盐酸格拉司琼口崩片在健康人体内的药动学及生物等效性

Pharmacokinetics and Bioavailability of Granisetron Hydrochloride Tablets in Healthy Volunteers

研究了盐酸格拉司琼口崩片的药动学,并以盐酸格拉司琼片为参比制剂,评价其生物等效性。20例健康志愿者单剂量随机交叉口服受试制剂和参比制剂各1mg,用HPLC-荧光法测定血药浓度。受试制剂与参比制剂的主要药动学参数分别为cmax(3.32±0.93)和(3.20±0.86)ng/ml,tmax(1.65±0.52)和(1.88±0.86)h,t1/2(6.16±0.90)和(6.22±0.81)h,AUC0→t(19.50±8.10)和(19.70±7.78)ng·h·ml-1,AUC0→∞(20.90±9.11)和(21.10±8.57)ng·h·ml-1。受试制剂的相对生物利用度为(99.8±15.3)%,结果表明两种制剂具有生物等效性。

The pharmacokinetics of granisetron hydrochloride orally disintegrating tablets （test preparation） and its related bioavailability to granisetron hydrochloride tablets （reference preparation） are discussed. According a single dose crossover design, 20 healthy volunteers were administrated with lmg of test and reference preparations. The plasma concentrations were determined by HPLC-fluorescence detector. The pharmacokinetic parameters of the test and reference preparations were as follows： Cmax （3.32±0.93） and （3.20±0.86） ng/ml, tmax （1.65±0.52） and （1.88±0.86） h, t1/2 （6.16±0.90） and （6.22±0.81） h, AUC0→t （19.50±8.10） and （19.70±7.78） ng·h·ml^-1,AUC→∝ （20.90±9.11） and （21.10± 8.57） ng·h·ml^-1. The relative bioavailability of the test preparation was （99.8±15.3） %. The result showed that the two preparations were bioequivalent.