复方甲磺酸培氟沙星口服液的制备及安全性试验

发布时间：2018-04-18 08:53

本文选题：甲磺酸培氟沙星 + 对乙酰氨基酚　；参考：《西北农林科技大学》2015年硕士论文

【摘要】：目的:本试验以甲磺酸培氟沙星为主药,确定了用于治疗由培氟沙星敏感菌所导致的各种感染的复方口服制剂,并且利用紫外分光光度计法建立了测定方法,同时又从其理化性质、稳定性、体外抑菌效果以及安全性等方面对复方甲磺酸培氟沙星口服液做了深入的研究,以确定其能否成为一种广谱的、新型、高效、安全可靠的抗菌解热药,从而给以后复方甲磺酸培氟沙星口服液在兽医临床上的开发及应用提供有效的理论依据。方法:①根据口服液自身的特征和各成分的属性,确定口服液中所用增溶剂、络合剂、防腐剂等的最佳组成及其比例。②利用紫外分光光度法,建立含量分析方法。③通过强光照射试验、高温和低温试验以及加速试验考察复方甲磺酸培氟沙星口服液的稳定性。④对沙门氏菌、金黄色葡萄球菌、无乳链球菌、大肠杆菌这4种细菌MIC试验确定其体外抑菌浓度。⑤依据急性毒性试验对复方甲磺酸培氟沙星口服液进行安全性评价。结果:本试验筛选出来的最佳配方是:甲磺酸培氟沙星2%,对乙酰氨基酚0.2%,络合剂EDTA-2Na适量,防腐剂焦亚硫酸钠适量,增溶剂乙醇和PEG400适量,纯化水加至100mL。通过紫外分光光度法,在277 nm和202 nm处分别测定复方甲磺酸培氟沙星口服液中甲磺酸培氟沙星和对乙酰氨基酚的含量,该分析方法的精密度高,回收率和重复性好。稳定性试验结果表明,复方甲磺酸培氟沙星口服液对光照敏感、对温度变化不敏感,需要避光保存。该制剂对沙门氏菌、金黄色葡萄球菌、无乳链球菌、大肠杆菌这4种细菌的均有抗菌活性,较甲磺酸培氟沙星单药的抗菌活性有明显的提高。对雏鸡的LD50为1453.3mg/kg,这表明该制剂安全性良好,毒性低,临床上可以广泛应用。结论:本试验确定的复方甲磺酸培氟沙星口服液,符合质量要求,且制备工艺简单,可以扩大生产应用于兽医临床。
[Abstract]:Objective: to determine the compound oral preparation of pefloxacin mesylate for the treatment of various infections caused by pefloxacin sensitive bacteria, and to establish a method for its determination by ultraviolet spectrophotometer.At the same time, the physical and chemical properties, stability, bacteriostatic effect in vitro and safety of compound pefloxacin mesylate oral liquid were studied in order to determine whether it could become a broad spectrum, new type and high efficiency.Safe and reliable antimicrobial and antipyretic drugs, thus providing an effective theoretical basis for the development and application of compound pefloxacin mesylate oral liquid in veterinary clinic.Methods according to the characteristics of oral liquid and the properties of each component, the optimum composition and proportion of solvent, complexing agent and preservative used in oral solution were determined by UV spectrophotometry.A method for content analysis was established. 3 the stability of compound pefloxacin mesylate oral liquid was investigated by high light irradiation test, high temperature and low temperature test and accelerated test. 4 pairs of salmonella, Staphylococcus aureus, streptococcus lactococcus were studied.According to acute toxicity test, the safety of compound pefloxacin mesylate oral liquid was evaluated by MIC test of Escherichia coli.Results: the optimum formula was: pefloxacin mesylate 2, paracetamol 0.2, EDTA-2Na proper, sodium pyrosulfite proper, solvent ethanol and PEG400 appropriate, purified water 100mL.The content of pefloxacin mesylate and paracetamol in compound pefloxacin mesylate oral liquid was determined by UV spectrophotometry at 277 nm and 202 nm, respectively. The precision, recovery and repeatability of the method were high.The results of stability test showed that the compound Pefloxacin Mesylate oral liquid was sensitive to light and not sensitive to temperature change, so it needed to be preserved without light.The antimicrobial activity of this preparation against salmonella, Staphylococcus aureus, streptococcus acidis and Escherichia coli was significantly higher than that of pefloxacin mesylate.The LD50 of chicks was 1453.3 mg / kg, which indicated that the preparation was safe, low toxicity and could be widely used in clinic.Conclusion: the compound pefloxacin mesylate oral liquid can meet the quality requirements, and the preparation process is simple, which can be used in veterinary clinic.
【学位授予单位】：西北农林科技大学
【学位级别】：硕士
【学位授予年份】：2015
【分类号】：S859.79

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