姜黄素前体脂质体在大鼠体内药动学研究  

Pharmacokinetics and Bioavailability of Curcumin-Proliposomes in Rats

作　　者：徐文杰 李智勇 陈雪婷 XU Wen-jie;LI Zhi-yong;Chen Xue-ting(Guangdong Second Traditional Chinese Medicine Hospital(Guangdong Research Institute of Traditional Chinese Medicine Manufacturing Technology),Guangdong Provincial Key Laboratory of Traditional Chinese Medicine Research and Development,Guangdong Guangzhou 510095)

机构地区：[1]广东省第二中医院(广东省中医药工程技术研究院),广东省中医药研究开发重点实验室,广东广州510095

出　　处：《按摩与康复医学》2021年第9期63-66,共4页Chinese Manipulation and Rehabilitation Medicine

基　　金：广东省医学科学技术研究基金项目,编号:A2017563。

摘　　要：目的:建立测定大鼠血浆中姜黄素的HPLC/MS方法,评价姜黄素和其前体脂质体在大鼠体内的药代动力学特征。方法:SD大鼠随机分为姜黄素原料药组和姜黄素前体脂质体组,灌胃给药,分别于给药后不同时间点取血,采用HPLC/MS测定姜黄素的血药浓度,绘制药时曲线,运用药动学软件计算单次给药后的姜黄素药动学参数。结果:原料药组与前体脂质体组的姜黄素均符合二室开放模型,与原料药相比,前体脂质体AUC0→∞、tmax、Cmax、CL均有显著性差异(P<0.01),t1/2α、t1/2β、V均无显著性差异(P>0.05)。给药后10min~480min,口服姜黄素原料药和姜黄素前体脂质体的药动学参数AUC0→∞分别为(0.35±0.037)和(11.51±0.047)mg·L-1·h,t1/2α分别为(0.32±0.06)和(10.05±0.02)h-1,t1/2β分别为(3.05±0.11)和(4.98±0.08)h-1,tmax分别为(0.580±0.001)和(2.43±0.002)h,Cmax分别为(0.13±0.049)和(0.58±0.042)mg·L-1,CL分别为(1020.61±38.51)和(80.78±8.63)L·h-1·kg-1,V分别为(439.04±20.22)和(80.20±7.45)L·kg-1。结论:将姜黄素制备成前体脂质体能提高其生物利用度,达到了实验预期要求。Objective:To establish a high-performance liquid chromatography-mass spectrometry (HPLC-MS) method for simultaneously determining the contents of curcumin in rat’s plasma,and study the pharmacokinetics of the curcumin and the curcumin-proliposomes,to investigate the relative bioavailability of Curcumin-Proliposomes.Methods:SD rats were divided randomly into two groups for the respective administration of a single dose of curcumin and curcumin-proliposomes.Blood samples were collected at different times points and the concentrations of curcumin in rat plasma were simulataneously determined by HPLC-MS.The pharmacokinetic parameters were calculated by pharmacokinetic program.Results:The pharmacokintic parameters of curcumin and curcumin-proliposomes were as follows:AUC0→∞(0.35±0.037) and (11.51±0.047) mg·L-1·h,t1/2α(0.32±0.06) and (10.05±0.02) h-1,t1/2β(3.05±0.11) and (4.98±0.08) h-1,tmax(0.580±0.001) and (2.43±0.002) h,Cmax(0.13±0.049) and (0.58±0.042) mg·L-1,CL(1020.61±38.51) and (80.78±8.63) L·h-1·kg-1,V (439.04±20.22) and (80.20±7.45) L·kg-1,respectively.Conclusions:The bioavailability of curcumin was increased by making them into proliposomes,and the biopharmaceutical property of curcumin was improved.

关 键 词：姜黄素 前体脂质体 药动学 生物利用度 

分 类 号：R2749[医药卫生—中医骨伤科学] R246[医药卫生—中医学]