發(fā)布時間：2019-02-17 17:49

【摘要】：目的建立唑來膦酸與多柔比星包封率的測定方法,以包封率為指標優(yōu)化唑來膦酸與多柔比星共載脂質體的處方及制備工藝,以期獲得包封率高、穩(wěn)定性好的制劑。方法將唑來膦酸配制成銨溶液作為水化介質,使用改良乙醇注入法制備唑來膦酸脂質體,在此基礎上通過銨梯度法主動包載多柔比星以實現兩種藥物在脂質體中的共載。分別采用G-150葡聚糖凝膠微柱-高效液相色譜法與陽離子交換纖維微柱-紫外可見分光光度法測定唑來膦酸與多柔比星的包封率,通過對脂質體外水相中唑來膦酸的去除及對水化介質中陰離子濃度的考察,優(yōu)化脂質體的處方與制備工藝。結果最優(yōu)處方與工藝下制備的共載脂質體粒徑約為110 nm,Zeta電位為-0.87 m V,其中唑來膦酸的包封率為6.5%,多柔比星的包封率大于90%。脂質體于4℃下避光放置60 d,粒徑和包封率均無顯著性變化,穩(wěn)定性良好。結論唑來膦酸與多柔比星共載脂質體的包封率較高,穩(wěn)定性較好。
[Abstract]:Objective to establish a method for the determination of the entrapment efficiency of zoledronic acid and doxorubicin, and to optimize the formulation and preparation process of liposomes co-loaded with zoledronic acid and doxorubicin with high entrapment efficiency and good stability. Methods Zoledronic acid was prepared into ammonium solution as hydration medium and liposomes were prepared by modified ethanol injection method. Doxorubicin was encapsulated by ammonium gradient method to realize the co-loading of two drugs in liposomes. The encapsulation efficiency of zoledronic acid and doxorubicin was determined by G-150 dextran gel microcolumn and cationic exchange fiber microcolumn UV-visible spectrophotometry, respectively. The formulation and preparation process of liposomes were optimized by the removal of zoledronic acid from the aqueous phase of liposomes and the investigation of anion concentration in hydrated media. Results the particle size of the cocarrier liposomes prepared by the optimal formulation and process was about -0.87mV with a potential of -0.87mV. The entrapment efficiency of zoledronic acid was 6.5, and that of doxorubicin was more than 90m. The particle size and entrapment efficiency of liposomes kept at 4 鈩，

本文編號：2425431