葡萄糖酸依诺沙星注射液细菌内毒素的检测

目的 建立葡萄搪酸依诺沙星注射液细菌内毒素检查法.方法 参照〈中国药典〉2010年版二部附录细菌内毒素检查方法[1]要求进行试验,用不同批号的鲎试剂对葡萄糖酸依诺沙星注射液进行干扰试验.结果 葡萄糖酸依诺沙星注射液稀释4倍,对细菌内毒素检查无干扰.结论 细菌内毒素检查法代替热原检查法,方法可行.     

氧氟沙星、乳酸环丙沙星、葡萄糖酸依诺沙星注射液细菌内毒素检查方法标准研究

目的:建立氧氟沙星、乳酸环丙沙星、葡萄糖酸依诺沙星注射液细菌内毒素检查方法.方法:按2000年版中国药典二部附录XIE、XIXF进行实验和结果判断.结果:氧氟沙星、乳酸环丙沙星、葡萄糖酸依诺沙星注射液最大无干扰浓度分别为3、4、4倍稀释液(0.67mg/ml、0.5mg/ml、0.5mg/ml).结论:氧氟沙星、乳酸环丙沙星、葡萄糖酸依诺沙星注射液可以建立细菌内毒素检查项.     

注射用葡萄糖酸依诺沙星在木糖醇注射液中的稳定性观察

目的 观察室温(25℃)下注射用葡萄糖酸依诺沙星在木糖醇注射液中的稳定性.方法 用紫外分光光度法测定配伍液中注射用葡萄糖酸依诺沙星的含量,并观察外观、pH值的变化.结果 注射用葡萄糖酸依诺沙星与木糖醇注射液配伍后6h内其外观、pH值及含量均无明显变化.结论 室温(25℃)下注射用葡萄糖酸依诺沙星在木糖醇注射液中稳定性良好.     

注射用葡萄糖酸依诺沙星在木糖醇注射液中的稳定性观察

目的观察室温（25℃）下注射用葡萄糖酸依诺沙星在木糖醇注射液中的稳定性。方法用紫外分光光度法测定配伍液中注射用葡萄糖酸依诺沙星的含量,并观察外观、pH值的变化。结果注射用葡萄糖酸依诺沙星与木糖醇注射液配伍后6h内其外观、pH值及含量均无明显变化。结论室温（25℃）下注射用葡萄糖酸依诺沙星在木糖醇注射液中稳定性良好。     

葡萄糖酸依诺沙星注射剂质量分析

目的评价葡萄糖酸依诺沙星注射剂的质量现状和问题。方法采用法定检验方法并结合探索性研究,对葡萄糖酸依诺沙星注射剂的质量现状进行评价。结果现行标准中的有关物质项目存在明显缺陷;部分药包材对葡萄糖酸依诺沙星质量产生不良影响;由于葡萄糖酸依诺沙星在水溶液中光照降解明显,大输液的杂质含量明显高于其他剂型。结论葡萄糖酸依诺沙星注射剂现行标准存在不足,需要改进;药包材和葡萄糖酸依诺沙星注射液（大输液）的质量需加以关注。     

注射用葡萄糖酸依诺沙星的研究

论证选择试制可供注射用依诺沙星可溶性盐——葡萄糖酸依诺沙星的依据，研究了制备工艺并较好地解决了可供注射用成盐剂——Ｄ－葡萄糖酸的来源问题，适合于工业生产。试制的葡萄糖酸依诺沙星及其配制的依诺沙星注射液已获得卫生部批准。     

依诺沙星注射液与酚磺乙胺注射液的配伍稳定性观察

目的观察葡萄糖酸依诺沙星注射液与酚磺乙胺注射液在5％葡萄糖注射液中配伍的稳定性。方法在25℃下,模拟临床常用浓度,将葡萄糖酸依诺沙星注射液与酚磺乙胺注射液在5％葡萄糖注射液中配伍,观察6h内配伍液的外观,测定pH值,扫描紫外吸收图谱,用紫外分光光度法测定依诺沙星和酚磺乙胺的吸收度,计算依诺沙星和酚磺乙胺含量。结果6h内配伍液的外观、pH值和紫外吸收图谱均无明显变化,依诺沙星和酚磺乙胺含量无明显变化。结论在25℃下,葡萄糖酸依诺沙星注射液与酚磺乙胺注射液在5％葡萄糖注射液中配伍稳定,可配伍使用。     

盐酸氨溴索注射液在葡萄糖酸依诺沙星注射液中的配伍稳定性考察

目的考察盐酸氨溴索注射液与葡萄糖酸依诺沙星注射液配伍的稳定性。方法在室温[（20±1）℃],避光条件下,盐酸氨溴索与葡萄糖酸依诺沙星配伍后0～6 h内测定pH,观察外观及性状变化,采用高效液相色谱法-二极管阵列检测器测定盐酸氨溴索与葡萄糖酸依诺沙星的含量变化。结果 6 h内混合液外观、pH及含量均无明显变化。结论在室温[（20±1）℃]避光条件下,盐酸氨溴索注射液与葡萄糖酸依诺沙星注射液6 h内可以配伍使用。     

