磷酸川芎嗪滴丸在健康人体的药代动力学和生物等效性

Pharmacokinetics and bioequivalence of Ligustazine phosphate pills in healthy volunteers

目的 研究单次口服磷酸川芎嗪(LTP)滴丸或片后的药代动力学及其生 物等效性。方法 用自身交叉2周期设计,20名健康男性志愿者单次口服LTP 滴丸或片,用HPLC紫外检测、外标法定量测定药物浓度,用BAPP2．0软件包计 算2制剂的药代动力学参数并进行生物等效性评价。结果 LTP滴丸或LTP 片在人体内的吸收、分布、代谢行为相似,2者的Cmax分别为(4．50±0．96), (4．45±1．69)μg·mL-1;tmax分别为(0．5±0．2),(0．8±0．3)h;t1／2分别为(1．32 ±0．24),(1．30±0．22)h;MRT分别为(1．94±0．26),(2．02±0．22)h;AUC0-8 分别为(6．88±1．71),(6．71±1．25)μg·h·mL-1;AUC0-∞分别为(7．01± 1．76),(6．82±1．27)μg·h·ml-1,LTP滴丸的相对生物利用度为(102．7± 18．6)％。经方差分析和双单侧检验,无显著性差异(P>0．05)。结论 2制剂 为生物等效制剂。

Objective To study the pharmacokinetics and bioequivalence of Ligustazine phosphate pills （test） and its tablet （reference） in 20 Chinese healthy male volunteers. Methods A single oral dose 300 mg Ligustazine phosphate of test or reference formulations was given to each volunteer according to an open randomized crossover design. The Ligustazine phosphate concentrations in serum were determined by HPLC with UV detection method. The pharmacokinetic parameters were determined by BAPP 2. 0 program and bioequivalence were compared. Results The main pharmacokinetic parameters of Ligustazine phosphate were as the following- Cmax were （4. 50 ± 0. 96） and （4. 45 ± 1.69） μg·mL^-1, tmax were （0. 5 ± 0.2） and （0.8 ±0.3） h, t1/2 were （1.32±0.24） and （1.30 ±0.22）h, MRT were （1.94±0.26） and （2.02 ±0.22）h, AUC0-8 were （6.88 ±1.71） and （6.71 ±1.25） μg·h·mL^-1, AUC0-∞ were （7.01 ±1.76） and （6.82 ± 1.27 ）μg·h·mL^-1 for test and reference, respectively. The relative bioavailability of test to reference drug were （ 102.7 ± 18.6 ） %. Conclusion The results of statistical analysis showed that two formulations were bioequivalent.