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目的:研究叶黄素微胶囊和叶黄素油悬浮液两种叶黄素制品在大鼠体内的药代动力学和相对生物利用度。方法:建立大鼠血浆中叶黄素的LC-MS/MS测定方法。考察大鼠分别灌胃给予100 mg/kg叶黄素微胶囊或叶黄素油悬浮液后血药浓度变化,应用DAS 2.0软件计算药动学参数,根据叶黄素微胶囊和叶黄素油悬浮液药-时曲线下面积AUC(0-t)计算相对生物利用度。结果:叶黄素浓度5 ng/ml~200 ng/ml的浓度范围内线性关系良好(r=0.997);定量下限为为5 ng/ml;10 ng/ml、50 ng/ml和160 ng/ml三个浓度剂量组的方法回收率分别为69.7%、94.9%和98.1%;提取回收率分别为75.3%、70.9%和73.4%。大鼠单剂量给予叶黄素微胶囊和叶黄素油悬浮液的主要药动学参数Cmax分别为(65.8±38.9)mg/L和(48.3±17.3)mg/L,Tmax分别为(4.7±3.0)h和(3.7±0.8)h,AUC(0-32)分别为(566.6±203.6)mg/L·h和(385.2±107.3)mg/L·h,叶黄素微胶囊的相对生物利用度为147.1%。结论:所建立LC-MS/MS方法简单、快速,可用于大鼠叶黄素血药浓度的测定和药动学研究。以叶黄素油悬浮液为参比制剂,叶黄素微胶囊在大鼠体内的生物利用度明显提高。
Objective: To study the pharmacokinetics and relative bioavailability of two lutein preparations of lutein microcapsule and lutein oil suspension in rats. Methods: To establish a method for the determination of lutein in rat plasma by LC-MS / MS. The concentration of lutein microcapsules or lutein oil suspension was intragastrically administered to rats at 100 mg / kg, and the pharmacokinetic parameters were calculated by DAS 2.0 software. According to the drug-time curve of lutein microcapsules and lutein oil suspension Under the area AUC (0-t) to calculate the relative bioavailability. Results: The linear range of lutein concentration was 5 ng / ml ~ 200 ng / ml (r = 0.997); the lower limit of quantitation was 5 ng / ml; the concentrations of 10 ng / ml, 50 ng / ml and 160 ng / ml, respectively. The recoveries of three methods were 69.7%, 94.9% and 98.1% respectively. The recoveries were 75.3%, 70.9% and 73.4% respectively. The main pharmacokinetic parameters (Cmax) were (65.8 ± 38.9) mg / L and (48.3 ± 17.3) mg / L, and the Tmax were (4.7 ± 3.0) h in single dose of lutein microcapsule and lutein oil suspension respectively (3.7 ± 0.8) h and (566.6 ± 203.6) mg / L · h and (385.2 ± 107.3) mg / L · h, respectively. The relative bioavailability of lutein microcapsules was 147.1%. Conclusion: The established LC-MS / MS method is simple and rapid and can be used for the determination of lutein blood concentration and pharmacokinetics in rats. Taking lutein oil suspension as reference preparation, the bioavailability of lutein microcapsules in rats was significantly increased.