盐酸特拉唑嗪口腔崩解片人体生物等效性研究

Pharmacokinetics and bioequivalence of terazosin orally disintegrating tablets

目的研究特拉唑嗪口腔崩解片在健康人体内的药动学行为,并以胶囊剂为参比进行生物等效性评价。方法采用液质联用(LC-MS-MS)法测定服药后受试者血浆中特拉唑嗪的质量浓度并计算主要药动学参数。结果 18名受试者口服含盐酸特拉唑嗪2 mg的受试制剂和参比制剂后,血浆中特拉唑嗪的tmax为(1.3±0.8)、(1.2±0.8)h,ρmax为(62.9±20.4)、(62.0±15.3)μg.L-1,t1/2为(10.2±1.3)、(10.7±1.3)h,AUC0-t为(556.3±162.6)、(584.2±124.2)μg.h.L-1,AUC0-∞为(576.4±169.9)、(611.7±126.5)μg.h.L-1。以AUC0-t计算,盐酸特拉唑嗪口腔崩解片中特拉唑嗪的相对生物利用度为(96.2±22.4)%。结论受试制剂和参比制剂具有生物等效性。

Objective To study the pharmacokinetics and bioequivalence between two kinds of terazosin tablets in healthy volunteers. Methods A single oral dose of two kinds of terazosin tablets was given to 18 healthy volunteers in a randomized two-period crossover study. The concentrations of terazosin in plasma were determined by the liquid chromatography tandem mass spectrometry （LC-MS-MS）. The plasma concentration-time curves were plotted and the main pharmacokinetic parameters were calculated. Results The main pharmacokinetic parameters of test and reference tablets in plasma were shown as follows ： tmax were （1.3 ±0.8） and （1.2 ±0. 8）h,ρmax were （62.9±20.4） and （62.0 ± 15.3） μg·L^-1,t1/2 were （10.2 ± 1.3 ） and （ 10. 7 ± 1.3 ） h, AUC0-t were （ 556. 3 ± 162. 6 ） and （ 584. 2 ± 124. 2 ） μg·h·L^-1, AUC0-∞ were （576. 4 ± 169.9） and （ 611.7 ± 126.5 ） μg·h·L^-1, respectively. The relative bioavailability of the tested drug was （96. 2 ± 22.4） %. Conclusions The two kinds of terazosin formulations are bioequivalent in healthy volunteers.