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水飞蓟宾-卵磷脂复合物对水飞蓟素胶囊的相对生物利用度研究
Relative bioavailability of silybin-phosphatidylcholine compound
【摘要】 目的:评价水飞蓟宾-卵磷脂复合物对水飞蓟素胶囊的相对生物利用度。方法:选择22例20~40岁健康成年男性受试者,随机分为两组,自身前后交叉依次口服水飞蓟宾-卵磷脂复合物胶囊8粒(相当于水飞蓟宾280mg)和水飞蓟素胶囊2粒(相当于水飞蓟素280 mg,含水飞蓟宾112 mg),应用高效液相色谱法测定各受试者给药后不同时间点的血药浓度,并用3P97软件计算药动学参数。结果:水飞蓟宾-卵磷脂复合物和水飞蓟素胶囊的实测Tmax分别为(1.53±0.68)和(1.51±0.84)h;实测Cmax分别为(3525.2±1852.1)和(412.0±241.1) ng·mL-1;梯形法计算AUC0~11h分别为(5064.1±1881.6)和(842.0±327.3)ng·h·mL-1;t1/2β分别为(2.41±0.61)和(2.30±0.62)h。经统计学分析,两者的AUC0~11h和Cmax有显著性差异(P<0.05)。水飞蓟宾-卵磷脂复合物对于水飞蓟素胶囊的相对生物利用度为(270.4±139.6)%。结论:水飞蓟宾-卵磷脂复合物的生物利用度优于水飞蓟素胶囊。
【Abstract】 Objective:To assess the relative bioavailability of silybin-phosphatidylcholine com- pound (SPC) versus silymarin capsules (SC).Methods:22 Chinese healthy male volunteers were ran- domized to receive a single oral crossover dose of SPC (8 capsules equivalent to 280 mg silybin) or sily- marin capsules (2 capsules equivalent to 280 mg silymarin or 112 mg silybin).The plasma silybin con- centrations at certain timepoints after the administration of the two formulations were measured by HPLC. The pharmacokinetics parameters of SPC and SC were as follows:Tmax (1.53±0.68) vs.(1.51±0.84)h,Cmax(3525.2±1852.1)vs.(412.0±241.1)ng·mL-1,AUC0~11h(5064.1±1881.6)vs. (842.0±327.3)ng·h·mL-1 and t1/2β(2.41±0.61)vs.(2.30±0.62)h;the P values of these parameters were significantly different.The relative bioavailability of SPC was (270.4±139.6)%. Conclusion:The bioavailability of silibinin-phosphatidylcholine compound is superior to silymarin capsules.
【Key words】 silybin-phosphatidylcholine compound; silybin; silymarin; high performance liquid chromatography (HPLC); bioavailability;
- 【文献出处】 中国新药杂志 ,Chinese Journal of New Drugs , 编辑部邮箱 ,2006年10期
- 【分类号】R96
- 【被引频次】17
- 【下载频次】439