摘要
目的比较紫杉醇脂质体与紫杉醇注射液在大鼠体内的血药浓度及相关药动学参数。方法大鼠经尾静脉注射紫杉醇注射液或紫杉醇脂质体注射液12 mg/kg后,采用HPLC法测定大鼠体内的血药浓度,得出药-时曲线图及采用3p87药动学软件得到相关药动学参数;同时采用SPSS17.0统计软件进行t检验。结果紫杉醇注射液及紫杉醇脂质体在大鼠血浆样品中的浓度分别为(0.21±0.11)、(48.12±9.42)C·mg-1·L-1,差异具有统计学意义(t=12.457,P<0.001);紫杉醇脂质体药-时曲线下面积(AUC)较紫杉醇注射液大(17.578±2.428 vs 10.422±2.784,t=4.745,P<0.001),清除率(Cl)较紫杉醇注射液慢〔(7.4±1.1)vs(1.3±2.5)×10-4L,t=5.471,P<0.001〕,表观分布容积(Vc)较紫杉醇注射液小〔(1.523±1.882)×10-3L vs(5.314±1.211)×10-3L,t=4.059,P<0.002〕。结论紫杉醇脂质体与紫杉醇注射液在大鼠体内药动学显著不同,不仅能使药物在体内的浓度维持较长时间,而且使药物更好的聚集于肿瘤靶组织,从而增加治疗疗效,减少毒副作用。
Objective To compare the parameters of serum concentration and pharmacokinetic of paclitaxel liposome and injection in rats.Methods The blood paclitaxel liposome concentration of rats were determined by HPLC method after intravenous injections of pacli -tarel injection or paclitaxel liposome injection 12 mg/kg, the concentration-time curve was obtained and 3p87 pharmacokinetic software was used to get the pharmacokinetic parameters .Results The concentration of paclitarel injection and paclitaxel liposome in rat plasma samples were (0.21±0.11) and (48.12±9.42) C· mg-1· L-1 respectively (t=12.457,P<0.001),the area under curve of the drug concentration-time (AUC) of paclitaxel liposome was bigger than that of paclitarel injection (17.578±2.428 vs 10.422±2.784,t=4.745,P<0.001),the clearance rate(Cl) was slower than that of paclitarel injection〔(7.4±1.1) vs (1.3±2.5) ×10-4 L,t=5.471,P<0.001〕 and the apparent volume of distribution (Vc) was smaller than that of paclitarel injection〔(1.523±1.882)×10-3 vs (5.314±1.211)×10-3 L,t=4.059,P<0. 002〕.Conclusions The pharmacokinetic of paclitaxel liposome is significantly different from that of paclitarel injection , which could not on-ly remain the drug for a longer time in vivo , but also make better aggregation drugs in tumor tissue , so as to increase the treatment efficacy and reduce the toxic side effect .
出处
《中国老年学杂志》
CAS
CSCD
北大核心
2014年第15期4234-4236,共3页
Chinese Journal of Gerontology
基金
国家自然科学基金(No.81172097)
关键词
紫杉醇
脂质体
注射液
药动学
Paclitaxel
Liposome
Injection
Pharmacokinetics
