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采用热熔乳化超声-低温固化法制备长春西汀固体脂质纳米粒,并考察大鼠静注给药后体内的药动学特征。长春西汀固体脂质纳米粒平均粒径为(201.6±25.5)nm,多分散系数为0.257±0.047,ζ电位为(-34.3±3.8)mV,包封率为(89.1±3.2)%,载药量为(3.7±0.4)mg/ml。长春西汀注射液和长春西汀固体脂质纳米粒在大鼠体内的t1/2为0.94和2.35 h,AUC0→t为3.50和10.76ug·ml-1·h,体内清除率为5.87和1.95 L/h。表明长春西汀固体脂质纳米粒显著延长了药物在血浆中的滞留时间,提高药物在大鼠体内的生物利用度。
The vinpocetine solid lipid nanoparticles were prepared by hot-melt emulsification ultrasound-low temperature solidification method and the pharmacokinetics in rats after intravenous injection were investigated. The average particle size of vinpocetine solid lipid nanoparticles was (201.6 ± 25.5) nm, the polydispersity coefficient was 0.257 ± 0.047, the zeta potential was (-34.3 ± 3.8) mV and the entrapment efficiency was (89.1 ± 3.2) The dose was (3.7 ± 0.4) mg / ml. The t1 / 2 of vinpocetine injection and vinpocetine solid lipid nanoparticles in rats were 0.94 and 2.35 h, AUC0 → t was 3.50 and 10.76 ug · ml-1 · h, the in vivo clearance rates were 5.87 and 1.95 L / h. The results showed that vinpocetine solid lipid nanoparticles significantly prolonged drug residence time in plasma and increased the bioavailability of the drug in rats.