注射用胸腺肽-α_1在健康人体的生物等效性研究

Bioequivalence of Thymosin Alpha 1 for injection in healthy Chinese subjects

目的研究国产的注射用胸腺肽-α1在健康人体的药物动力学,并评价其与同剂量的进口参比制剂的生物等效性。方法采用双周期交叉试验设计,20名男性健康受试者分别给予单剂量皮下注射试验制剂或参比制剂1.6mg。采用HPLC-MS/MS法测定给药后各时间点采集血样的血药浓度,计算主要药物动力学参数,以进口制剂为参比制剂,计算其相对生物利用度,判断其生物等效性。结果试验制剂中胸腺肽-α1的主要药物动力学参数Cmax为90.95±35.05μg.L-1;tmax为1.8±0.4 h;AUC0→12为435.4±192.8μg.h.L-1;t1/2为3.9±1.2 h。参比制剂中胸腺肽-α1的主要药物动力学参数Cmax为90.77±35.45μg.L-1;tmax为1.9±0.4 h;AUC0→12为427.6±187.8μg.h.L-1;t1/2为3.9±1.3 h。受试制剂的相对生物利用度F为101.7%±8.0%。结论2种制剂具有生物等效性。

OBJECTIVE To evaluate the pharmacokineties and bioequivalenee between native and foreign Thymosin Alpha 1 for injection in the healthy Chinese subjects. METHODS According to a randomized cross-over design, a single dose of 1.6 mg of subcutaneous injection （test or reference preparation） was given to 20 Chinese healthy young volunteers. Blood samples were collected at serial interval for a period of 12 h after the injection and the day befor injection. Thymosin Alpha 1 concentration in the plasma was analyzed by HPLC-MS/MS. The pharmaeokineties parameters of native preparation were analyzed to estimate the bioequivalenee to foreign preparation. RESULTS The main pharmacokinetie parameters of the test drug and reference drug were as follows： tmax （1.8±0. 4）h and （1. 9±0. 4）h; Cmax（90.95±35.05）μg·L^-1 and （90.77±35.45）μg·L^-1; t1/2（3.9±1. 2）hand （3.9±1.3）h; AUC0→12 （435.4±192.8）μg·h·L^-1 and （427.6±187.8）μg·h·L^-1 respectively. The relative bioavailability of Thyrnosin Alpha 1 was 101.7 % ± 8.0 %. CONCLUSIONS The bioequivalence of Thyrnosin Alpha 1 was consistent between the test drug and the reference drug.