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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

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【作者】 李伟高钧丁宁赵洪芝魏峰

【Author】 LI Wei~1 GAO Jun~1 DING Ning~2 ZHAO Hong-zhi~1 WEI Feng~1 (1 Institute of Modern TCM,Tianjin Tasly Group Co.,Ltd.,Tianjin 300402,China;2 Department of Marketing,Tianjin Tasly Medicine Distribution Group Co.,Ltd.,Tianjin 300402,China)

【机构】 天津天士力集团药物研究院现代中药研究所天津天士力医药营销集团有限公司天津天士力集团药物研究院现代中药研究所 天津 300402天津 300402

【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.

  • 【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
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