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目的:考察紫杉醇原位凝胶制剂PECT/PTX小鼠瘤体内植入后的药动学特点,评价该制剂是否具有控释、缓释作用。方法:对EAC荷瘤小鼠分别进行PECT/PTX瘤体内给药(A组,40 mg·kg-1),PTX瘤体内给药(B组,40 mg·kg-1)和PTX腹腔给药(C组,40 mg·kg-1),给药后于设定的时间点采血,应用HPLC法测定血浆中PTX的含量,DAS 2.1.1药动学分析软件计算主要药动学参数。结果:血浆中A、B、C 3组的Cmax分别为(2.23±0.16),(25.25±0.83),(258.38±10.34)mg·L-1;t1/2分别为(473.81±195.13),(10.89±0.87),(17.87±6.29)h;AUC0-t分别为(623.57±23.48),(340.72±2.73),(843.35±25.93)mg·L-1·h;Vd分别为(17.01±2.24),(1.76±0.13),(1.07±0.25)L·kg-1;CL分别为(0.024±0.010),(0.105±0.001),(0.040±0.004)L·h-1·kg-1。与B组相比,A、C 2组主要药动学参数均具有显著的统计学差异(P<0.01)。结论:PECT/PTX原位凝胶制剂瘤体内给药具有缓慢释放PTX的作用。
OBJECTIVE: To investigate the pharmacokinetic characteristics of paclitaxel in situ gel preparation PECT / PTX in vivo and evaluate whether the preparation has controlled release and sustained release. Methods: EAC tumor-bearing mice were treated with PECT / PTX in vivo (group A, 40 mg · kg-1), PTX tumor in vivo (group B, 40 mg · kg- (Group C, 40 mg · kg-1). Blood samples were collected at the set time points after administration. The content of PTX in plasma was determined by HPLC. The main pharmacokinetic parameters were calculated by DAS 2.1.1 pharmacokinetic analysis software. Results: The plasma Cmax were (2.23 ± 0.16), (25.25 ± 0.83) and (258.38 ± 10.34) mg · L-1 in group A, group B and group C respectively, and (473.81 ± 195.13) and 10.89 ± 0.87 and 17.87 ± 6.29 h respectively; AUC0-t were (623.57 ± 23.48), (340.72 ± 2.73) and (843.35 ± 25.93) mg · L-1 · h, respectively; Vd was (17.01 ± 2.24) , (1.76 ± 0.13) and (1.07 ± 0.25) L · kg-1, respectively; CL were (0.024 ± 0.010), (0.105 ± 0.001) and (0.040 ± 0.004) L · h-1 · kg- Compared with group B, the main pharmacokinetic parameters of group A and C 2 had significant statistical difference (P <0.01). Conclusion: The intratumoral administration of PECT / PTX in situ gel preparation has the effect of slow release of PTX.