国产富马酸比索洛尔胶囊的人体相对生物利用度研究

RELATIVE BIOAVAILABILITY OF DOMESTIC BISOPROLOL HEMIFUMARATE CAPSULE IN HEALTHY VOLUNTEERS

10名男性健康志愿受试者单剂量交叉口服10mg富马酸比索洛尔胶囊和富马酸比索洛片,用高效液相色谱荧光检测法测定血浆富马酸比索洛尔浓度,进行富马酸比索洛尔胶囊的药代动力学和相对生物利用度研究.结果表明:富马酸比索洛尔胶囊和片剂的血药浓度时间曲线图均符合口服吸收二室模型,主要药动学参数T_ρ口分别为1.05±1.89h和2.20±l.75h,C_mAX分别为63.27±16.05υg·L^-1和57.49±10.49υg·L^-1/,t_1/2β分别12.79±2.86h和13.11±3.93h,AUC分别为788.50±105.02υg·L^-1和759.22±111.56υg·L^-1.两种剂型的药代动力学参数经统计学分析无明显性差异(P>0.05).富马酸比索洛尔胶囊的相对生物利用度为100.1±18.7%,结果提示受试的胶囊剂和对照的片剂生物等效.

The pharmacokinetic profiles and the bioavailability of domestic Bisoprolol hemifumarate capsules were studied in 10 healthy male volunteers. A single oral dose of 10mg Bisoprolol capsules and tablets were given according to a cross over design. Plasma concentrations were measured by HPLC. The concentration - time curves of the two products of Bisoprolol were fitted to a two - comparment model with oral absorption. There were no significant difference in each phamacokinetic parameters between the capsules and the tablets (P>0.05). T_pwere 2.05±1.89 h and 2.20±1.75 h, C_(max) were 63.27±16.05μg·L^(-1) and 57.49±10.49μg·L^(-1), t_(1/2/β)were 12.79±2.86 h and 13.11±3.93 h, AUC were 788.50±105.02μg·h·L^(-1) and 795.22±111.56μg·h·L^(-1). The relative bioavilability of the Bisoprolol capsule to the tablet was 100.1±18.7%. These results suggested that two products are bioequivalent.