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番茄红素脂质体的体外释放及大鼠体内药代动力学和抗氧化功能
引用本文:田艳燕,葛兰,段相林,高志清,常彦忠.番茄红素脂质体的体外释放及大鼠体内药代动力学和抗氧化功能[J].药学学报,2007,42(10):1107-1111.
作者姓名:田艳燕  葛兰  段相林  高志清  常彦忠
作者单位:1. 河北师范大学,河北省动物生理生化与分子生物学重点实验室,河北,石家庄,050016
2. 河北省药品审评认证中心,河北,石家庄,050091
基金项目:河北师范大学校科研和教改项目
摘    要:利用旋转薄膜-超声法制备了番茄红素脂质体并研究其体外释放,大鼠体内药代动力学和对机体抗氧化能力的影响。用液相色谱法测定大鼠体内的番茄红素含量,所得数据进行3P97程序处理,得到各主要药代动力学参数;配制人工胃液和肠液,比较番茄红素油和番茄红素脂质体的体外释放效果;番茄红素油和番茄红素脂质体灌胃后,用试剂盒测定大鼠血清和肝组织匀浆中的超氧化物歧化酶活性、丙二醛、总抗氧化能力、过氧化氢酶及谷胱甘肽过氧化酶的含量。结果显示,脂质体体外释放呈肠溶性;番茄红素油及番茄红素脂质体的Tmax分别为4.45和7.45 h;Cmax为0.473和0.654 μg·mL-1;AUC分别为12.38和21.67 μg·h·mL-1。抗氧化指标测定结果表明:番茄红素脂质体比番茄红素油显著地提高机体内抗氧化酶的活力,抑制脂质过氧化。

关 键 词:番茄红素  脂质体  高效液相色谱法  药代动力学
文章编号:0513-4870(2007)10-1107-05
收稿时间:2007-04-30
修稿时间:2007-04-30

Lycopene liposomes: lycopene release in vitroand pharmaceutical behaviors and antioxidation in vivo
TIAN Yan-yan,GE Lan,DUAN Xiang-lin,GAO Zhi-qing,CHANG Yan-zhong.Lycopene liposomes: lycopene release in vitroand pharmaceutical behaviors and antioxidation in vivo[J].Acta Pharmaceutica Sinica,2007,42(10):1107-1111.
Authors:TIAN Yan-yan  GE Lan  DUAN Xiang-lin  GAO Zhi-qing  CHANG Yan-zhong
Institution:1. The Key Laboratory of Animal Physiology, Biochemistry and Molecular Biology of Hebei Province, Hebei Normal University, Shijiazhuang 050016, China; 2. Hebei Drug Evaluation and Certification Center, Shijiazhuang 050091, China
Abstract:Lycopene liposomes were prepared by conventional rotary-evaporated film-ultrasonication method. The release of lycopene from lycopene liposome was evaluated in vitro. The pharmacokinetic parameters of lycopene liposomes (L-LYC) and lycopene (LYC) oil, the effect of LYC and L-LYC on antioxidation were also investigated in rats. HPLC method was used to assay the concentration of lycopene in rat's plasma. Pharmacokinetic parameters were estimated by 3P97 program. The release of L-LYC and LYC were measured in the artificial stomach liquid and bowel liquid. After 4 weeks of L-LYC or LYC feeding, the activity of SOD, T-AOC, GSH-Px, MDA and CAT in serum and liver were measured separately. The pharmacokinetic parameters of LYC oil and L-LYC in a single dose were 4.45 and 7.45 h for Tmax; 0.473 and 0.654 microg x mL(-1) for Cmax; 12.38 and 21.67 mirog x h x mL(-1) for AUC,respectively. The activities of GSH-Px and T-AOC in serum and liver of the L-LYC group increased (P < 0.05) and the concentrations of MDA and CAT decreased significantly (P < 0.05). It could be concluded that lycopene liposomes could prolong the time of absorption. L-LYC could increase antioxidative effect and reduce lipid peroxidation obviously compared with LYC in rats.
Keywords:lycopene  liposome  high performance liquid chromatography  pharmacokinetics
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