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目的制备辣椒碱多囊脂质体,并考察其包封率和在大鼠体内的药动学。方法采用复乳法制备辣椒碱多囊脂质体、单因素筛选处方,并考察大鼠sc辣椒碱多囊脂质体后的体内药动学。结果制备的辣椒碱多囊脂质体的外观圆整,大小均匀,包封率为71.9%±3.8%,平均粒径为8.1μm。大鼠sc辣椒碱多囊脂质体后,与辣椒碱溶液相比,Cmax分别为405.72±53.87、804.06±108.17 ng.mL-1;AUC0-t为16.7836±2.8541、3.7622±0.6651μg.h.mL-1;消除时间分别为32.31±2.64、3.23±0.34 h,72 h时血浆中仍可检测到药物。结论采用复乳法可成功将脂溶性药物辣椒碱载入多囊脂质体中,大鼠体内的药动学研究显示有明显的缓释特征。
OBJECTIVE To prepare capsaicin multivesicular liposomes and study their entrapment efficiency and pharmacokinetics in rats. Methods The capsaicin multivesicular liposomes were prepared by double emulsion method. The pharmacokinetics of capsaicin multivesicular liposomes were determined by single factor and in vivo. Results The capsaicin multivesicular liposomes were round and uniform in size with the encapsulation efficiency of 71.9% ± 3.8% and the average particle size of 8.1 μm. Compared with capsaicin solution, rat C capsaicin multilocase liposomes had Cmax of 405.72 ± 53.87,804.06 ± 108.17 ng.mL-1 and AUC0-t of 16.7836 ± 2.8541 and 3.7622 ± 0.6651μg.h respectively. mL-1; the elimination time was 32.31 ± 2.64,3.23 ± 0.34 h, and the drug was still detected in plasma at 72 h. Conclusions Double liposomes can be successfully loaded into capsular liposomes by double emulsion method. Pharmacokinetic studies in rats show that they have obvious sustained release characteristics.