莲心总碱在大鼠体内的血药浓度及组织分布  

Plasma Concentration and Tissue Distribution of Total Alkaloids of Lianzixin after Intragastric and Intravenous Administration in Rats

作　　者：黄颖[1] 班翊[1] 胡本容[1] 王嘉陵[1] 向继洲[1] 

机构地区：[1]华中科技大学同济医学院基础医学院药理学系,武汉430030

出　　处：《华中科技大学学报（医学版）》2006年第1期23-26,共4页Acta Medicinae Universitatis Scientiae et Technologiae Huazhong

基　　金：华中高科项目(No.3183507009);卫生部科研基金(No.98DJ15-87)资助项目

摘　　要：目的研究大鼠灌胃及静脉注射莲心总碱(Total alkaloids of Lianzixin,TAL)的血药浓度和组织分布。方法给予TAL后,采用反相高效液相色谱法检测各时间点血浆和组织药物浓度,用DAS(drug and statistics)程序拟合房室模型并计算药代动力学参数。结果静脉注射TAL 20 mg/kg,药时曲线符合三室模型,其主要药代动力学参数为:分布t1/2α为0.367 min,消除t1/2γ为841.597 min,血浆清除率(CL)为2.336 L/min,曲线下面积AUC0-1080和AUC0-∞分别为639.392和823.754(mg.min)/L,MRT0-∞为866.354 min;灌胃TAL 20 mg/kg,曲线下面积AUC0-1080和AUC0-∞分别为508.578和787.035(mg.min)/L,MRT0-∞为1466.040 min。计算所得TAL的绝对生物利用度为80%。TAL 20mg/kg灌胃后,迅速分布至各主要器官组织,其中以肝浓度最高;肺、心次之,脑组织最低。肝浓度在30 min有一谷值,而此时其他各组织的浓度则有所上升。与灌胃不同,静脉注射TAL以肺中浓度最高,其次为心、肾。5 min时,心、肺、肾组织各出现一浓度峰值,随后下降,4 h时又可见药物浓度回升。结论TAL吸收迅速,分布广泛,Vc较大,t1/2γ较长。除脑分布较少外,其他脏器的浓度均远高于血浆药物浓度。Objective To study the blood concentration and tissue distribution of total alkaloids of Lianzixin （TAL） after intragastric and intravenous administration. Methods The plasma and tissuc concentrations of TAL were detected by using reversed phase high performance liquid chromatography method and the data was deah with drug and statistics program to calculate the pharmacokinetics parameters and select apartment modcl. Results The time-concentration curve of TAI. （20 mg/kg） intravenous administration corresponded to the model of thrce apartmcnts. The main pharmacokinetics parameters were： t1 2α = 0.367 min. t12γ= 841.597 min. （CL=2. 336Lmin. AUC0 1080 =639.392 （mg · min）/LAUC0, =823.754 （mg · min）/L and MRT0 =866. 354 min. After intragastric administration of TAL （20 mg/kg）, the parameters were as follows： AUC0 1080 =508.578 （mg·min）/L AUC0=787.035 （mg·min）/L and MRT0=1466.040 min. The calculated absolute bioavailability was 80 %. TAL. after intragastric administration at 20 mg kg · was quickly distributed to main organs, highest in liver at 10 or 30 min after administration, followed by lung and heart, lowcst in brain at 30 min or 1 h. Meanwhile. the eoneentrations in other tissues were increased gently. After intravenous administration of TAL. the highest level appeared in the lung. followed by heart and kidney. At 5 min. a concentration peak occurred in heart, lung and kidney tissues separately, and dropped subsequently.then re-ascended to a higher level at 4 h. Conclusion The pharmacokinetics characters of TAL are extensive distribution, quick transfer, long in t1 2α=and large in Vc. The concentration of TAl. in all tissues, except brain, is higher than that in plasma.

关 键 词：莲心总碱 药代动力学 组织分布 反相高效液相色谱法 

分 类 号：R285.5[医药卫生—中药学]