线下面积,单用茶碱回归方程为：AUC0-12^ss=-3．01＋11．15C2（R^2=0．97,P〈0．05）或AUC0-12^ss=-1．34＋10．91 C4（R^2=0．97,P〈0．05）。联用加替沙星的回归方程：AUC0-12^ss-3．14＋10．27 C2（R^2=0．90,P〈0．05）或AUC0-12^ss=-9．68＋11．74 C4（R^2=0．96,P〈0．05）。二点预测可用给药后2h及12h的血药浓度值,单用茶碱回归方程为：AUC0-12^ss=-0．28＋8．47 C2＋3．18 C12（R^2=0．98,P〈0．05）。联用加替沙星回归方程为：AUC0-12^ss=5．74＋3．64 C2＋8．54 C12（R^2=0．99．P〈0．05）。结论考虑到给药后2h为药物的达峰时间,推荐单点预测时用给药后2h的血药浓度值;用2个浓度点进行预测采用给药后2、12h的血药浓度值。