肾康注射液对大鼠体内厄贝沙坦药动学的影响
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篇名: 肾康注射液对大鼠体内厄贝沙坦药动学的影响
TITLE:
摘要: 目的:研究肾康注射液对大鼠体内厄贝沙坦药动学的影响。方法:取18只SD大鼠随机分为对照组(生理盐水)和肾康注射液组(以生药量计为4 g /kg),每组9只,每天ip给药2次,连续给药7 d。末次给药1 h后,两组大鼠均ig厄贝沙坦25 mg/kg,分别于厄贝沙坦给药前及给药后0.25、0.5、1、2、4、8、12、24、32、48、56、72、96 h经眼底静脉丛采血0.3 mL。以联苯双酯为内标,采用高效液相色谱法测定大鼠血浆中厄贝沙坦的血药浓度,利用Phoenix WinNolin® 6.1药动学软件中非房室模型拟合并计算药动学参数。结果:对照组和肾康注射液组大鼠ig厄贝沙坦后,AUC0-96 h分别为(28.82±10.49)、(35.64±9.99) mg·h/L,cmax分别为(0.64±0.15)、(0.76±0.33) mg/L,tmax分别为(13.07±16.70)、(10.23±3.97) h,CLZ/F分别为(0.85±0.35)、(0.63±0.21) L/(h·kg),VZ/F分别为(38.24±24.87)、(30.99±9.75) mL/kg,组间比较差异均无统计学意义(P>0.05)。结论:肾康注射液在正常给药剂量下不影响厄贝沙坦在大鼠体内的药动学过程。
ABSTRACT: OBJECTIVE: To study the effect of Shenkang injection on the irbesartan pharmacokinetics in rats in vivo. METHODS: 18 SD rats were randomly divided into control group (normal saline) and Shenkang injection (calculated by crude drug as 4 g/kg), 9 in each group, which were intraperitoneally injected twice a day, for 7 d. After 1 h of last administration, 25 mg/kg irbesartan was intragastrically administrated. 0.3 mL sample blood was taken in fundus venous plexus before administration of irbesartan and after 0.25, 0.5, 1, 2, 4, 8, 12, 24, 32, 48, 56, 72, 96 h of administration. Using biphenyl diester as inner standard, HPLC was adopted to determine the plasma concentration of irbesartan in plasma of rats, and pharmacokinetic parameters were calculated by using non-compartmental model in Phoenix WinNolin® 6.1 pharmacokinetic software. RESULTS: After intragastrically administrated irbesartan in rats in control group and Shenkang injection group, AUC0-96 h were (28.82±10.49), (35.64±9.99) mg·h/L; cmax were (0.64±0.15), (0.76±0.33) mg/L; tmax were (13.07±16.70), (10.23±3.97) h; CLZ/F were (0.85±0.35), (0.63±0.21) L/(h·kg); VZ/F were (38.24±24.87), (30.99±9.75) mL/kg respectively, with no statistical significances (P>0.05). CONCLUSIONS: Shenkang injection will not affect the in vivo pharmacokinetics process of irbesartan in normal dose on rats.
期刊: 2017年第28卷第34期
作者: 金贞姬,常泽娜,朱震菡,杨长青
AUTHORS: JIN Zhenji,CHANG Zena,ZHU Zhenhan,YANG Changqing
关键字: 肾康注射液;厄贝沙坦;药动学;大鼠
KEYWORDS: Shenkang injection; Irbesartan; Pharmacokinetics; Rats
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