依诺沙星滴眼液辅料及药包材相容性研究

Study on the Compatibility of Excipients and Medicament Packing Material in Enoxacin Eye Drops

关键词:  依诺沙星  氟喹诺酮类  有关物质  含量测定  聚山梨酯80  相容性

Key words:  enoxacin  fluoroquinolone  the related substances  assay  polysorbate 80  compatibility

摘要:

目的 通过分析依诺沙星滴眼液的有关物质与含量，进行辅料与药包材相容性研究。方法 采用HPLC测定50批依诺沙星滴眼液的有关物质及含量。采用Thermo Accucore XL C₁₈色谱柱（4.6 mm×250 mm，4 μm），以0.025 mmol·L^-1磷酸溶液（以三乙胺调节pH值至3.0）-乙腈-甲醇（86∶9∶5）为流动相A，以0.025 mmol·L^-1磷酸溶液（以三乙胺调节pH值至3.0）-乙腈-甲醇（350∶325∶325）为流动相B进行梯度洗脱，测定依诺沙星滴眼液中的有关物质。根据影响因素试验和加速试验，进行辅料及药包材的相容性研究。结果 处方中的聚山梨酯80可导致特定杂质及杂质总量的增加；光照可导致杂质增大及含量降低，采用遮光包装可降低光降解反应的发生。结论 依诺沙星滴眼液的生产过程中应避免使用可导致杂质增加的辅料，并应采用遮光材料进行包装。

Abstract:

OBJECTIVE To study the compatibility between excipients and medicament packing materials by analyzing the related substances and content of enoxacin eye drops. METHODS The related substances and content of 50 batches of enoxacin eye drops were determined by HPLC. Thermo Accucore XL C₁₈ column(4.6 mm×250 mm, 4 μm) was used. The mobile A was 0.025 mmol·L^-1 phosphoric acid solution(adjust with triethylamine to a pH of 3.0)-acetonitrile-methanol(86:9:5), the mobile B was 0.025 mmol·L^-1 phosphoric acid solution(adjust with triethylamine to a pH of 3.0)-acetonitrile-methanol(350:325:325), with gradient elution to determine the related substances in enoxacin eye drops. Accomplished the study on the compatiblity of excipients and medicament packing material according to the influence factor test and accelerated test. RESULTS Polysorbate 80 in the formula could lead to the increase of specific impurities and the total amount of impurities. Light could lead to the increase of the total amount impurities and the decrease of enoxacin. The photodegradation reaction could be reduced by using shading packaging. CONCLUSION Excipients that can increase impurities should be avoided in the production of enoxacin eye drops, and shading materials should be used for packaging.