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采用溶剂注入-高压均质法制备羟喜树碱脂质体。结果显示,本品平均粒径为(182.5±5.6)nm,ζ电位为-(33.10±0.56)mV,包封率大于90%。以市售注射液为参比制剂,采用单剂量双周期交叉试验考察静脉给药后羟喜树碱脂质体在Beagle犬体内的药动学行为。结果表明,羟喜树碱经脂质体包裹后可维持较高的血药浓度,延长了药物在体内的消除时间。
Hydroxycamptothecin liposomes were prepared by solvent injection - high pressure homogenization. The results showed that the average particle size of this product was (182.5 ± 5.6) nm, the zeta potential was - (33.10 ± 0.56) mV, and the encapsulation efficiency was over 90%. Commercially available injections as reference preparation, a single dose of two-cycle cross-over study of intravenous administration of hydroxycamptothecin liposomes in Beagle dogs pharmacokinetic behavior. The results showed that hydroxycamptothecin could maintain high plasma concentration after liposomes encapsulation, prolonging the elimination time of the drug in the body.