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目的:研究尿酸酶(uricase,URE)和过氧化氢酶(catalase,CAE)联合制备成脂质体后尿酸酶在大鼠体内的药动学。方法:大鼠随机分成2组,静脉分别注射尿酸酶复合脂质体(uricase and catalase liposome,UCLP)和URE后,测定不同时间点大鼠血液中URE的活性,计算URE的药动学参数及生物利用度。结果:UCLP和URE的主要药动学参数AUC0-t分别为(118.06±19.26)和(48.16±6.31)mU·h·ml-1,Cmax为(88.70±8.52)和(75.65±9.04)mU·ml-1,tmax为0.50 h和0.17 h;UCLP的绝对生物利用度为245.14%;UCLP和URE的达峰时间(tmax)、曲线下面积(AUC0-t)等参数具有显著性差异(P<0.05)。结论:UCLP与游离URE相比,UCLP有缓释效果;生物利用度良好;两者不具有生物等效性。
OBJECTIVE: To study the pharmacokinetics of uricase (URE) in rats by combining uricase (URE) and catalase (CAE). Methods: The rats were randomly divided into 2 groups. The urease and catalase liposomes (UCLP) and URE were injected intravenously to determine the activity of URE in rat blood at different time points. The pharmacokinetic parameters of URE and bioavailability. RESULTS: The major pharmacokinetic parameters AUC0-t for UCLP and URE were (118.06 ± 19.26) and (48.16 ± 6.31) mU · h · ml-1, respectively, with Cmax values of (88.70 ± 8.52) and (75.65 ± 9.04) The absolute bioavailability of UCLP was 245.14%. The peak time (tmax) and area under the curve (AUC0-t) of UCLP and URE were significantly different (P < 0.05). CONCLUSIONS: UCLP has a sustained release profile compared with free URE; its bioavailability is good; and both are not bioequivalent.