满山红总黄酮固体分散体的制备工艺考察

Investigation of Preparation Technology of Rhododendri Daurici Folium Total Flavonoids Solid Dispersions

摘要:

目的: 优选满山红总黄酮固体分散体的制备工艺。方法: 分别以聚乙二醇6000(PEG6000),聚乙烯吡咯烷酮K30(PVPK30),泊洛沙姆188(Pluronic F68)为载体,采用适合载体的熔融-溶剂法和溶剂法制备满山红总黄酮-载体不同比例(1:1,1:2,1:4,1:6)的固体分散体。以满山红总黄酮为检测指标,通过UV测定体外溶出度,计算各固体分散体的T_d值。结果: 最佳制备工艺为以4倍量PVPK30为载体,加20倍量无水乙醇溶解,于50℃旋蒸除去无水乙醇,满山红总黄酮的体外溶出率达100%。PEG6000为载体时,不同比例的固体分散体T_d分别为6.329,5.225,0.096,4.755 min;Pluronic F68为载体时,各固体分散体T_d分别为4.045,3.561,0.018,0.026 min;PVPK30为载体时,各固体分散体T_d分别为5.000,5.000,0.005,0.056 min。结论: 溶剂法可用于制备满山红总黄酮固体分散体,具有很好的增溶效果,但不适合工业生产。

Abstract:

Objective: To optimize preparation technology of Rhododendri Daurici Folium total flavonoids solid dispersions. Method: With polyethylene glycol 6000(PEG6000),polyvinyl pyrrolidone(PVPK30 K30) and poloxamer 188 (Pluronic F68) as carrier respectively,suitable carrier melting-solvent method and solvent method were used to prepare solid dispersions with different proportion(1:1,1:2,1:4,1:6) of total flavonoids from Rhododendri Daurici Folium-carrier.With total flavonoids from Rhododendri Daurici Folium as detection index,in vitro dissolution of the dispersions was analyzed by UV,and T_d of each solid dispersions was calculated. Result: Optimum preparation process was as following:with 4 times the volume of PVPK30 as carrier,dissolved in 20 times the amount of ethanol,rotary evaporation to remove ethanol at 50℃,in vitro dissolution of total flavonoids from Rhododendri Daurici Folium in PVPK30 solid dispersions were up to 100%.With PEG6000 as carrier,T_d of solid dispersions with different proportion(1:1,1:2,1:4,1:6) of total flavonoids from Rhododendri Daurici Folium-carrier were 6.329,5.225,0.096,4.755 min,respectively;Pluronic F68 as carrier,T_d were 4.045,3.561,0.018,0.026 min,respectively;PVPK30 as carrier,T_d were 5.000,5.000,0.005,0.056 min,respectively. Conclusion: Solvent method could successfully prepare Rhododendri Daurici Folium total flavonoids solid dispersions with good solubilization effect,but this method was not suitable for industrial production.