阿司匹林磷脂复合物自微乳在大鼠体内的药动学及生物利用度研究  

Pharmacokinetic and Bioavailability Study of Aspirin Phospholipid Complex Self-microemulsion in Rats in vivo

作　　者：徐旖旎 王益 严俊丽 贺智勇 周雪 沈祥春 陶玲 

机构地区：[1]贵州医科大学药学院,贵阳550004 [2]贵州省普通高等学校天然药物药理与成药性评价重点实验室,贵阳550025

出　　处：《中国药房》2017年第31期4373-4376,共4页China Pharmacy

基　　金：贵州省科技计划项目(No.黔科合支撑[2017]2890);贵州省科技创新人才团队建设项目(No.黔科合人才团队[2015]4025号);贵州省高层次创新型人才培养项目(No.黔科合人才[2015]4029);贵阳市科技计划项目(No.筑科合同[20141001]12号);贵州省普通高等学校创新团队建设项目(No.黔教合人才团队字[2014]31)

摘　　要：目的:研究阿司匹林磷脂复合物自微乳在大鼠体内的药动学行为及生物利用度。方法:将12只SD大鼠随机分为阿司匹林混悬液组(10 mg/kg)和阿司匹林磷脂复合物自微乳组(10 mg/kg),每组6只。各组大鼠分别ig给药,并于给药前及给药0.083、0.25、0.5、0.75、1.0、2.0、3.0、4.0、6.0、8.0、12.0 h后于颈静脉采血0.6 mL。采用高效液相色谱法测定2组大鼠血浆中水杨酸的浓度,并采用DAS 2.0药动学软件计算药动学参数和相对生物利用度。结果:阿司匹林混悬液和阿司匹林磷脂复合物自微乳在大鼠体内的药动学过程均符合一室模型。水杨酸在阿司匹林混悬液组和阿司匹林磷脂复合物自微乳组大鼠的c_(max)分别为(1.904±0.208)、(6.457±1.091)μg/mL,AUC_(0-12 h)分别为(12.860±1.327)、(47.270±12.860)μg/(h·mL),t_(max)分别为(2.167±0.983)、(0.917±0.540)h。与ig阿司匹林混悬液比较,ig阿司匹林磷脂复合物自微乳在大鼠体内水杨酸的c_(max)、AUC_(0-12 h)均显著增加(P<0.01),t_(max)显著减小(P<0.05),相对生物利用度为367.57%。结论:阿司匹林制成磷脂复合物自微乳后可提高水杨酸在胃肠道的吸收,相对生物利用度较高。OBJECTIVE：To study the pharmacokinetics behaviors and the bioavailability of aspirin phospholipid complex selfmicroemulsion in rats in vivo. METHODS：12 SD rats were randomly divided into aspirin suspension group（10 mg/kg）and aspirin phospholipid complex self-microemulsion group（10 mg/kg）,6 in each group. Rats were intragastrically administrated,and blood sample 0.6 mL was taken from jugular vein before administration and after 0.083,0.25,0.5,0.75,1.0,2.0,3.0,4.0,6.0,8.0,12.0 h of administration. HPLC was used to determine the concentration of salicylic acid in rats＇ plasma. DAS 2.0 pharmacokinetic software was adopted to calculate the pharmacokinetic parameters and relative bioavailability. RESULTS：The pharmacokinetic processes of both aspirin suspension and aspirin phospholipid complex self-microemulsion were in line with one-compartment model. The salicylic acid of c（max） of rats in aspirin suspension group and aspirin phospholipid complex self-microemulsion group were（1.904±0.208）,（6.457±1.091）μg/mL;AUC（0-12 h） were（12.860 ± 1.327）,（47.270 ± 12.860） μg/（h·mL）;t（max） were（2.167 ±0.983）,（0.917±0.540）h,respectively. Compared with aspirin suspension,salicylic acid of c（max）and AUC（0-12 h） of aspirin phospholipid complex self-microemulsion in rats in vivo were significantly increased（P〈0.01）,while t（max） was significantly decreased（P〈0.05）;the relative bioavailability was 367.57%. CONCLUSIONS：Making aspirin into phospholipid complex self-microemulsion can improve the gastrointestinal absorption,with high relative bioavailability.

关 键 词：阿司匹林 磷脂复合物 自微乳 高效液相色谱法 药动学 相对生物利用度 大鼠 

分 类 号：R945[医药卫生—微生物与生化药学]