注射用葡萄糖酸依诺沙星与头孢哌酮钠舒巴坦钠及头孢匹胺钠的配伍变化

目的考察注射用葡萄糖酸依诺沙星分别与两种头孢菌素类抗生素混合发生的配伍变化.方法分别观察配伍液外观变化,采用酸度计测定pH值变化,应用紫外分光光度法测定葡萄糖酸依诺沙星含量变化.结果葡萄糖酸依诺沙星分别与两种头孢菌素类抗生素配伍时均出现浑浊,葡萄糖酸依诺沙星含量下降,下降的程度与其配伍浓度有关.结论葡萄糖酸依诺沙星与头孢匹胺钠及头孢哌酮钠舒巴坦钠存在配伍禁忌.     

葡萄糖酸依诺沙星与盐酸林可霉素配伍稳定性的研究

目的：研究葡萄糖酸依诺沙星注射液与盐酸林可霉素注射液的配伍稳定性。方法：考察溶液配伍前后的颜色、pH值、不溶性微粒等变化情况，并用UV法和HPLC法分别考察配伍前后葡萄糖酸依诺沙星和盐酸林可霉素的含量变化。结果：葡萄糖酸依诺沙星注射液与盐酸林可霉素注射液配伍．6h内溶液颜色基本无变化、pH值、不溶性微粒及含量无明显变化。结论：两药配伍后的理化性质稳定．在6h内可以配伍使用。     

葡萄糖酸依诺沙星注射液与利巴韦林注射液配伍稳定性的研究

目的研究葡萄糖酸依诺沙星注射液与利巴韦林注射液的配伍稳定性。方法考察溶液配伍前后的颜色、pH值、不溶性微粒等变化情况,并用UV和HPLC分别考察配伍前后葡萄糖酸依诺沙星和利巴韦林的含量变化。结果葡萄糖酸依诺沙星注射液与利巴韦林注射液配伍,6 h内溶液颜色基本无变化、pH值、不溶性微粒及含量无明显变化。结论两药配伍后的理化性质稳定,在6h内可以配伍使用。     

依诺沙星注射液与替硝唑注射液的配伍稳定性考察

目的考察葡萄糖酸依诺沙星注射液与替硝唑注射液配伍的稳定性。方法取依诺沙星注射液与替硝唑注射液配伍后的溶液,采用紫外分光光度法,测定其在25℃下6 h内不同时间的吸收度,计算依诺沙星、替硝唑配伍前后的含量。扫描紫外吸收图谱,观察溶液的外观,测定pH值。结果在25℃下,0～6 h内配伍液外观、pH值和紫外吸收图谱无明显变化,依诺沙星和替硝唑的含量无明显变化。结论依诺沙星注射液与替硝唑注射液在25℃下可配伍使用。     

葡萄糖酸依诺沙星致一过性视力丧失和听力下降

1例58岁女性患者有青霉素过敏史,因痔感染给予葡萄糖酸依诺沙星注射液0.4g,1次/d静脉滴注。治疗的第1～2天出现恶心和食欲下降。第3天治疗后约30min,患者出现视力丧失、听力下降、四肢颤抖和烦躁不安。给予异丙嗪和葡萄糖酸钙治疗,症状缓解。停用依诺沙星,未再出现上述症状。     

依诺沙星注射液与奥硝唑氯化钠注射液配伍稳定性考察

目的考察葡萄糖酸依诺沙星注射液与奥硝唑氯化钠注射液配伍稳定性。方法采用紫外分光光度法,在依诺沙星注射液与奥硝唑氯化钠注射液配伍后,测定溶液在25℃下6h内不同时间的吸收度,计算依诺沙星与奥硝唑配伍前、后的含量。扫描紫外吸收图谱,观察溶液的外观并测定其pH值。结果在25℃下,0～6h内配伍液外观、pH值和紫外吸收图谱无明显变化,依诺沙星和奥硝唑的含量无明显变化。结论依诺沙星注射液与奥硝唑氯化钠注射液在25℃下可配伍使用。     

The possible mechanism of interaction between xanthines and quinolone

To clarify the mechanism of interaction between theophylline and enoxacin, the effects of enoxacin and its metabolite, 4-oxo-enoxacin, on the disposition of new xanthine derivatives, 1-methyl-3-propylxanthine (MPX) and 3-propylxanthine (enprofylline), as models of theophylline have been investigated in rats. Pretreatment with enoxacin significantly delayed the elimination of MPX from plasma. No significant change in the volume of distribution of MPX was observed in the presence of enoxacin, but the total body clearance of MPX was significantly decreased by approximately 60 and 80% after pretreatment with 25 and 100 mg kg-1 of enoxacin, respectively. The amount of the decrease in total body clearance depended on the dose of enoxacin. 4-Oxo-enoxacin had little or no effect on MPX disposition. A newly developed quinolone, NY-198, which does not affect the disposition of theophylline, also did not affect the disposition of MPX. Enoxacin also had no effect on the disposition of enprofylline. These results indicate that the mechanism for decrease in theophylline clearance induced by enoxacin may not be due to its metabolite, 4-oxo-enoxacin, but to enoxacin itself, and that enoxacin does not inhibit solely the elimination process depending on cytochrome P450 isoenzyme for N-demethylation. It is likely that enoxacin has no influence on the renal excretion of xanthines.     

