盐酸格拉司琼胶囊的人体药物动力学和相对生物利用度

目的 :研究盐酸格拉司琼胶囊在健康人体内的药物动力学和相对生物利用度。方法 :12名健康男性志愿受试者单剂量口服盐酸格拉司琼胶囊或市售片 12 mg后 ,采用高效液相色谱法测定血浆中格拉司琼浓度。结果 :经 3P87药物动力学程序处理 ,以格拉司琼胶囊和片剂的 AUC0→ t分别为 (133.7± 6 1.8)、(131.1± 5 7.4) ng· h/m l;AUC0→∞ 分别为 (15 0 .9± 6 9.8)、(15 0 .6± 6 7.5 ) ng· h/m l,tmax分别为 (2 .9± 0 .4)、(2 .9± 0 .3) h,cmax分别为 (2 4.6± 9.3)、(2 4.6± 8.7) ng/ml。经配对 t检验两种盐酸格拉司琼制剂的 AU C及 cmax无显著性差异 (P>0 .0 5 )。以盐酸格拉司琼片为标准参比制剂 ,盐酸格拉司琼胶囊的相对生物利用度为 F0→ t(10 1.5± 11.2 ) % ;F0→∞ (10 0 .2± 13.5 ) %。结论 :盐酸格拉司琼胶囊和片剂为生物等效制剂。

Pharmacokinetics and relative bioavailability of granisetron hydrochloride capsules in healthy volunteers

AIM: To study the pharmacokinetics and relative bioavailabilityof granisetron hydrochloride capsules and tablets in healthy volunteers. METHODS: The granisetron hydrochloride concentration in serum was determined by high performance liquid chromatography (HPLC) method after a single oral dose (12 mg) of capsule or tablet was administered to 12 healthy male volunteers respectively in an open randomized cross-over test. RESULTS: After being processed by 3P87 pharmacokinetic program, the experiment data showed that the pharmacokinetic parameters of the capsules and the tablets were AUC0→t: (133.7±61.8) and (131.1±57.4) (ng.h)/ml；AUC0→∞: (150.9±69.8) and (150.6±67.5) (ng.h)/ml；tmax: (2.9±0.4) and (2.9±0.3) h；cmax: (24.6±9.3) and (24.6±0.7) ng/ml respectively. There were no significant differences between AUC and cmax of these 2 preparations (P＞0.05). The relative bioavailability of granisetron hydrochloride capsules was F0→t: (101.5±11.2)% and F0→∞: (100.2±13.5)%. CONCLUSION: These 2 preparations are bioequivalent.