静脉给予尿酸酶自组装空心纳米微球的药代动力学和生物等效性初步研究

Pharmacokinetics and Bioequiavailability of Intravenous Uricase Self-Assembly Hollow Nanospheres

摘要:

研究了载尿酸酶聚乙二醇-透明质酸（Hyaluronic acid-graft-polyethylene glycol，HA-g-PEG）/磺丁基-β-环糊精（Sulfobutyl ether-beta-cyclodextrin，SCD）自组装空心纳米微球（HA-g-PEG/SCD self-assembly hollow spheres encapsulated uricase，UHPSD）在大鼠体内的药代动力学和生物等效性。大鼠单剂量静脉注射给予UHPSD和游离尿酸酶（Uricase，UOX），眼底静脉丛取血，测定给药后不同时间点大鼠血浆中尿酸酶的活性。采用DAS 2.1.1软件分析处理药动学数据，并对UHPSD和UOX进行生物等效性评价。UHPSD和UOX血药活性曲线符合二室模型。UHPSD提高了尿酸酶的生物利用度，UHPSD与UOX不具有生物等效性。

Abstract:

To study the pharmacokinetic and bioequivalence of hollow nanospheres self-assembled by hyaluronic acid-graft-poly（ethylene glycol）（HA-g-PEG） and sulfobutyl ether-beta-cyclodextrin（SCD） containing uricase（UHPSD） in SD rats. Rats were administrated with（i.v.） UHPSD and UOX，respectively. Blood sample were collected from eye socket，and the activity of uricase were assayed. Compartmental pharmacokinetics were analyzed by DAS 2.1.1 software，then the bioequivalence was judged. The activity-time curve of UHPSD and UOX were conformed to a two-compartment model with a lag time.