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目的:考察注射用纳米羟基喜树碱静脉推注给药后,家兔血浆药物浓度随时间变化趋势和药代动力学参数,并与注射用羟基喜树碱进行比较,评价纳米针药动学特性。方法:建立HPLC检测家兔血浆中羟基喜树碱含量的方法,采用3p97药代动力学计算软件模拟房室模型并计算药代动力学参数。结果:注射用羟基喜树碱家兔耳静脉单次推注给药符合1 C2 权重的二室模型,而注射用纳米羟基喜树碱符合1 C2 权重的三室模型。注射用羟基喜树碱的血浆Cmax是同剂量纳米针的3倍,AUC也是纳米针的2～3倍。同剂量下HCPT纳米针组Vc 均大于粉针组。纳米针消除半衰期(T1 2 β)较冻干粉针延长。结论:注射用纳米羟基喜树碱在家兔体内的药动学特性与普通粉针比较发生显著变化。
OBJECTIVE: To investigate the trend and pharmacokinetic parameters of plasma drug concentration in rabbits after intravenous injection of nano-hydroxycamptothecin for injection and compare with injection of hydroxycamptothecin to evaluate the pharmacokinetics of nano-needle characteristic. Methods: A HPLC method for the determination of hydroxycamptothecin in rabbit plasma was established. Pharmacokinetic software 3p97 was used to simulate the compartment model and the pharmacokinetic parameters were calculated. RESULTS: A single-bolus injection of hydroxycamptothecin for injection in rabbits gave a two-compartment model that conformed to a 1 C 2 weight while a narcotic three-compartment model conformed to a C 1 C weight for injection with hydroxycamptothecin. The plasma Cmax of hydroxycamptothecin for injection was 3 times that of the same dose nanoneedles and the AUC was also 2 to 3 times of the nanoneedles. The same dose of HCPT nano-needle group Vc were greater than the powder group. The half-life of nano-needle elimination (T1 2 β) is longer than that of lyophilized powder. CONCLUSION: The pharmacokinetics of N-hydroxycamptothecin for injection in rabbits changed significantly compared with that of common powder injection.