【摘要】 目的研究厄贝沙坦氢氯噻嗪胶囊(抗高血压药)在健康人体的生物等效性。方法 22名健康志愿者,随机双交叉单剂量口服厄贝沙坦氢氯噻嗪胶囊(试验制剂)和厄贝沙坦氢氯噻嗪片(参比制剂),剂量为厄贝沙坦300 mg、氢氯噻嗪25 mg。分别于服药后36 h内,多点抽取静脉血,用高效液相色谱法分别测定血浆中厄贝沙坦和氢氯噻嗪的浓度。用DAS程序计算相对生物利用度,并评价2种制剂生物等效性。结果单剂量口服厄贝沙坦氢氯噻嗪胶囊和片剂后的药代动力学参数,厄贝沙坦:Cmax分别为(2.61±0.62)和(2.57±0.46)mg·L-1;AUC0-36分别为(15.14±3.43)和(15.39±3.91)mg·h·L-1;AUC0-∞分别为(16.37±3.42)和(16.80±4.28)mg·h·L-1;相对生物利用度为(100.75±19.42)%。氢氯噻嗪:Cmax分别为(162.51±27.55)和(168.18±25.71)μg·L-1;AUC0-36分别为(1115.41±147.34)和(1144.15±171.62)μg·h·L-1;AUC0-∞分别为(1212.68±160.77)和(1252.75±211.27)μg·h·L-1;相对生物利用度为(98.53±13.35)%。结论 2种制剂具有生物等效性。更多还原

【Abstract】 Objective To study the bioequivalence of irbesartan and hydrochlorothiazide capsules in healthy volunteers.Methods A single oral dose of test and reference formulations were given to 22 healthy volunteers in a randomised crossover study.The concentrations of irbesartan and hydrochlorothiazide in plasma were determined by HPLC,respectively.The pharmacokinetic parameters were calculated and the bioavailability and bioequivalence of irbesartan and hydrochlorothiazide were evaluated by DAS program,respectively.Results After a single dose,the pharmacokinetic parameters of irbesartan for test and reference formulations were as follows: Cmax were(2.61±0.62) and(2.57±0.46) mg·L-1;AUC0-36 were(15.14±3.43) and(15.39±3.91) mg·h·L-1;AUC0-∞ were(16.37±3.42) and(16.80±4.28) mg·h·L-1,respectively.The relative bioavailability of irbesartan was(100.75±19.42)%.The pharmacokinetic parameters of hydrochlorothiazide for test and reference formulations were as follows: Cmax were(162.51±27.55) and(168.18±25.71) μg·L-1;AUC0-36 were(1115.41±147.34) and(1144.15±171.62) μg·h·L-1;AUC0-∞ were(1212.68±160.77) and(1252.75±211.27) μg·h·L-1,respectively.The relative bioavailability of hydrochlorothiazide was (98.53±13.35)%.Conclusion The results of the statistic analysis showed that the two formulations were bioequivalence.更多还原