紫杉醇聚乙二醇单甲醚-乳酸-羟基醋酸嵌段共聚物大鼠体内药动学考察  

Study on pharmacokinetics of paclitaxel polyethylene glycol monomethyl ether-lactic acid-hydroxy acetate copolymer

作　　者：廖明[1] 方琴[2] 谭蓉[2] 李明[2] 

机构地区：[1]贵阳市妇幼保健院,贵州贵阳550004 [2]贵阳医学院附属医院,贵州贵阳550002

出　　处：《中国医院药学杂志》2014年第7期532-534,共3页Chinese Journal of Hospital Pharmacy

摘　　要：目的:对紫杉醇聚乙二醇单甲醚-乳酸-羟基醋酸嵌段共聚物进行大鼠体内药动学考察。方法:SD大鼠以6mg·kg-1剂量于尾静脉注射自制紫杉醇聚乙二醇单甲醚-乳酸-羟基醋酸嵌段共聚物与紫杉醇注射液,以高效液相色谱仪测定给药后不同时间血浆中紫杉醇的药物浓度。结果:紫杉醇聚乙二醇单甲醚-乳酸-羟基醋酸嵌段共聚物与紫杉醇注射液经大鼠尾静脉注射后均符合二室模型,t1/2α分别为(12.45±3.06)min和(2.37±1.71)min;t1/2β分别为(43.27±14.55)min和(38.50±2.26)min;AUC分别为(2 381.22±314.31)mg·L-1·min和(1 156.33±300.04)mg·L-1·min。结论:紫杉醇与聚乙二醇单甲醚-乳酸-羟基醋酸形成嵌段共聚物后,紫杉醇体内消除减慢,驻留时间延长,维持较高药物浓度时间延长。OBJECTIVE To study pharmacokinetics of paclitaxel polyethylene glycol monomethyl ether-lactic acid-hydroxy acetate copolymer. METHODS Paclitaxel nanoparticle and paclitaxel injection were administered through tail vein at the dose of 6 mg·kg^-1. HPLC was used for quantifying paclitaxel in rat plasma and tissue at different time after administration. RESULTS The concentration-time data of paclitaxel nanoparticle and paclitaxel injection were all fitted to two compartment- model, t1/2α were （12. 45 ± 3.06）min and （2. 37 ± 1.71）min,t1/2β were （43. 27 ± 14. 55）min and （38. 50 ± 2. 26）min,AUC were （2381.22±314.31）mg·L^-1·min and（1 156. 33 ± 300. 04）mg·L^-1·min. CONCLUSION Paclitaxelpolyethyleneglycolmono- methyl ether-lactic acid-hydroxy acetate copolymer eliminated in vivo slowly, and has a longer time on a high drug concentra- tion.

关 键 词：紫杉醇 聚乙二醇单甲醚-乳酸-羟基醋酸 药动学 

分 类 号：R969.1[医药卫生—药理学]