盐酸小檗碱磷脂复合物在兔体内的药动学及相对生物利用度研究

目的:考察盐酸小檗碱磷脂复合物在兔体内的药动学及相对生物利用度。方法:将6只兔随机均分为A、B组,分别灌服盐酸小檗碱原料药和盐酸小檗碱磷脂复合物(50mg·kg-1,以盐酸小檗碱计),于给药前及给药后0.5、1、1.5、2、3、4、6、8、10、12、24h股静脉取血,给药1周后,2组交叉给药,相同时间点取血,采用高效液相色谱法测定其中盐酸小檗碱浓度,并计算药动学参数及相对生物利用度。结果:血浆中盐酸小檗碱检测浓度的线性范围为20.0～640.0μg·L-1(r=0.9996);A组和B组的tmax分别为(0.24±0.12)、(0.23±0.27)h,t1分别为(5.01±0.17)、(3.80±0.16)h,cmax分别为(59.88±6.10)、(194.26±8.60)μg·L-1,AUC0～24/2βh分别为(446.98±10.50)、(1110.12±28.40)μg·h·L-1;盐酸小檗碱磷脂复合物相对于其原料药的相对生物利用度为(273.3±3.40)%。结论:盐酸小檗碱磷脂复合物与其原料药比较,增加了血浆中药物浓度,显著提高了盐酸小檗碱的相对生物利用度。

Pharmacokinetics and Relative Bioavailability Study of Berberine Hydrochloride Phytosome in Rabbits

OBJECTIVE： To study pharmacokinetics and relative bioavailability of berberine hydrochloride phytosome in rabbits. METHODS： 6 rabbits were randomly divided into group A and group B. Two groups were given berberine hydrochloride or berberine hydrochloride phytosomes （50 mg. kg-1 of berberine hydrochloride） respectively. Blood samples of femoral vein were collected before administration and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 after administration. After one week of treatment, therapy of two groups intercrossed. The concentrations of berberine hydrochloride in plasma were determined by HPLC. The pharmacokinetic parameters and relative bioavailability were calculated. RESULTS： The linear range of berberine hydrochloride was 20.0-640.0 μg.L^-1 （r=0.999 6）. The pharmacokinetic parameters of group A vs. group B were as follows： tmax： （0.24 ± 0.12）h vs.（0.23 ± 0.27） h, t1/2β： （5.01 ± 0.17） h vs.（3.80 ± 0.16） h, cmax： （59.88± 6.10） μg.L^-1 vs.（194.26 ± 8.60） μg.L^-1, AUC0-24h： （446.98 ± 10.50）μg.h.L^-1 vs. （1 110.12 ± 28.40） μg.h.L^-1. The relative bioavailability of berberine hydrochloride phytosome was （273.3 ± 3.40）%, compared with raw material. CONCLUSIONS： Compared with raw material, berberine hydrochloride phytosomes significantly increases the plasma concentration of berberine hydrochloride and improves the relative bioavailability of it.