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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 the pharmacokinetics of paclitaxel polyethylene glycol monomethyl ether-lactic acid-hydroxyacetic acid block copolymer in rats. Methods: Sprague-Dawley rats were injected with tail vein injection of 6mg · kg-1 paclitaxel polyethylene glycol monomethyl ether-lactic acid-hydroxyacetic acid block copolymer and paclitaxel injection, and determined by high performance liquid chromatography Time plasma paclitaxel drug concentration. Results: Paclitaxel-polyethylene glycol monomethyl ether-lactic acid-hydroxyacetic acid block copolymer and paclitaxel injection were all consistent with the two compartment model after injection into the tail vein of rats. The t1 / 2α values were (12.45 ± 3.06) min and (2.37 ± 1.71) min and t1 / 2β were (43.27 ± 14.55) min and (38.50 ± 2.26) min, respectively; AUC were (2 381.22 ± 314.31) mg · L-1 · min and (1 156.33 ± 300.04) mg · L -1 · min. Conclusion: Paclitaxel and polyethylene glycol monomethyl ether - lactic acid - hydroxy acetic acid form a block copolymer, paclitaxel elimination in vivo slowed down, dwell time extended to maintain a higher drug concentration for a prolonged period of time.