苯磺贝他斯汀滴眼液的制备与评价

Preparation and evaluation of bepotastine besilate eye drops

目的:制备苯磺贝他斯汀滴眼液,进行质量评价,并比较不同含量测定分析方法。方法:以氯化钠、磷酸二氢钠一水合物、氢氧化钠和苯扎氯铵为辅料,蒸馏水为溶剂制备苯磺贝他斯汀滴眼液。对滴眼液性状、渗透压摩尔浓度比、pH、可见异物、装量、R-异构体和有关物质进行检查;采用高效液相色谱法使用内标法与外标法进行含量测定对比分析,并进行含量测定。结果:制备的滴眼液为无色澄明液体、渗透压摩尔浓度比均值为0. 99,pH约为6. 8,无可见异物,装量合格,R-异构体杂质在1. 0%以下,有关物质检查符合要求;外标法和内标法的含量测定方法学考察均符合要求,含量测定结果无显著性差异,测得含量分别为:97. 08%和97. 39%。结论:苯磺贝他斯汀滴眼液的处方和制备工艺合理,质量符合要求。用于含量测定的外标法或内标法的方法学考察合格,结果准确可靠,均可应用于苯磺贝他斯汀滴眼液质量控制研究。

Objective:To prepare bepotastine besilate eye drops and evaluate their quality,and compare the content analysis methods.Methods:Bepotastine besilate eye drops were prepared by using sodium chloride,sodium dihydrogen phosphate monohydrate,sodium hydroxide and benzalkonium chloride as auxiliary materials,and water as solvent;Eye drops properties,osmotic molar concentration ratio,pH,visible foreign matter,drug loading capacity,the content of R-isomer and related substances were examined;HPLC was used for content determination and the internal standard method and external standard method were compared.Results:The prepared eye drops were colorless and clear,the average osmolality ratio was 0.99,the pH was about 6.8,no visible foreign matter was observed,the quantity was qualified,the content of R-isomer impurity was below 1.0%,and the related substance inspection met the requirements;the external standard method and internal standard method for the determination of content both met the requirements,without significant difference for the results of content determination,which were 97.08%and 97.39%,respectively.Conclusion:The formulation and preparation process of bepotastine besilate eye drops are reasonable,and the quality meets the requirements.The externalstandard method or internal standard method for content determination is qualified,accurate and reliable,and can be applied to the quality control study of bepotastine besilate eye drops.