盐酸依匹斯汀片在健康人体的药代动力学和相对生物利用度

Pharmacokinetics and relative bioavailiability of epinastine hydrochloride tablets in Chinese healthy volunteers

目的研究国产和进口盐酸依匹斯汀片(抗组胺药)在健康人体的药代动力学和相对生物利用度,并进行生物等效性评价。方法20名男性健康志愿者随机交叉单剂量口服国产和进口盐酸依匹斯汀片40mg后,用反相高效液相色谱法测定血浆盐酸依匹斯汀浓度,用DAS软件计算其药代动力学参数。结果2种制剂在人体的药时曲线均符合二室开放模型,主要药代动力学参数:t1/2分别为(10.12±1.28)和(10.43±2.44)h;tmax分别为(2.18±0.47)和(2.03±0.41)h;Cmax分别为(65.90±16.45)和(68.17±13.25)μg·L-1;AUC0-36分别为(591.63±88.22)和(600.90±93.74)μg·L-1.h;AUC0-∞分别为(647.04±101.58)和(657.96±87.56)μg·L-1.h。与进口制剂比较,国产制剂的相对生物利用度F0-36为(99.40±12.77)%;F0-36为(98.85±13.72)%。结论国产和进口制剂具有生物等效性。

Objective To study the pharmacokinetics and relative bioavailability of epinastine hydroehloride tablets in Chinese healthy volunteers and to evaluate the bioequivalenee. Methods A single oral dose of 40 mg epinastine hydroehloride test and reference tablets were given to 20 male healthy volunteers in a randomized, two - way crossover study. Plasma epinastine hydroehloride concentrations were determined by RP- HPLC method. The pharmaeokinetie parameters and relative bioavailability were calculated with DAS software to evaluate the bioequivalenee of the two preparations. Results The plasma concentration - time course followed a two -compartment open model and its main pharmaeokinetie parameters of test and reference preparations were as follows： t（1/2） were （10.12±1.28） and （10.43 ±2.44）h; tmax were （2. 18 ±0.47） and （2.03 ± 0.41 ） h ; Cmax were （ 65.90 ± 16.45 ） and （ 68. 17 ± 13.25 ）μg·L^-1 ; AUC（0-36） were （591.63 ± 88.22） and（600.90 ±93.74）μg·L^-1; AUC（0-∞） were（647.04 ± 101.58）and （657.96 ±87.56） μg·h·L^-1 , respectively. The relative bioavailability of F（0-36） and F（0-∞） were （99.40 ± 12.77） % and （98.85 ± 13.72） %, respectively. Conclusion The domestic and imported preparations are bioequivalent.