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目的:建立咪喹莫特固体脂质纳米粒包封率的测定方法。方法:采用热乳匀法制备咪喹莫特固体脂质纳米粒。用葡聚糖凝胶柱色谱法分离含药固体脂质纳米粒与游离药物,以蒸馏水和1.0×10-3mol·L-1盐酸溶液为洗脱液,用HPLC法测定游离药物量。结果:凝胶柱色谱法能够将包封药物和游离药物分开。游离咪喹莫特在0.335-2.69μg·ml-1浓度范围内,线性关系良好(r=0.999 9)。游离药物柱回收率为98.6%,柱的加样回收率为97.7%。样品的平均包封率为(51.43±0.88)%。结论:该方法操作简便,结果准确,可用于咪喹莫特固体脂质纳米粒包封率测定。
Objective: To establish a method for determination of entrapment efficiency of imiquimod solid lipid nanoparticles. Methods: Imiquimod solid lipid nanoparticles were prepared by hot homogenization. The drug-loaded solid lipid nanoparticles and free drug were separated by dextran gel column chromatography. The amount of free drug was determined by HPLC with distilled water and 1.0 × 10-3mol·L-1 hydrochloric acid as eluent. Results: Gel column chromatography separates the encapsulated drug from the free drug. The free imiquimod had good linearity (r = 0.999 9) at a concentration range of 0.335-2.69μg · ml-1. The free drug column recovery was 98.6% and the column recovery was 97.7%. The average entrapment efficiency of the sample was (51.43 ± 0.88)%. Conclusion: The method is simple, accurate and can be used to determine the encapsulation efficiency of imiquimod solid lipid nanoparticles.