欣梦颗粒中丹参素在大鼠体内的药动学研究  

The Pharmacokinetics of Danshensu in Rats after Intragastric Administration of Xinmeng Granules

作　　者：王红玉[1] 李晶晶[1] 周莹[1] 俸珊[1] 徐晓玉[1] 

机构地区：[1]西南大学药学院&中医药学院重庆市高校中药新药筛选重点实验室国家中医药管理局中药药理学重点建设学科,重庆400715

出　　处：《中药新药与临床药理》2017年第4期494-498,共5页Traditional Chinese Drug Research and Clinical Pharmacology

基　　金：国家科技重大新药创制专项(2014ZX09304-306-04);教育部基本科研专项(XDJK2016E133)

摘　　要：目的研究不同剂量的欣梦颗粒给药后丹参素在大鼠体内的药代动力学特征。方法将18只大鼠随机分为3组,分别以1.25,2.50,5.00 g·kg^(-1)的剂量灌胃给予欣梦颗粒,RP-HPLC法检测大鼠血浆中丹参素的浓度,软件DAS 3.2.1计算药动学参数并比较药动学参数的差异。结果欣梦颗粒以1.25,2.50,5.00 g·kg^(-1)的剂量给药后,丹参素药-时曲线下面积(AUC_(0-t))分别为(5.88±1.02)、(19.44±2.22)、(64.14±14.28)μg·mL^(-1)·h;峰浓度(C_(max))分别为(2.931±0.479)、(5.413±0.429)、(11.509±2.684)μg·mL^(-1);达峰时间(T_(max))分别为(30.0±5.4)、(60.0±9.7)、(115.0±31.3)min;半衰期(t_(1/2))分别为(123.8±17.8)、(234.9±79.1)、(280.8±71.9)min;清除率(CL)分别为(198±28)、(128±16)、(80±18)L·h-1·kg^(-1)。增加给药剂量后,丹参素的AUC_(0-t)、C_(max)均增大,但均与剂量不成线性关系,且T_(max)和t_(1/2)均延长,CL减小。结论在1.25~5.00 g·kg^(-1)剂量范围内,剂量对欣梦颗粒中丹参素在大鼠体内的药动学有显著影响,丹参素呈现非线性药动学特征。Objective To study the pharmacokinetics of danshensu in rats intragastricly administrated with different doses of Xinmeng Granules. Methods Eighteen rats were randomly divided into 3 groups and were intragastricly administrated with Xinmeng Granules at the doses of 1.25, 2.50 and 5.00 g·kg^-1, respectively. The plasma of the rats were collected, and the concentrations of Danshensu in the plasma were detected by RP-HPLC. Then the pharmacokinetic parameters of Danshensu under different gavage doses were analyzed by the DAS 3.2.1 software package. Results After the rats have been intragastricly administrated with the Xinmeng Granules with the given doses, the pharmaeokinetic parameters of Danshensu in the rats are as follows： the areas under the curve（AUC0-t） were（5.88±1.02）μg·mL^-1·h, （19.44±2.22）μg·mL^-1·h and （64.14 ±14.28）μg·mL^-1·h, respectively; the peak concentrations （Cmax） were （2.931±0.479）μg·mL^-1, （5.413±0.429）μg·mL^-1 and （11.509±2.684）μg·mL^-1, respectively; the peak times（Tmax） were （30.0±5.4）min, （60.0±9.7）min and （115.0±31.3）min, respectively; the elimination half-lifes （t1/2） were （ 123.8 ±17.8）min, （264.9±79.1 ）min and （280.8±71.9）rain respectively; and the clearance rates（CL） were（ 198±28）L·h^-1·kg^-1, （128±16）L·h^-1·kg^-1 and （80±18）L·h^-1·kg^-1. With the increase of intragastric doses, both of the AUC0-t and the Cmax increased, but non-linearly. Meanwhile, the Tmax and the t1/2 also increased, but the CL decreased with the dose. Conclusion The pharmacokinetics of Danshensu in rats was significantly influenced by doses of Xinmeng Granules within the range from 1.25 to 5.00g·kg^-1 with a non-linear feature.

关 键 词：欣梦颗粒 丹参素 药物动力学 反相高效液相色谱法 非线性吸收 

分 类 号：R284.1[医药卫生—中药学]