Evaluation of transdermal iontophoresis of enoxacin from polymer formulations: in vitro skin permeation and in vivo microdialysis using Wistar rat as an animal model

Polymers were used in vehicles to form hydrogel matrices in this study to evaluate the in vitro permeation and in vivo microdialysis of enoxacin. The highest transdermal delivery determined by area under flux-time curve (AUC) and intracutaneous enoxacin concentration were observed in methylcellulose (MC) and polyvinylpyrrolidone (PVP) hydrogels, respectively. To avoid the pH shift in vehicles during iontophoresis, buffer species were added to formulations to increase the buffer capacity. As expected, the permeability of enoxacin of anodal iontophoresis was larger than that of cathodal iontophoresis. Combination of benzalkonium chloride, a cationic surfactant as an enhancer, and iontophoresis exerted an enhancing effect for anionic enoxacin at pH 10.0. However, no effect or a negative effect was detected for cationic enoxacin in deionized water or pH 5.0 buffer, due to the shielding of the negative charge in the skin. The skin residue of enoxacin was slightly increased after the incorporation of Azone in PVP hydrogel. The result of in vivo microdialysis was in accordance with that of in vitro study. The effect of Azone on the intracutaneous enoxacin was more significant for in vivo microdialysis than in the in vitro study indicating the clinical feasibility of Azone for iontophoretic delivery. Microdialysis can be considered as a useful technique to investigate the pharmacokinetics of transdermal iontophoresis in vivo.     

The effect of age on the pharmacokinetics of enoxacin

Summary We have studied the pharmacokinetics of enoxacin in two groups of subjects, 10 young (18–45 years) and 10 elderly adults (>65 years) after a single oral dose of enoxacin (600 mg). Enoxacin was absorbed rapidly, peak plasma concentrations being reached within two hours in both groups. However, the peak plasma concentration of enoxacin was significantly higher in the elderly than in the young adults. The area under the concentration-time curve extrapolated to infinity was also significantly greater in the elderly compared with the young subjects, and the apparent renal clearance was significantly less in the elderly than in the young adults. Consequently, the urinary elimination of unchanged enoxacin was significantly reduced in the elderly. The apparent volume of distribution in the elderly was significantly less than in the young adults. The elimination half-time of enoxacin was similar in the two groups.     

The pH dependent uptake of enoxacin by rat intestinal brush-border membrane vesicles.

The mechanism of the intestinal transport of enoxacin, an orally active fluoroquinolone antibiotic, has been investigated using brush-border membrane vesicles isolated from rat small intestine. The initial rate and time-course of enoxacin uptake were considerably dependent upon the medium pH (pH 5.5 greater than pH 7.5) and upon the percent ionization of the carboxyl group (pKa 6.2, anionic charge), namely, the degree of uptake of cationic form was higher than that of the zwitterionic form. There was evidence of transport into the intravesicular space as shown by the effect of extravesicular medium osmolarity on enoxacin uptake at steady state (30 min). This transport across the brush-border membrane was stimulated by the valinomycin-induced K(+)-diffusion potential (interior negative) and an outward H(+)-diffusion potential. Furthermore, changing the pH of the medium from 5.5 to 7.5 significantly decreased the effect of valinomycin-induced K(+)-diffusion potential on the enoxacin uptake. These results suggest that the uptake behaviour of the cationic form of enoxacin plays an important role in the intestinal absorption process of enoxacin.     

Effect of liposomes and niosomes on skin permeation of enoxacin

The skin permeation and partitioning of a fluorinated quinolone antibacterial agent, enoxacin, in liposomes and niosomes, after topical application, were elucidated in the present study. In vitro percutaneous absorption experiments were performed on nude mouse skin with Franz diffusion cells. The influence of vesicles on the physicochemical property and stability of the formulations were measured. The enhanced delivery across the skin of liposome and niosome encapsulated enoxacin had been observed after selecting the appropriate formulations. The optimized formulations could also reserve a large amount of enoxacin in the skin. A significant relationship between skin permeation and the cumulative amount of enoxacin in the skin was observed. Both permeation enhancer effect and direct vesicle fusion with stratum corneum may contribute to the permeation of enoxacin across skin. Formulation with niosomes demonstrated a higher stability after 48 h incubation compared to liposomes. The inclusion of cholesterol improved the stability of enoxacin liposomes according to the results from encapsulation and turbidity. However, adding negative charges reduced the stability of niosomes. The ability of liposomes and niosomes to modulate drug delivery without significant toxicity makes the two vesicles useful to formulate topical enoxacin.