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目的:建立测定以脂肪乳为载体地塞米松滴眼液中药物在各相中的分布和包封率方法,并分析其作为载药性能评价指标的可行性。方法:根据脂质乳中相密度差异,在8℃、30 000 r·min~(-1)离心力下分离在油、水及油水界面相中的药物;依据凝胶分子筛原理对脂质乳滴表面的游离药物和包封于乳滴中的药物进行柱分离;色谱条件:采用Sun Fire C_(18)色谱柱(250 mm×4.6 mm,5μm),以乙腈-水(28∶72)为流动相,流速1.0 m L·min~(-1),检测波长240 nm,柱温30℃,进样量20μL。结果:水相、油相、油水界面磷脂层中地塞米松的占比为42.43%、31.12%、24.45%,体系中地塞米松的包封率为50.11%。结论:相分布和包封率指标合用能准确评价脂肪乳的载药性能,所建立的方法可作为以脂肪乳为载体滴眼液的质量控制的手段之一。
OBJECTIVE: To establish a method for determining the distribution and entrapment efficiency of drug in dexamethasone eye drops using lipid emulsion as carrier and to evaluate its feasibility as an evaluation index for drug-loading performance. Methods: According to the difference of phase density in lipid emulsion, the drug in oil, water and oil-water interface was separated under centrifugal force of 30 000 r · min -1 at 8 ℃. According to the principle of gel molecular sieve, The free surface drug and the drug encapsulated in the emulsion were separated by column chromatography. The chromatographic conditions were as follows: using a Sun Fire C 18 column (250 mm × 4.6 mm, 5 μm) with acetonitrile-water (28:72) The flow rate was 1.0 m L · min -1, the detection wavelength was 240 nm, the column temperature was 30 ℃ and the injection volume was 20 μL. Results: The proportion of dexamethasone in the lipid layer, oil phase and oil-water interface was 42.43%, 31.12% and 24.45%, respectively. The encapsulation efficiency of dexamethasone in the system was 50.11%. Conclusion: The combination of phase distribution and encapsulation efficiency can accurately evaluate the drug-loading performance of lipid emulsion. The established method can be used as one of the means to control the quality of lipid-based emulsion.