枸橼酸托烷司琼注射液人体药代动力学研究

Comparative Experiment of In Vivo Pharmacokinetics of Tropisetron Citrate Injection and Tropisetron Hydrochloride Injection

目的研究枸橼酸托烷司琼注射液在健康志愿者体内的生物利用度及生物等效性。方法20名健康志愿者按体重随机、配对交叉静脉滴注试验制剂枸橼酸托烷司琼注射液和参比制剂盐酸托烷司琼注射液,剂间间隔为1周,剂量均为5 mg∶5 mL。采用液相色谱-质谱/质谱联用法测定血清中托烷司琼的质量浓度。结果健康志愿者静脉滴注试验制剂和参比制剂的最大血药浓度(Cmax)分别为(41.244±11.457)ng/mL和(39.580±11.902)ng/mL,达峰时间(Tmax)分别为(0.467±0.136)h和(0.487±0.087)h,0～48 h药时曲线下面积(AUC0-48)分别为(178.887±85.675)ng.h/mL和(172.815±86.248)ng.h/mL,0～∞药时曲线下面积(AUC0-∞)分别为(191.055±90.297)ng.h/mL和(183.626±94.120)ng.h/mL,半衰期(t1/2)分别为(8.756±3.267)h和(8.101±3.819)h。结论枸橼酸托烷司琼注射液和盐酸托烷司琼注射液在健康志愿者体内的药代动力学参数相似,具有生物等效性。

Objective To investigate the bioavailability and the bioequivalence of Tropisetron Citrate Injection in healthy volunteers. Methods Twenty healthy volunteers were intravenously dripped with the test preparation Tropisetron Citrate Injection and the reference preparation Tropisetron Hydrochloride Injection according to the bodyweight by the pairing randomized cross way, at a dose of 5 mg： 5 mL and the inter-dose interval of 1 week. The plasma drug concentrations were determined by LC- MS/MS. Results The pharma- cokinetic parameters of the test preparation and the reference preparation were as follows： Cmax was （41.244±ll.457）ng/mL and （39.580＋11.902） ng/mL; Tmax was （0.467＋0.136） h and （0.487±0.087） h; AUCo-48 was （178.887±85.675） ng h/mL and （172. 815 ±86. 248）ngh/mL; AUCo-∞ was （191. 055±90. 297）ng h/mL and （183. 626 ±94. 120）ng h/mL; was （8. 756 ±3. 267） h and （8. 101 ±3. 819） h, respectively. Conclusion The test preparation Citrate Tropisetron Injection and the reference prepration Tropisetron Hydrochloride Injection have similar in vivo pharmacokinetic parameters in healthy volunteers and possess the bioequivalence.