人参皂苷Rg3固体分散体的制备与体外特性研究

目的 采用固体分散技术,比较3种不同载体对人参皂苷Rg3的溶解度和体外溶出度的作用.方法 分别以泊洛沙姆188(F68)、聚维酮k29/32(PVP)和聚乙二醇6000(PEG)为载体,采用熔融法或溶剂法,制备人参皂苷Rg3固体分散体,测定溶解度,进行溶出度试验,并采用差热量热分析(DSC)法鉴别药物在固体分散体中的存在状态.结果 各种固体分散体均能显著增加人参皂苷Rg3的溶解度,加快其体外溶出.人参皂苷Rg3可充分分散在载体中并形成低共熔物.结论 F68作为载体制成固体分散体,对增加人参皂苷Rg3的溶解度和体外溶出度的效果优于PEG和PVP.

Preparation and dissolution characteristics of solid dispersion of ginsenoside Rg3

Objective To prepare the solid dispersion of ginsenoside Rg₃ with different carriers and measure their solubility and dissolution characterisitics. Methods The solid dispersion of ginsenoside Rg₃ was prepared by the melted and dissolved methods with Poloxamer 188(F68), PVP k29/32, and PEG 6000 as carriers, respectively. The equilibrium solubility and dissolution characteristics of the solid dispersion in vitro were measured by HPLC. The existing state of ginsenoside Rg₃ in the solid dispersion was identified by the differential scanning calorimetery. Results The ginsenoside Rg₃ was completely dispersed in carrier and formed a mixture with carriers. The solubility and dissolution rates of all solid dispersion were increased obviously. Conclusion The solid dispersion of ginsenoside Rg₃ with Poloxamer 188 as carriers is better on improving dissolution and solubility than those with PVP and PEG 6000 as carriers.