叶黄素制品在大鼠体内药代动力学和生物利用度  

Pharmacokinetics and relative bioavailability of lutein preparation in rats

作　　者：张莉华[1] 许新德[1] 邵斌[1] 周慧[2] 洪毅敏[1] 虞雷明[1] 章鹏飞[1] 

机构地区：[1]浙江医药股份有限公司新昌制药厂,新昌312500 [2]浙江大学药学院药物分析与代谢研究室,杭州310058

出　　处：《中药药理与临床》2014年第5期47-50,共4页Pharmacology and Clinics of Chinese Materia Medica

摘　　要：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 relatively bioavailability of two lutein preparation（ lutein oil suspension and lutein microencapsulation） in rats. Methods： A LC-MS / MS method was developed for determination of lutein in rats plasma. Oral dose of 100 mg / kg of lutein microencapsulation or lutein oil suspension was administered to rats,and the concentrations of lutein were determined by the LC-MS /MS method. The pharmacokinetic parameters were calculated by the program DAS 2. 0. The relatively bioavailability of lutein was calculated according to AUC（ 0-t）. Results： Excellent linear relationship was obtained in the range of 5 ng / ml ~ 200 ng / ml（ r = 0. 997）. Lowest limit of quantification（ LLOQ） of lutein was 5 ng / ml. The relative recoveries were 69. 7%,94. 9% and 98. 1% respectively at three concentrations（ 10,50 and 160 ng/ml）,extraction of recoveries were 75. 3%,70. 9% and 73. 4%,respectively. The Cmax,Tmax,AUC（ 0-32）of lutein microencapsulation and lutein oil suspension were（ 65. 8 ± 38. 9） mg / L and（ 48. 3 ± 17. 3） mg / L,（ 4. 7 ± 3. 0） h and（ 3. 7 ± 0. 8） h,（ 566.6 ± 203. 6） mg / L·h and（ 385. 2 ± 107. 3） mg / L·h,respectively. The relative bioavailability of lutein microencapsulation was 147. 1%.Conclusion： The established LC-MS / MS method was simple and rapid,which can be used to determine lutein plasma concentration and study the pharmacokinetic profiles. Compared with lutein oil suspension,lutein microencapsulation has improved the bioavailability of lutein in rats.

关 键 词：叶黄素微胶囊 叶黄素油悬浮液 药代动力学 生物利用度 大鼠 

分 类 号：R285[医药卫生—中药学]