甘草黄酮纳米混悬剂的制备及其体外溶出率

摘要

目的 制备甘草黄酮纳米混悬剂,并测定其体外溶出率.方法 沉淀-高压均质法制备纳米混悬剂.以平均粒径与多分散指数(PDI)为评价指标,黄酮、聚维酮K30 (PVPK30)、聚乙二醇400 (PEG-400)质量浓度为影响因素,星点设计-效应面法优化制备工艺.冷冻干燥法制备冻干粉后,筛选最优冻干保护剂种类和比例.再比较冻干粉和口物理混合物的体外溶出率.结果 最佳条件为黄酮质量浓度10.00 mg/mL,PVPK30、PEG-400质量浓度2.30mg/mL,平均粒径(172.3±1.2) nm,PDI 0.175±0.004.最佳冻干保护剂为5％甘露醇-乳糖(3:2),复溶后平均粒径为(239.7±2.1) nm,PDI为0.193±0.032.冻干粉在60 min内的体外溶出率达87.7％,明显高于物理混合物(低于30％).结论 纳米混悬剂可有效改善甘草黄酮的体外溶出率.%AIM To prepare nanosuspensions of flavonoids from Glycyrrhizae Radix et Rhizoma and to determine the in vitro dissolution rate.METHODS Precipitation-high pressure homogenization method was adopted in the preparation of nanosuspensions.With mean particle size and polydispersity index (PDI) as evaluation indices,concentrations of flavonoids,povidone K30 (PVP K30) and polyethylene glycol 400 (PEG 400) as influencing factors,central composite design-response surface method was applied to optimizing the preparation.For the freedried powder prepared by freeze-drying method,the optimal kind and ratio of lyoprotectant were screened.Then the in vitro dissolution rates of freeze-dried powder and physical mixture were compared.RESULTS The optimal conditions were determined to be 10.00 mg/mL for flavonoids' concentration,and 2.30 mg/mL for both PVP K30 and PEG 400 concentrations,the mean particle size and PDI were (172.3 ± 1.2) nm and 0.175 ± 0.004,respectively.The optimal lyoprotectant was 5％ mannitol-lactose (3 ∶ 2),the mean particle size and PDI after redissolution were (239.7 ±2.1) nm and 0.193 ±0.032,respectively.The in vitro dissolution rate of lyoprotectant reached 87.7％ within 60 min,which was much higher than that of physical mixture (less than 30％).CONCLUSION Nanosuspension can effectively improve the in vitro dissolution rate of flavonoids from Glycyrrhizae Radix et Rhizoma.