伏立康唑胶囊在健康人体的生物等效性研究

Study on Bioequivalence of Voriconazol Capsules and Tablets in Healthy Volunteers

目的研究伏立康唑胶囊和片剂在健康人体的生物等效性。方法采用随机自身交叉给药方法,24例健康男性志愿者单剂量口服伏立康唑胶囊与片剂。用液质联用方法测定血浆中的伏立康唑浓度,计算药代动力学参数。结果伏立康唑胶囊和片剂的的主要药代动力学参数,Tmax分别为(0.9±0.46)、(0.9±0.54)h;Cmax分别为(2340.83±607.95)、(1950.83±656.25)μg·L-1;t1/2分别为(8.6±3.53)、(8.8±4.16)h;AUC0-tn分别为(11529.38±6501.42)、(10217.92±5428.32)μg.h.L-1;AUC0-∞分别为(12779.70±8020.12)、(11404.55±7156.16)μg.h.L-1。受试制剂与参比制剂比较,受试制剂的相对生物利用度F0-tn、F0-∞分别为(114.08±20.92)%、(113.84±22.50)%。结论伏立康唑胶囊和片剂具有生物等效性。

Aim To evaluate the bioequivalence of voriconazole capsules and tablets in Chinese healthy volunteers. Methods A single oral dose （200mg） of voriconazole capsule or tablet was given to 24 healthy volunteers respectively in a randomized cross-over study. The concentration of voriconazole in plasma was determined by LS-MS- MS method developed in our laboratory. Results The main pharmacokinetic parameters of voriconazole capsules and tablets were as follows： Tmax was（0.93 ±0.46）and（0.94 ±0.54）h; Cmax was（2 340. 83 ±607.95）and （1 950.83 ± 656.25）μg·L^-1; t1/2 was （8.59 ±3.53）and（8.81 ±4. 16）h;AUC0-tn was （11 529.38 ±6 501.42）and （10 217.92 ±5 428.32） μg·h·L^-1 ,AUC0-∞ was （12 779.70 ±8 020. 12）and （11 404.55 ±7 156.16）μg·h·L^-1; Relative bioequivalence F0-tn and F0-∞ was （ 114.08 ± 20.92） % and （ 113.84 ± 22.50 ） %, respectively. Conclusion The two preparations are bioequivalent.