前列地尔注射液包封率测定方法的比较研究  

Comparative Study on the Determination Method of Entrapment Efficiency of Alprostadil Injection

作　　者：段玉龙 赵龙山[1] DUAN Yulong;ZHAO Longshan(School of Pharmacy,Shenyang Pharmaceutical University,Shenyang 110016,China;Shijiazhuang Si yao Group Pharmaceutical Research Institute,Shijiazhuang 050000,China;Chemical Sterile Preparation Industry Technology Research Institute,Shijiazhuang 050000,China;Hebei Province High Capacity Injection Engineering Technology Research Center,Shijiazhuang 050000,China)

机构地区：[1]沈阳药科大学药学院,沈阳110016 [2]石家庄四药集团药物研究院,石家庄050000 [3]化学药品无菌制剂产业技术研究院,石家庄050000 [4]河北省大容量注射剂工程技术研究中心,石家庄050000

出　　处：《中国药学杂志》2025年第2期166-171,共6页Chinese Pharmaceutical Journal

摘　　要：目的 建立前列地尔注射液包封率测定方法,比较超滤离心法和微柱离心法测定前列地尔注射液包封率的差异,筛选最优方法。方法 高压均质法制备前列地尔注射液,采用不同截留相对分子质量的超滤管,通过筛选离心转速和时间,建立超滤离心法;以葡聚糖凝胶SephadexG-50制备微柱,采用离心洗脱方式分离包封和游离药物。通过建立大豆油和游离前列地尔的洗脱曲线,考察分离效果,同时考察不同洗脱溶剂之间的差异,筛选最优洗脱溶剂,建立微柱离心法,采用高效液相色谱法及柱后衍生装置测定药物含量,计算包封率。结果 超滤离心法测得三批前列地尔注射液的包封率在98.6%~99.5%,微柱离心法测得包封率在89.5%~91.3%。结论 超滤离心法包封率测定结果偏高,不适用于本品包封率的测定;采用甘油水溶液作为洗脱溶剂的微柱离心法,适用于本品包封率的测定。OBJECTIVE To establish a method for determining the entrapment efficiency of alprostadil injection,compare the differences between ultrafiltration centrifugation and microcolumn centrifugation methods for determining the entrapment efficiency of alprostadil injection,and select the optimal method.METHODS High pressure homogenization method was used to prepare alprostadil injection.Ultrafiltration membrane with different molecular weights were used to establish the ultrafiltration centrifugation method by selecting the centrifugation speed and time.The micro column was prepared with Sephadex G-50,and the encapsulated and free drugs were separated by centrifugal elution.The separation effect was evaluated by establishing the elution curve of soybean oil and free alprostadil.At the same time,the difference between different elution solvents was investigated,the optimal elution solvent was screened,and the microcolumn centrifugation method was established.The drug content was determined by high-performance liquid chromatography and post column derivatization device,and the entrapment efficiency was calculated.RESULTS The entrapment efficiency of three batches of alprostadil injection measured by ultrafiltration centrifugation method ranged from 98.6%to 99.5%,while the entrapment efficiency measured by microcolumn centrifugation method ranged from 89.5%to 91.3%.CONCLUSION The results of the ultrafiltration centrifugation method for determining the entrapment efficiency are too high and not suitable for the determination of the entrapment efficiency of this product.The microcolumn centrifugation method using glycerol aqueous solution as the eluting solvent is suitable for the determination of the entrapment efficiency of this product.

关 键 词：前列地尔注射液 包封率 超滤离心法 微柱离心法 

分 类 号：R917[医药卫生—药物分析学]