匹多莫德糖浆在健康人体的药动学和生物等效性评价

Pharmacokinetics and Bioequivalence of Pidotimod Syrup in Healthy Volunteers

目的:研究匹多莫德糖浆的人体相对生物利用度和生物等效性。方法:健康志愿者20名,随机双交叉单剂量口服匹多莫德糖浆(受试制剂)和溶液(参比制剂),剂量分别为20 ml(800 mg)和14 ml(800 mg),采用HPLC法测定血浆中匹多莫德的浓度,用DAS2.1药动学程序计算药动学参数和生物利用度,并进行生物等效性评价。结果:单剂量口服匹多莫德受试和参比制剂后,血浆匹多莫德的C_(max)分别为(4.45±1.80)μg·ml^(-1)和(5.17±1.57)μg·ml^(-1),t_(max)分别为(2.28±0.550)h和(2.18±0.61)h,t_(1/2)分别为(2.27±1.07)h和(1.98±0.77)h,AUC_(0-14)分别为(21.77±6.48)μg·h·ml^(-1)和(21.13±5.30)μg·h·ml^(-1),AUC_(0-∞)分别为(22.28±6.48)μg·h·ml^(-1)和(21.56±5.36)μg·h·ml^(-1)。AUC_(0-14)、AUC_(0-∞)和C_(max)的90%可信区间分别为89.2%～116.4%,89.8%～116.9%和74.8%～94.2%。受试制剂的相对生物利用度F_(0-14)和F_(0-∞)分别为(107.69±37.25)%和(108.20±37.13)%。结论:匹多莫德受试制剂和参比制剂具有生物等效性。

Objective： To study the relative bioavailability and bioequivalenee of pidotimod syrup in healthy volunteers. Method： A single oral dose of pidotimod （800 mg test and referenee preparations） were given to 20 male healthy volunteers in a randomized erossover study. The concentration of pidotimod in plasma was determined by HPLC. The pharmaeokinetie parameters were calculated and the relative bioavailability and bioequivalenee of two formulations were evaluated by DAS ver2. 1 program. Result： After a single dose,the pharmaeokinetie parameters of the test and reference pidotimod were as follows： Cmax （4. 45 ±1.80） μg.ml^-1 and（5.17± 1.57）μg·ml^-1 ,tmax （2.28±0. 550） h and（2. 18 ±0. 61 ） h,t1/2 （2. 27±1.07） h and （ 1.98 ±0. 77） h,AUC0-14 （21.77 ±6. 48） μg·h·ml^-1 and （21.13 ±5.30） μg·h·ml^-1 ,AUC0-∞ （22.28±6.48） μg·h·ml^-1and （21.56 ±5.36） μg·h·ml^-1,respectively. The 90% confidential interval of AUC0-t ,AUC0-∞ and Cmax were 89. 2%-116. 4% ,89. 8%-116. 9% and 74. 8%-94. 2% , respectively. The relative bioavailability was （108.20 ±37.13）%. Conclusion： The results of the statistic analysis showed that the two formulations were bioequivalent.