摘要
目的:对盐酸拓扑替康脂质体进行质量评价,测定盐酸拓扑替康脂质体的包封率。方法:采用超滤法分离脂质体与游离药物;采用HPLC测定药物含量,计算包封率。结果:超滤法能很好地将脂质体与游离药物分离,游离药物的平均回收率在96.9%~102.3%之间,超滤加样回收率在96.7%~101.6%之间,脂质体不能透过截留相对分子质量为50000的超滤膜。在所选色谱条件下,盐酸拓扑替康得到良好分离,辅料不干扰测定,盐酸拓扑替康在1.0~40.0mg·L^-1内线性关系良好(r=0.9998),日内和日间RSD均〈3.0%(n=5),加样回收率在98.5%~100.3%之间,RSD为1.4%。用此方法测定3份盐酸拓朴替康脂质体的包封率为92.41%~95.14%,RSD在1.26%~2.03%。结论:该方法可用于盐酸拓扑替康脂质体包封率的测定。
Objective:To determine the entrapment efficiency of topotecan hydrochloride liposomes. Methods:An ultrafihration was employed to separate the free drug from the liposomes. The content of topotecan hydrochloride was quantified by HPLC consisted of a Kromasil C,s column, a mobile phase of water-acetonitrile-trifluoroacetic acid (85 : 20:0.1 ) with a flow rate of 0.8 mL· min^-1 and UV detection wavelength at 228 nm. Results: The free topotecan hydrochloride was well separated from the liposomes using uhrafihration membrane that blocks the penetration of a compound with molecular weight of 50 000 or above. The recovery rate of topotecan hydrochloride by uhrafihration and free topotecan was in a range of 96.7% - 101.6% and 96.9% - 102.3% , respectively. A calibrated linear curve of topotecan concentration was within 1.0 -40.0mg·L^-1( r = 0. 999 8 ) , and RSD within day and between days was all less than 3.0% ( n = 5) , the recovery rate of topotecan with blank liposomes was in a range of 98.5% - 100.3% with RSD of 1.4% or below. The entrapment efficiency of three batches of topotecan hydrochloride liposomes was in a range of 92.41% - 95.14% ,with RSD of 1.26% -2.03% by uhrafiltration-HPLC. Conclusion : The ultrafiltration-HPLC method may be used for the determination of entrapment efficiency of topotecan hydrochloride liposomes.
出处
《中国新药杂志》
CAS
CSCD
北大核心
2007年第1期58-61,共4页
Chinese Journal of New Drugs
基金
国家自然科学基金(39570843)
关键词
超滤法
高效液相色谱法
盐酸拓扑替康
脂质体
包封率
ultrafihration
high performance liquid chromatography ( HPLC )
topotecan hydro- chloride
liposomes
entrapment efficiency