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
x

请在关注微信后,向客服人员索取文件

篇名: 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
TITLE:
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cmax分别为(1.904±0.208)、(6.457±1.091) μg/mL,AUC0-12 h分别为(12.860±1.327)、(47.270±12.860) μg/(h·mL),tmax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cmax、AUC0-12 h均显著增加(P<0.01),tmax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。
ABSTRACT: OBJECTIVE: To study the pharmacokinetics behaviors and the bioavailability of aspirin phospholipid complex self-microemulsion 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 cmax of rats in aspirin suspension group and aspirin phospholipid complex self-microemulsion group were (1.904±0.208), (6.457±1.091) μg/mL; AUC0-12 h were (12.860±1.327), (47.270±12.860) μg/(h·mL); tmax were (2.167±0.983), (0.917±0.540) h, respectively. Compared with aspirin suspension, salicylic acid of cmax and AUC0-12 h of aspirin phospholipid complex self-microemulsion in rats in vivo were significantly increased (P<0.01), while tmax 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.
期刊: 2017年第28卷第31期
作者: 徐旖旎,王益,严俊丽,贺智勇,周雪,沈祥春,陶玲
AUTHORS: XU Yini,WANG Yi,YAN Junli,HE Zhiyong,ZHOU Xue,SHEN Xiangchun,TAO Ling
关键字: 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
KEYWORDS: Aspirin; Phospholipid complex; Self-microemulsion; HPLC; Pharmacokinetics; Relative bioavailability; Rats
阅读数: 163 次
本月下载数: 1 次

* 注:未经本站明确许可,任何网站不得非法盗链资源下载连接及抄袭本站原创内容资源!在此感谢您的支持与合作!