氢化与非氢化卵磷脂对阿霉素脂质体药动学参数的影响

The effects of hydrogenated and non-hydrogenated egg phosphatidylcholine on the pharmacokinetic parameters of doxorubicin liposomes

目的 研究卵磷脂 (EPC)和氢化卵磷脂 (HEPC)对阿霉素长循环脂质体 (Dox SSL)药动学参数的影响。方法 10只Wistar大鼠平均分成二组 ,分别尾静脉注射Dox·EPC SSL和Dox HEPC SSL脂质体 ,用高效液相色谱法测定血中Dox浓度。用 3P87程序拟合计算药动学参数。结果 两种制剂均符合二室模型 ,权重为 1/C2 ,方差分析结果表明 ,二者的α与Vc无显著性差异 (P>0 .0 5 ) ,而 β ,CLs及AUC有显著性差异 (P <0 .0 1) ,Dox HEPC SSL的β ,CLs较Dox EPC SSL小 ,而AUC较Dox EPC SSL大。 结论 作为药物载体 ,HEPC SSL较EPC

OBJECTIVE: To study the effects of hydrogenated and non-hydrogenated egg phosphatidylcholine on the pharmacokinetic parameters of doxorubicin sterically stabilized liposomes (Dox-SSL). METHODS: 10 Wistar rats were divided into two groups randomly and were injected Dox-EPC-SSL and Dox-HEPC-SSL through tail vein, respectively. The blood samples were collected and the concentrations of doxorubicin were determined by HPLC. RESULTS: The two preparations were fitted to two-compartment model. There was no significant difference of α and Vc (P > 0.05), but β, CLs and AUC had significant difference (P < 0.01. β and CLs of Dox-HEPC-SSL were less than those of Dox-EPC-SSL, and AUC of Dox-HEPC-SSL was larger than that of Dox-EPC-SSL. CONCLUSION: As a drug carrier, HEPC-SSL seems to be better than EPC-SSL.