国产和进口盐酸格拉司琼片人体药物动力学和相对生物利用度

Pharmacokinetics and relative bioavailability of granisetron hydrochloride tablets in healthy volunteers

目的 :比较国产和进口盐酸格拉司琼片 (Gra)的药物动力学和生物利用度。方法 :按照随机交叉试验方法研究了国产及进口 Gra片在 9名男性自愿者中的药物动力学和相对生物利用度。 po单剂量 2 mg上述两种制剂 ,采用 HPL C-荧光检测法测定给药后不同时间的血药浓度。结果 :国产片和进口片的 tmax分别为 (1.45± 0 .98)和 (1.2 9± 0 .5 2 ) h;cmax分别为 (7.2 3±1.94)和 (6 .78± 2 .86 ) ng/ m l;T1 /2 分别为 (5 .33± 2 .6 5 )和 (5 .43± 2 .32 ) h;Vd 分别为 (2 36 .3± 79.2 5 )和 (30 8.8± 15 4.9) L ;CL分别为 (30 .7± 5 .2 )和 (39.4± 5 .7) L / h;MRT分别为 (6 .41± 2 .10 )和 (6 .73± 1.75 ) h;AU C0→∞ 分别为 (70 .5 5± 5 0 .19)和(6 8.0 9± 42 .6 8) ng· h/ m l。经配对 t检验上述参数差异均无显著意义 (P>0 .0 5 )。国产片相对于进口片的生物利用度为(10 2 .45± 16 .91) %。结论 :2种制剂具有生物等效性。

AIM: To compare the pharmacokinetics and relative bioavailability of domestic and imported granisetron hydrochloride tablets. METHODS: The pharmacokinetics and relative bioavailability of domestic granisetron hydrochloride in tablets after oral administration were determined with a balance cross over study in 9 healthy male volunteers in comparison with imported granisetron hydrochloride in tablets. Each volunteers received 2 single doses (2 mg) grsnisetron tablet, 1 domestic and 1 imported. The granisetron in plasma was detected by high performance liquid chromatography (HPLC). RESULTS: The pharmacokinetic parameters of domestic and imported granisetron hydrochloride tablets were as follows ( ±s ): t max was (1 45±0 98) and (1 29±0 52) h; c max was (7 23±1 94) and (6 78±2 86) ng/ml, T 1/2 was (5 33±2 65) and (5 43±2 32) h, V d was (236 3±79 25) and (308 8±154 9) L, CL was (30 7±5 2) and (39 4±5 7) L/h, MRT was (6 41±2 10) and (6 73±1 75) h, and AUC 0→∞ was (70 55±50 19) and (68 09±42.68) ng·h/ml, respectively. All the parameters were not different with statistic significance examined by paired t test ( P >0 05). The relative bioavailabitity of domestic granisetron hydrochloride tablet in comparison with imported granisetron hydrochloride tablet was (102 45±16 91)%. CONCLUSION: The results show that the 2 products are bioequivalent.