黄藤中巴马汀与药根碱在大鼠体内药动学及口服生物利用度的研究

Pharmacokinetics and oral bioavailability of palmatine and jatrorrhizine in Huangteng in rats

该文通过灌胃和尾静脉2种方式对大鼠给予黄藤总生物碱,采用RP-HPLC测定大鼠血浆中巴马汀与药根碱的浓度变化后,通过3P97软件计算巴马汀与药根碱的药代动力学参数和口服生物利用度。大鼠经灌胃与尾静脉2种方式给予黄藤总生物碱60 mg·kg^(-1)后,测得的主要药代动力学参数如下:灌胃给药组中巴马汀和药根碱的Cmax分别为(0.91±0.06),(0.70±0.08)mg·L^(-1),tmax分别为(35.24±0.83),(47.76±1.24)min,t1/2分别为(187.03±1.53),(105.64±16.99)min,AUC分别为(280.30±18.69),(144.36±1.06)mg·min·L^(-1);静脉注射给药组中巴马汀和药根碱的t1/2分别为(172.18±12.38),(147.26±1.82)min,AUC分别为(2 553.14±214.91),(328.83±10.81)mg·min·L^(-1)。巴马汀的口服生物利用度为10.98%,药根碱的口服生物利用度为43.90%。

In this study, the total alkaloids of Huangteng were given to the rats by the methods of intragastric administration and tail vein. After the concentration changes of palmatine and jatrorrhizine in the plasma of rats were determined by RP-HPLC, pharmacoki- netie parameters and oral bioavailahility were calculated by 3P97 software. After the rats were pre-treated with total alkaloid 60 mg · kg- 1 by the methods of intragastrle administration and tail vein, the main pharmacokinetie parameters were determined as follows ： in the intragastric administration group, the Cmax of palmatine and jatrorrhizine were （0. 91 ± 0. 06 ）, （0. 70 ± 0. 08 ） mg ·L- 1 ; tmax of palma- tine and jatrorrhizine were （ 35. 24 ± 0. 83 ）, （47. 76 ± 1.24 ） rain ; t1/2 of palmatine and jatrorrhizine were （ 187. 03± 1.53 ）, （ 105.64 ± 16. 99） min, AUC of palmatine and jatrorrhizine were （280. 30 ± 18.69 ）, （ 144. 36 ±1.06） mg · min · L- 1 ; in the intra- venous injection group, the t1/2 of palmatine and jatrorrhizine were （ 172. 18 ± 12. 38） , （ 147. 26± 1.82） min; AUC of palmatine and jatrorrhizine were （2 553.14 ±214. 91 ）, （328.83 ± 10. 81 ）mg ·min ·L-1. The oral bioavailability of palmatine was 10. 98% andjatrorrhizine was 43.90%.