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目的:对六甲蜜胺脂质体进行质量评价,建立六甲蜜胺脂质体包封率的测定方法。方法:采用(凝胶)微柱离心法分离游离药物与脂质体;利用流动相:甲醇-乙腈-水(50∶35∶15);柱温:30℃;流速:0.8 mL·min-1;紫外检测波长:228 nm的HPLC条件测定六甲蜜胺的含量,最终计算得包封率。结果:微柱离心法能够将100%的空白脂质体和小于3.5%的游离药物洗脱下来,游离药物与脂质体可被分离,游离药物基本上被截留于微柱中。在本法选择的色谱条件下,六甲蜜胺得到良好的分离,辅料不干扰测定,六甲蜜胺在2.0～40.0 mg·L-1内线性关系良好(r=0.9996),日内和日间RSD均<2.0%(n=5),加样回收率在97.9%～98.5%之间(RSD<2.0%,n=5)。用该方法测得3份六甲蜜胺脂质体的包封率在82.49%～86.56%之间(RSD均<2.0%,n=3)。结论:本方法可用于测定六甲蜜胺脂质体包封率。
OBJECTIVE: To evaluate the quality of hexamethonine liposomes and establish the method for determining the encapsulation efficiency of hexamethonine liposomes. Methods: Free drug and liposome were separated by (gel) micropillar centrifugation. The mobile phase was methanol-acetonitrile-water (50:35:15), the column temperature was 30 ℃, the flow rate was 0.8 mL · min -1 ; UV detection wavelength: 228 nm HPLC conditions determination of altretamine content, the final calculation of the entrapment efficiency. Results: Micropipette centrifugation was able to elute 100% of the blank liposomes and less than 3.5% of the free drug. The free drug and the liposomes could be separated and the free drug was essentially trapped in the microcolumn. Under the chromatographic conditions selected by this method, altretamine was well separated and the excipients did not interfere with the determination. The calibration curve of altretamine was good (r = 0.9996) in the range of 2.0-40.0 mg · L-1, both intra-day and inter-day RSD <2.0% (n = 5). The recoveries were between 97.9% and 98.5% (RSD <2.0%, n = 5). The entrapment efficiency of 3 parts hexamethonine liposomes measured by this method ranged from 82.49% to 86.56% (RSD <2.0%, n = 3). Conclusion: This method can be used to determine the entrapment efficiency of altretamine liposomes.