平衡透析法测定人体外血浆中原花青素B2、表儿茶素蛋白结合率  

Plasma protein binding rate of procyanidin B2,epicatechin by equilibrium dialysis method in human plasma

作　　者：程小桂[1] 居文政[2] 戴国梁[1] 马世堂[1] 谈恒山[3,4] 

机构地区：[1]南京中医药大学药学院,江苏南京210002 [2]南京中医药大学附属医院临床药理科,江苏南京210029 [3]南京中医药大学 [4]南京军区总医院,江苏南京210002

出　　处：《中国药理学通报》2013年第10期1465-1467,共3页Chinese Pharmacological Bulletin

基　　金：江苏省中医药领军人才项目(No LJ200906);江苏高校优势学科建设工程资助项目2010;中药新药临床评价研究技术平台(南京)建设(No 2012ZX09303009-002)重大新药创制

摘　　要：目的建立检测原花青素B2、表儿茶素在血浆中药物浓度的方法,并测定其体外血浆蛋白结合率。方法采用平衡透析法测定血浆蛋白结合率,建立HPLC法测定各成分的血药浓度及游离药物浓度,生物样本用乙酸乙酯溶液提取的方法。结果在低、中、高3种浓度下,原花青素B2和表儿茶素在人体外血浆中的蛋白结合率分别为(44.21±2.80)%,(52.60±1.92)%,(48.11±3.09)%和(47.12±2.85)%,(55.03±2.47)%,(43.69±1.53)%。结论采用HPLC法对原花青素B2、表儿茶素进行分离,方法简便、可靠、稳定。体外实验中原花青素B2和表儿茶素与人血浆属中等结合型药物,且蛋白结合率随着药物浓度的增加无明显的浓度依赖性。Aim To establish a detection method for determina- tion of procyanidin B2 and epicatechin in plasma and to study their plasma protein binding rates. Methods The equilibrium dialysis was carried out to determine the plasma protein binding rate, and the drug concentration was detected by HPLC method. The biological samples were all handled with acetic ether-extrac- ting. Results The binding rates of procyanidin B2 and epicate- chin in human plasma at three concentration levels were （44. 21 ±2.80）%, （52.60± 1.92）%, （48.11 ±3.09）% and （47.12±2.85）%, （55.03 ±2.47）%, （43.69 ±1.53）%, respectively. Conclusions The method of determining the con- centration of procyanidin B2 and epicatechin by HPLC is simple, reliable and stable. In human plasma, procyanidin B2 and epi- eateehin are bonded with protein moderately. Moreover, the binding rates do not proportionally depend on the eoneentration of procyanidin B2 and epicatechin.

关 键 词：原花青素B2 表儿茶素 平衡透析法 蛋白结合率 高效液相色谱法 人体外血浆 

分 类 号：R282.71[医药卫生—中药学] R284.1[医药卫生—中医学]