过氧化氢酶脂质体的药代动力学和生物等效性初步研究

发布时间：2019-03-06 09:28

【摘要】：目的:研究过氧化氢酶脂质体(catalase liposomes,CALP)在SD大鼠体内的药代动力学和生物等效性。方法:采用逆向蒸发法制备了CALP,并测定其粒径、Zeta电位及包封率。将12只雄性SD大鼠随机分为2组,分别静脉注射CALP和游离过氧化氢酶(catalase,CAT),测定给药后不同时间点大鼠血浆中过氧化氢酶的活性。采用DAS 2.1.1软件计算药物代谢动力学参数,并对CALP和CAT进行生物等效性评价。结果:CALP的包封率为(53.72±1.67)%,粒径和Zeta电位分别为(405.40±21.89)nm和(-15.70±3.22)m V。CALP和CAT的主要药物代谢动力学参数AUC0-t分别为(203.22±11.75)U(ml·h)和(50.92±3.51)U(ml·h),Cmax分别为(70.79±1.33)U/ml和(51.48±2.78)U/ml,Tmax分别为(0.58±0.14)h和(0.17±0.00)h。ln AUC、ln Cmax经方差分析和双单侧检验证明差异具有统计学意义(P0.05)。AUC0-t、AUC0-∞和Cmax的90%可置信区间分别为133.8%~140.1%,132.3%~146.7%,104.7%~107.5%。CALP和CAT的Tmax经非参数法检验差异无统计学意义(P0.05)。CALP的相对生物利用度为(399.1±23.1)%。结论:CALP提高了过氧化氢酶的生物利用度,CALP与CAT不具有生物等效性。
[Abstract]:Aim: to study the pharmacokinetics and bioequivalence of catalase liposomes (catalase liposomes,CALP) in SD rats. Methods: CALP, was prepared by reverse evaporation and its particle size, Zeta potential and entrapment efficiency were determined. Twelve male SD rats were randomly divided into two groups. CALP and free catalase (catalase,CAT) were injected intravenously. The activities of catalase in plasma of rats were measured at different time points after administration. The pharmacokinetic parameters were calculated by DAS 2.1.1 software, and the bioequivalence of CALP and CAT was evaluated. Results: the encapsulation efficiency of CALP was (53.72 卤1.67)%. The main pharmacokinetic parameters of (405.40 卤21.89) nm and (- 15.70 卤3.22) m V.CALP and CAT were (203.22 卤11.75) U (ml 路h and (50.92 卤3.51) U (ml 路h, respectively. The main pharmacokinetic parameters were (405.40 卤21.89) nm and (- 15.70 卤3.22) m V.CALP, respectively. ) U (ml 路h), The Cmax values were (70.79 卤1.33) U/ml and (51.48 卤2.78) U / ml, (0.58 卤0.14) h and (0.17 卤0.00) h.ln AUC, respectively. Ln Cmax was statistically significant by variance analysis and bilateral one-sided test (P0.05). The 90% confidence intervals of AUC0-t,AUC0- 鈭，

本文编号：2435406